Product Name:
Synonym:
Definition: Pine Bark Extract are majorly composed of
Chemical information disclosed as following table:
Research update of Pine Bark Extract Proanthocyanidins related.:
Phlebotonics for venous insufficiency.:MJ Martinez
Background:Chronic venous insufficiency (CVI) is a common condition caused by inadequate blood flow through the veins, usually in the lower limbs. It can result in considerable discomfort with symptoms such as pain, itchiness and tiredness in the legs. Sufferers may also experience swelling and ulcers. Phlebotonics are a class of drugs that are often used to treat CVI.
Objectives:To assess the efficacy of oral or topical phlebotonics.
Search strategy:We searched the Cochrane Peripheral Vascular Diseases Group trials register (April 2005), the Cochrane Central Register of Controlled Trials ( Issue 2, 2005), MEDLINE (January 1966 to April 2005), EMBASE (January 1980 to April 2005) and reference lists of articles. We also contacted pharmaceutical companies.
Selection criteria:Randomised, double blind, placebo ¨C controlled trials (RCTs) assessing the efficacy of rutosides, hidrosmine, diosmine, calcium dobesilate, chromocarbe, centella asiatica, disodium flavodate, french maritime pine bark extract, grape seed extract and aminaftone in CVI patients at any stage of the disease.
Data collection and analysis:Two reviewers independently extracted data and assessed trial quality. The effects of treatment were estimated by relative risk (RR) or by standardised mean differences (SMD) by applying a random effects statistical model. Sensitivity analyses were also performed.
Main results:Fifty ¨C nine RCTs of oral phlebotonics were included, but only 44 trials involving 4413 participants contained quantifiable data for the efficacy analysis: 23 of rutosides, ten of hidrosmine and diosmine, six of calcium dobesilate, two of centella asiatica, one of french maritime pine bark extract, one of aminaftone and one of grape seed extract. No studies evaluating topical phlebotonics, chromocarbe, naftazone or disodium flavodate fulfilled the inclusion criteria.
Outcomes included oedema, venous ulcers, trophic disorders, subjective symptoms (pain, cramps, restless legs, itching, heaviness, swelling and paraesthesias), global assessment measures and side effects. The results of many variables were heterogeneous. Phlebotonics showed some global benefit (i.e. oedema reduction) (relative risk 0.72, 95% confidence interval 0.65 to 0.81). The benefit for the remaining CVI signs and symptoms must be evaluated by phlebotonic group. There were no quantifiable data on quality of life.
Authors' conclusions:There is not enough evidence to globally support the efficacy of phlebotonics for chronic venous insufficiency. There is a suggestion of some efficacy of phlebotonics on oedema but this is of uncertain clinical relevance. Due to the limitations of current evidence, there is a need for further randomised, controlled clinical trials with greater attention paid to methodological quality.
Pine Bark Extract May Prevent Leg Clots.:
SOURCES: Cesarone, M.R. Clinical and Applied Thrombosis/Hemostasis, July 2005; vol 11: pp T1-T3. American Heart Association. Peter Rohdewald, PhD, Institute of Pharmaceutical Chemistry, University of Muenster.
Aug. 12, 2005 -- A supplement derived from French maritime pine bark may help reduce the risk of developing leg clots during long air flights.
Deep vein thrombosis (DVT) occurs as a result of the blood's circulation being restricted. Long periods of inactivity or immobility, dehydration, and low humidity and low cabin pressure that occur during air flights also cause DVTs. Because leg room and seating on airplanes is cramped DVT is frequently called economy-class syndrome.
Researchers show that the French maritime pine bark extract called Pycnogenol reduces leg swelling (edema) caused by lack of movement, which can increase the risk of DVTs during airplane flights lasting seven to 12 hours.
"Pycnogenol showed effectiveness in improving circulation and helping to prevent leg and ankle swelling," says researcher Peter Rohdewald, PhD, in a news release. "Most people will notice the effects of in-flight swelling if they take their shoes off during the flight and have difficulty getting back into them at the end of the flight. Leg and ankle swelling can lead to dangerous conditions such as deep vein thrombosis (DVT)."
Pycnogenol is a natural plant extract that originates from the bark of the Maritime pine that grows along the coast of southwest France.
Risk of DVT:
Small clots from a DVT can break off and travel to the lungs with the potential to cause life- threatening pulmonary embolisms -- lung clots that interfere with breathing.
Of the 2 million Americans who develop DVT each year, about 200,000 die, according to the American Heart Association.
Fortunately, a clot in most cases will dissolve on its own before it can affect blood flow and people are never aware they were even in danger.
Some people are at greater risk for developing DVT. Those with a history of heart disease or those who have developed blood clots in the past are especially vulnerable. That's not to say they're the only ones who can be affected. Younger people, and even athletes, are also at risk.
Reducing Risks of DVT:
In the study, which involved 169 participants, researchers show that oral Pycnogenol was effective not only in improving circulation but also in preventing leg and ankle swelling that frequently follows long airline flights.
Before the flight, ankle size was measured and assigned a score. Similar scores were found among participants given Pycnogenol and a comparison group before the flights.
After the flight those not treated with Pycnogenol had almost double the ankle-swelling score of those who received Pycnogenol.
"Our study shows that Pycnogenol prevents swellings by strengthening the venous walls," says Rohdewald.
Preventative Measures:
According to researchers, the veins' compression on the edge of the airplane seat may contribute to leg and ankle swelling and DVT. The risk is compounded by long periods of immobility, decreased fluid intake, and water loss in the airplane cabins, which are dry and compressed, they say.
There are certain preventative measures that can be taken during long flights. The idea is to get your circulation faster during flights to prevent the blood from becoming stagnant. Avoid excess alcohol during flights. Every hour, get up and walk the aisle or stand next to your seat. Perform knee and leg lifts, pointing your toes down and up. Also, make sure to stay well hydrated.
According to the American Heart Association, these steps aren't scientifically proven to prevent blood clots during long flights but they're common sense.
Treatment of Melasma With Pycnogenol.:
Ni Z, Mu Y, Gulati O.Phytother Res. 2002;16:567-571
Melasma (or chloasma) is a common disorder of cutaneous hyperpigmentation predominantly affecting sun-exposed areas in women. The pathogenesis of melasma is not fully understood and treatments are frequently disappointing and often associated with side effects. Pycnogenol is a standardized extract of the bark of the French maritime pine (Pinus pinaster), a well-known, potent antioxidant. Studies in vitro show that Pycnogenol is several times more powerful than vitamin E and vitamin C. In addition, it recycles vitamin C, regenerates vitamin E and increases the endogenous antioxidant enzyme system. Pycnogenol protects against ultraviolet (UV) radiation. Therefore its efficacy in the treatment of melasma was investigated. Thirty women with melasma completed a 30-day clinical trial in which they took one 25 mg tablet of Pycnogenol with meals three times daily, i.e. 75 mg Pycnogenol per day. These patients were evaluated clinically by parameters such as the melasma area index, pigmentary intensity index and by routine blood and urine tests. After a 30-day treatment, the average melasma area of the patients decreased by 25.86 ¡À 20.39 mm(2) (p < 0.001) and the average pigmentary intensity decreased by 0.47 ¡À 0.51 unit (p < 0.001). The general effective rate was 80%. No side effect was observed. The results of the blood and urine test parameters at baseline and at day 30 were within the normal range. Moreover, several other associated symptoms such as fatigue, constipation, pains in the body and anxiety were also improved. To conclude, Pycnogenol was shown to be therapeutically effective and safe in patients suffering from melasma.
Pine Bark Extract May Effectively Treat ADHD in Boys.:News Author: Laurie Barclay, MD.CME Author: Penny Murata, MD
June 23, 2006 ¡ª Pine bark extract (Pycnogenol) is effective for treating attention-deficit/hyperactivity disorder (ADHD), at least in boys, according to the results of a randomized trial reported in the May 13 Online First issue of European Child & Adolescent Psychiatry.
"These findings are especially notable for parents who are concerned about overmedicating children diagnosed with ADHD," coauthor Peter Rohdewald, MD, from the University of Munster in Germany, said in a news release. "Many families are seeking natural options to avoid the potentially dangerous side effects of prescription drugs."
Pycnogenol, an extract from the bark of the French maritime pine, consisting of phenolic acids, catechin, taxifolin and procyanidins, was associated with improvement of ADHD in case reports and in an open-label study.
In this double-blind trial, 61 children with ADHD were randomized 2:1 to receive 1 mg/kg/day pine bark extract or placebo for 4 weeks. Average age was 9.5 years. Standard questionnaires including Child Attention Problems (CAP) teacher rating scale, Conner's Teacher Rating Scale (CTRS), Conner's Parent Rating Scale (CPRS), and the modified Wechsler Intelligence Scale for Children were administered at the start of the trial, 1 month after starting treatment, and 1 month after completing treatment.
The pine bark extract group had a significant reduction in hyperactivity and improved attention, visual-motor coordination, and concentration, whereas there were no positive effects noted in the placebo group. One month after pine bark extract treatment ceased, patients had recurrence of symptoms. Treatment was not significantly effective for girls in contrast to boys, but there were only 6 girls in the pine bark extract group.
"The results of this study show Pycnogenol may serve as a safe, effective treatment for children diagnosed with ADHD," Dr. Rohdewald says. "French maritime pine bark extract reduced hyperactivity among study participants, while improving attention and visual-motor coordination and concentration of these children."
However, the authors note that their findings should be further confirmed by studies involving a greater number of patients, especially girls, and for a longer duration of treatment. Although the underlying mechanism is still unknown, urinalysis revealed a lower excretion of catecholamines in the pine bark extract group than in the placebo group, suggesting an influence of pine bark extract on catecholamine formation or metabolism.
"ADHD is affecting the quality of life for so many children and their families," Dr. Rohdewald concludes. "It is imperative that science explores natural means to provide expanded treatment options. We look forward to advancing this promising research."
Horphag Res. Ltd., VEGA, Ministry of Education of SR, Drug Research Institute, Modra, and Mind & Health supported this study.
Eur Child Adolesc Psychiatry. Posted online May 13, 2006.
Learning Objectives for This Educational Activity
Upon completion of this activity, participants will be able to:
Explain the effects of pine bark extract on hyperactivity, inattention, and motor-visual coordination in children with ADHD.
List adverse effects of pine bark extract on children with ADHD.
Clinical Context:
Children with ADHD are often treated with stimulant medication. Studies have been performed to evaluate the efficacy of pine bark extract in the treatment of ADHD. Pycnogenol, extracted from the bark of French maritime pine (Pinus pinaster), consists of procyanidins, phenolic acids, catechin, and taxifolin. In the October 21, 2000, issue of Mainichi Shimbun, Masao reported 70% success rate for pine bark extract treatment of children with ADHD. But a September 2002 study in the Journal of Attention Disorders by Tenenbaum and colleagues found no significant differences among adults with ADHD treated with placebo, methylphenidate, or pine bark extract. Trebatick¨¢ and colleagues reported results of a pilot study in 2004 that showed pine bark extract at a dose of 1 mg/kg/day improved ADHD symptoms.
The current trial is a randomized, double-blind, placebo-controlled study to evaluate the effect of pine bark extract treatment on ADHD symptoms in children.
Study Highlights:
61 children ages 6 to 14 years who met ADHD diagnostic criteria were enrolled: 44 had hyperkinetic disorder; 11 had hyperkinetic conduct disorder; 6 had attention deficit without hyperactivity; and 18 had additional specific learning disabilities.
Exclusion criteria included situational hyperactivity, pervasive developmental disorders, psychotic disorders, medical condition causing personality change, mental retardation, understimulating environments, conduct disorder, tics, dyskinesias, acute inflammatory diseases, renal disorder, cardiovascular disorders, and diabetes.
44 children were randomized to receive 1 mg/kg/day of pine bark extract, and 17 were randomized to receive placebo (58 mg of lactose and 65 mg of cellulose per tablet) every morning for 1 month; no other drugs were taken.
57 patients completed the study. 3 pine bark extract patients and 1 placebo patient withdrew.
Patient characteristics included average age of 9.5 years; male/female number, 37/7 in pine bark extract group and 13/4 in placebo group.
Patients were evaluated at baseline, after 1 month of treatment, and 1 month after treatment completion.
Evaluations consisted of psychiatric examination; teacher rating of inattention and hyperactivity by CAP teacher rating scale and CTRS; parent rating of inattention and hyperactivity by CPRS; psychologist weight score, a sum of values of 5 subtests of Performance Scale on Prague Wechsler Intelligence Scale for children (modified Wechsler Intelligence Scale).
CAP scores for inattention decreased significantly in pine bark extract group at 1 month vs pine bark extract group at baseline (P = .00014) and vs placebo group at 1 month (P = .0067) but returned to baseline at 1 month after treatment ended.
CAP scores for hyperactivity decreased significantly in pine bark extract group at 1 month vs pine bark extract group at baseline (P = .008) and vs placebo group at 1 month (P = .044) but returned to baseline at 1 month after treatment ended.
CTRS score results for inattention improved in pine bark extract group at 1 month vs placebo (P = .049) but did not improve vs pine bark extract group at baseline.
CTRS score results for hyperactivity did not significantly improve for pine bark extract group at 1 month vs pine bark extract group at 1 month or placebo group at 1 month.
CPRS scores for inattention and hyperactivity did not change significantly after 1 month of pine bark extract treatment.
Weight scores based on tests for visual-motor coordination and concentration improved in pine bark extract group at 1 month vs pine bark extract group at baseline (P = .019) and vs placebo at 1 month (P = .05); high scores persisted at 1 month after treatment ended.
Results of bilirubin, glucose, gamma-glutamyl transferase, alkaline phosphatase, aspartate aminotransferase, alanine aminotransferase, uric acid, and lipid profile remained in physiologic range at baseline and after 1 month of pine bark extract or placebo treatment.
No serious adverse effects were reported. 1 patient with increase of slowness and 1 patient with moderate gastric discomfort were in the pine bark extract group.
Study limitations included small sample size, short duration of study, and small number of girls in pine bark extract group.
Pearls for Practice:
In children with ADHD, pine bark extract treatment results in improved visual-motor coordination, concentration, and some improved teacher ratings of hyperactivity and inattention, but not significantly improved parent ratings of ADHD symptoms.
In children with ADHD, pine bark extract does not cause serious adverse effects or change in biochemical measurements.
Pycnogenol May Help Reduce Muscular Cramps and Pain.:News Author: Laurie Barclay, MD.CME Author: Charles Vega, MD, FAAFP.
June 20, 2006 ¡ª Pycnogenol is effective in reducing cramps and muscle pain at rest and before and after exercise in both patients with vascular disease and in otherwise healthy athletes, according to the results of a study reported in the June issue of Angiology.
"With the millions of athletes worldwide, this truly is a profound breakthrough and extremely significant for all individuals interested in muscle cramp and pain relief with a natural approach," coauthor Peter Rohdewald, MD, from the University of Muenster in Germany, said in a news release. "These findings indicate that Pycnogenol can play an important role in sports by improving blood flow to the muscles and hastening post-exercise recovery."
In the first part of the study, 66 healthy subjects took four 50-mg Pycnogenol capsules (total dose, 200 mg/day) and were instructed to drink at least 1.5 L of water daily. The difference between number of cramp attacks recorded within the 2 weeks before starting Pycnogenol and the number of episodes during the fourth (P < .05) and fifth (P < .05) week were statistically significant.
In healthy subjects, the average number of cramping episodes decreased from 4.8 ¡À 1.2 events per week to 1.3 ¡À 1.1 at 4 weeks (P < .05). In patients with vascular disease, the episodes decreased from 6.3 ¡À 1.1 to 2.6 ¡À 0.4 per week (P < .05). In athletes, the number of episodes decreased from 8.6 ¡À 2 to 2.4 ¡À 0.5 (P <. 05). At 5 weeks, all 3 groups had decreases to levels lower than before consumption of Pycnogenol (P < .05).
During the second part of the study, 47 patients with intermittent claudication and diabetic microangiopathy were evaluated and treated for 1 week with Pycnogenol or placebo after a 2-week run-in phase. There was a significant decrease in cramping episodes and in muscular pain in those patients receiving pycnogenol. Patients with diabetic microangiopathy had a 20.8% decrease in pain, and those with claudication had a 21% decrease while supplementing with pycnogenol. Patients receiving placebo had no decrease in pain.
"Pycnogenol improves the blood supply to muscle tissue creating a relief effect on muscle cramping and pain," Dr. Rohdewald says. "Nitric oxide (NO) a blood gas, is well known to enhance blood flow and Pycnogenol may be influencing the activity of NO. The insufficient production of NO is the common denominator responsible for impaired blood flow in vascular disease."
Angiology. 2006;57:331-339
Learning Objectives for This Educational Activity
Upon completion of this activity, participants will be able to:
List conditions that may be improved with the use of Pycnogenol.
Identify the effects of Pycnogenol on cramping and muscular pain among patients with various underlying conditions.
Clinical Context
Pycnogenol is a naturally occurring compound found in French maritime pine bark. Chemically, Pycnogenol is a combination of procyanidins and phenolic acids and is purported to have significant antioxidant effects, in part by enhancing the actions of vitamins C and E.
A review by Rohdewald, published in the April 2002 issue of the International Journal of Pharmacology and Therapeutics, noted that Pycnogenol had been demonstrated to be effective as a preventive or therapeutic medicine in a wide range of conditions, including sunburn, asthma, systemic lupus erythematosus, and, possibly, hypertension and cardiovascular disease. Pycnogenol was also suggested to improve symptoms of premenstrual syndrome, including abdominal cramps.
The current study examines whether Pycnogenol could improve cramps and abdominal pain among athletes as well as patients with diabetes and peripheral vascular disease.
Study Highlights
The first part of the study was an open-label trial of Pycnogenol among 3 patient groups: healthy subjects with cramps at least 4 times per week, patients with chronic venous insufficiency and cramps 4 to 6 times per week, and athletes who experienced cramps at least 8 times weekly during athletic events. All subjects also reported moderate to severe muscular pain at least 3 days per week. Individuals with other medical illnesses or who were receiving any other medications were not eligible for this trial.
Participants received 50 mg of Pycnogenol 4 times daily along with a recommendation to drink at least 1.5 L of water daily. The treatment period lasted 4 weeks.
Study outcomes included the frequency of cramps and a 10-point visual analog scale of muscular cramps and pain.
The study cohort included 22 individuals in the healthy patient subgroup, 21 patients with venous insufficiency, and 23 athletes. Equal numbers of men and women participated in the trial.
Mean baseline frequency of cramps per day in the healthy patient, patient with venous insufficiency, and athletic patient groups were 4.8, 6.3, and 8.6, respectively. These mean values decreased to 1.3, 2.6, and 2.4 cramps per day in the 3 groups, respectively, after 4 weeks of treatment withPycnogenol. The visual analog scores for muscle cramping and pain also decreased significantly with treatment in all participant subgroups, and follow-up evaluations of cramp severity and frequency demonstrated a significant effect for Pycnogenol for 1 week following the end of study treatment.
The second part of the study was a placebo-controlled test of 100 mg of Pycnogenol twice daily. Subjects included patients with intermittent claudication, defined by symptoms on a defined treadmill protocol, and patients with diabetes and microangiopathy and neuropathy. The treatment period was 4 weeks, and the outcome measures were again the frequency and severity of muscular cramping and pain.
25 patients with intermittent claudication participated in the trial along with 22 patients with diabetic microangiopathy.
The mean numbers of cramping episodes per day at baseline were 9.5 and 8.9 in the claudication and diabetes groups, respectively. These mean respective levels decreased to 3.2 and 3.0 episodes per day with study treatment. Pycnogenol was superior to placebo in this outcome.
While analog measurements of muscular cramping and pain remained stable in the placebo group during the treatment phase, Pycnogenol significantly improved symptoms. Again, the positive effects of Pycnogenol remained evident for 1 week following cessation of study therapy.
There were no adverse events associated with study treatment.
Pearls for Practice:
A previous review of Pycnogenol suggested that this naturally occurring compound could be effective in the prevention or management of a variety of maladies, including sunburn, asthma, systemic lupus erythematosus, premenstrual syndrome, and, possibly, hypertension and cardiovascular disease.
The current study demonstrates that Pycnogenol can reduce the frequency and severity of muscle cramps among healthy patients; athletes; and patients with chronic venous insufficiency, intermittent claudication, and diabetes with microangiopathy. Treatment effects lasted for 1 week beyond the end of Pycnogenol therapy, and there were no adverse events associated with treatment.
Procyanidin fractions from pine (Pinus pinaster) bark: radical scavenging power in solution, antioxidant activity in emulsion, and antiproliferative effect in melanoma cells.:
J Agric Food Chem. 2005; 53(12):4728-35 (ISSN: 0021-8561).Touri??o S; Selga A; Jim??nez A; Juli?? L; Lozano C; Liz??rraga D; Cascante M; Torres JL.Institute for Chemical and Environmental Research (IIQAB-CSIC), Jordi Girona 18-26, 08034 Barcelona, Spain.
Pine (Pinus pinaster) bark is a rich source of procyanidin oligomers. From a total polyphenolic extract, we have generated fractions of different procyanidin composition. The mixtures, devoid of gallate esters, were active as free radical scavengers against ABTS(*+), DPPH, and HNTTM. Pine bark fractions were tested for antioxidant activity in solution (hydrogen donation and electron transfer) and emulsion (inhibition of lipid peroxidation) and compared with their galloylated counterparts from grape origin. While galloylation clearly influenced the free radical scavenging efficiency in solution, it did not seem to play a determinant role in protection against lipid peroxidation in emulsion. The fractions were very mild inhibitors of cell proliferation. Because gallate esters appear to interfere with crucial cell functions, gallate free pine procyanidins may be the innocuous chemopreventative agents of choice for many applications in food and skin protection.
Single and multiple dose pharmacokinetics of maritime pine bark extract (pycnogenol) after oral administration to healthy volunteers.:
BMC Clin Pharmacol. 2006; 6:4 (ISSN: 1472-6904).Grimm T; Skrabala R; Chovanov?? Z; Muchov?? J; Sumegov?? K; Lipt??kov?? A; Durackov?? Z; H??gger P.Institut f??r Pharmazie und Lebensmittelchemie, Bayerische Julius-Maximilians-Universit??t, W??rzburg, Germany. hogger@pzlc.uni-wuerzburg.de
BACKGROUND: Since plant extracts are increasingly used as phytotherapeutics or dietary supplements information on bioavailability, bioefficacy and safety are warranted. We elucidated the plasma kinetics of genuine extract components and metabolites after single and multiple ingestion of the standardized maritime pine bark extract Pycnogenol (USP quality) by human volunteers.
METHODS: Eleven volunteers received a single dose of 300 mg pine bark extract, five volunteers ingested 200 mg daily for five days to reach steady state concentrations. Plasma samples were obtained before and at defined time points after intake of the extract. Samples were analyzed by HPLC with ion-pair reagents and simultaneous UV and electrochemical detection. RESULTS: We quantified total plasma concentrations of catechin, caffeic acid, ferulic acid, taxifolin and the metabolite M1 (delta-(3,4-dihydroxy-phenyl)-gamma-valerolactone). Additionally, we describe plasma time courses and steady state appearance of ten so far unknown compounds, U1 to U10. After single ingestion, compounds derived from the extract were rapidly absorbed and the majority of them were detectable over whole experimental period of 14 h. The analysis of steady state plasma samples revealed significant phase II metabolism.
CONCLUSION: We present the first systematic pharmacokinetic analysis of compounds derived from maritime pine bark extract. Beyond the known constituents and metabolites we uncovered the plasma time courses of ten unknown compounds. In concert with our previous detection of anti-inflammatory bioefficacy of these plasma samples ex vivo we suggest that constituents and metabolites of Pycnogenol bear potential for disclosure of novel active principles.
Efficient preparation of catechin thio conjugates by one step extraction/depolymerization of pine (Pinus pinaster) bark procyanidins.:
J Agric Food Chem. 2005; 53(20):7760-5 (ISSN: 0021-8561).Selga A; Torres JL.Institute for Chemical and Environmental Research (IIQAB-CSIC), Jordi Girona 18-26, 08034 Barcelona, Spain.
The skin penetrating antioxidant cysteamine derivative of (-)-epicatechin as well as other thio conjugates were efficiently obtained with high yields from pine (Pinus pinaster) bark by simultaneous one pot extraction and depolymerization using water and cysteamine hydrochloride. The influence of the concentration of bark, acid, and cysteamine, as well as the reaction time on the total conversion, was studied. The total conversion into the epicatechin and catechin conjugates was as high as 47 g/kg pine bark with 1666 g cysteamine/kg bark and 28 g/kg with 166 g cysteamine/kg bark. A fast cleanup step by absorption/desorption on XAD-16 greatly facilitated further purification of the active major component. At a pilot scale, 4beta-(2-aminoethylthio)epicatechin (1) (conversion 263 g, purity 35% by reversed phase high-performance liquid chromatography/weight) was obtained from 17 kg of pine bark after simultaneous extraction/depolymerization followed by cleanup with the polymeric resin in approximately 10 h. The results show that pine (P. pinaster) bark is a suitable source of flavanols for the preparation of active thio derivatives. Conditions are given for the fast and efficient preparation of the conjugates.
Preclinical evaluation of rapeseed, raspberry, and pine bark phenolics for health related effects.:
J Agric Food Chem. 2005; 53(15):5922-31 (ISSN: 0021-8561).Vuorela S; Kreander K; Karonen M; Nieminen R; H??m??l??inen M; Galkin A; Laitinen L; Salminen JP; Moilanen E; Pihlaja K; Vuorela H; Vuorela P; Heinonen M.Department of Applied Chemistry and Microbiology, Division of Food Chemistry, University of Helsinki, P.O. Box 27 (Latokartanonkaari 11), 00014 University of Helsinki, Finland.
Rapeseed, raspberry, and pine bark are promising bioactive sources of plant phenolics selected from among ca. 100 previously screened plant materials for in vitro preclinical evaluation of health related effects. Phenolic extracts and isolated fractions of the selected materials were investigated for antioxidant, antimicrobial, antiinflammatory, and antimutagenic properties as well as for cell permeability. It was shown that rapeseed and pine bark phenolics and raspberry anthocyanins were good or excellent antioxidants toward oxidation of phosphatidylcholine membrane (liposomes), rapeseed oil (crude) phenolics were effective radical scavengers (DPPH test), and both raspberry and pine bark phenolics inhibited LDL oxidation. Rapeseed oil phenolics, principally vinylsyringol, raspberry anthocyanins, and pinoresinol and matairesinol, the principal components of pine bark phenolic isolate, were effective against formation of the proinflammatory mediator, prostaglandin E(2). Raspberry ellagitannins inhibited the growth of Proteus mirabilis and Klebsiella oxytoca. Pine bark and rapeseed had minor effects on the permeability of model drugs in Caco-2 experiments. None of the tested extracts were mutagenic nor toxic to Caco-2 cells or macrophages. Thus, phenolic isolates from rapeseed, raspberry, and pine bark and are safe and bioactive for possible food applications including functional foods intended for health benefit.
In vivo antioxidant activity of procyanidin-rich extracts from grape seed and pine (Pinus maritima) bark in rats.:
Int J Vitam Nutr Res. 2006; 76(1):22-7 (ISSN: 0300-9831).Busserolles J; Gueux E; Balasi??ska B; Piriou Y; Rock E; Rayssiguier Y; Mazur A.Centre de Recherche en Nutrition Humaine d'Auvergne, Unit?? des Maladies M??taboliques et Micronutriments, INRA, Theix, Saint-Gen??s-Champanelle, France.
BACKGROUND: In vitro evidence exists for the potential antioxidant benefits of procyanidin-rich extracts, but in vivo studies are scarce. We have evaluated the effects of selected procyanidin-rich extracts on oxidative stress in rats in condition of prolonged consumption of these compounds and also after single administration i.e. in postprandial conditions.
METHODS: Rats were fed for 8 weeks with diets supplemented with either a grape seed extract (GE), a pine bark extract (PE), or a high-degree polymerized pine bark extract (HPE). An additional study was performed in order to assess the postprandial effect of these extracts on plasma antioxidant capacity. The ferric-reducing antioxidant power (FRAP) and thiobarbituric acid-reactive substances (TBARS) were determined in plasma. For lipid peroxidation study of heart tissue, homogenates were prepared and TBARS were measured after lipid peroxidation induced by FeSO4-ascorbate.
RESULTS: After 8 weeks of dietary treatment, total antioxidant capacity in plasma was significantly higher in the GE and PE groups as compared with the other two groups. Plasma TBARS concentrations and heart susceptibility to peroxidation were not significantly different between the groups. In the postprandial state, by comparing plasma antioxidant capacity 2 hours after ingestion of the different procyanidin-rich extracts (500 mg/kg body weight), we observed that FRAP values were higher in the procyanidin-rich extracts groups as compared with the control group. Moreover, plasma FRAP concentration was significantly higher in the GE group as compared with the other groups.
CONCLUSION: The results of the present experiment constitute positive evidence for an in vivo antioxidant effect at the plasma level of procyanidin-containing plant extracts.
Use of a pine bark extract and antioxidant vitamin combination product as therapy for migraine in patients refractory to pharmacologic medication.:
Headache. 2006; 46(5):788-93 (ISSN: 0017-8748).Chayasirisobhon S.Department of Neurology, Kaiser Permanente Medical Center, Anaheim, CA 92807, USA.
OBJECTIVE: To evaluate the potential benefit of a pine bark extract and antioxidant vitamin combination product in the treatment of migraine headache.
BACKGROUND: This was an uncontrolled preliminary study to investigate the potential of an antioxidant formulation as therapy for migraine headache.
METHODS: Twelve patients with a long-term history of migraine with and without aura who had failed to respond to multiple treatments with beta-blockers, antidepressants, anticonvulsants, and 5-hydroxytryptamine receptor agonists were selected for the study. They were treated with 10 capsules of an antioxidant formulation of 120 mg pine bark extract, 60 mg vitamin C, and 30 IU vitamin E in each capsule daily for 3 months. Following enrollment patients completed a migraine disability assessment (MIDAS) questionnaire to give a baseline measure of migraine impact on work, school, domestic, and social activities over the previous 3 months. Patients were then treated for 3 months with the antioxidant formulation while continuing to receive existing pharmacologic medications. A second MIDAS was given at the conclusion of the treatment period.
RESULTS: There was a significant mean improvement in MIDAS score of 50.6% for the 3-month treatment period compared with the 3 months prior to baseline (P < .005). The treatment was also associated with significant reductions in number of headache days and headache severity score. Mean number of headache days was reduced from 44.4 days at baseline (95% CI 28.9 to 59.8) to 26.0 days (95% CI 5.3 to 46.7; P < .005) after 3 months' therapy and mean headache severity was reduced from 7.5 of 10 (95% CI 6.7 to 8.4) to 5.5 (95% CI 4.1 to 7.0; P < .005). CONCLUSION: These data suggest that the antioxidant therapy used in this study may be beneficial in the treatment of migraine possibly reducing headache frequency and severity. Further clinical investigation into the efficacy of antioxidant as therapy for chronic migraine is warranted.
Pilot study on the clinical effects of dietary supplementation with Enzogenol, a flavonoid extract of pine bark and vitamin C.:
Phytother Res. 2003; 17(5):490-4 (ISSN: 0951-418X).Shand B; Strey C; Scott R; Morrison Z; Gieseg S.Lipid & Diabetes Research Group, Christchurch Hospital, Christchurch, New Zealand. Brett.shand@cdhb.govt.nz
Flavonoids are naturally occurring plant compounds with established in vitro antioxidant properties and potential cardioprotective effects. We carried out a 12-week pilot study on the effects of dietary supplementation with an extract of bioflavonoids prepared from the bark of Pinus radiata trees [Enzogenol] containing added vitamin C. Data was collected from 24 healthy subjects aged between 55-75 years at baseline and at 6 and 12 weeks and included, routine biochemical and haematological indices, and anthropometric, blood pressure, forearm blood flow and haemorheological measurements. Enzogenol supplementation at a dosage of 480 mg/day of pine bark extract and 240 mg/day vitamin C did not result in changes in any biochemical or haematological indice and was associated with a significant reduction in the means of body weight, percentage body fat, systolic blood pressure and plasma viscosity. Basal and hyperaemic blood fl ow in forearm resistance vessels measured by plethysmography increased significantly during the study. The findings of this pilot study indicate that dietary supplementation with Enzogenol is safe and well tolerated and is associated with a number of beneficial effects on a range of established cardiovascular risk factors. These changes need to be validated by a placebo-controlled study but are consistent with other studies that have reported beneficial clinical effects following supplementation with bioflavonoids.
Pycnogenol, French maritime pine bark extract, improves endothelial function of hypertensive patients.:
Life Sci. 2004; 74(7):855-62 (ISSN: 0024-3205).Liu X; Wei J; Tan F; Zhou S; W??rthwein G; Rohdewald P.Guang An Men Hospital of Chinese Medical Science Research Institute, Beijing, PR China.
A placebo-controlled, double-blind, parallel group study was performed with 58 patients to investigate effects of French maritime pine bark extract, Pycnogenol, on patients with hypertension. Supplementation of the patients with 100 mg Pycnogenol over a period of 12 weeks helped to reduce the dose of the calcium antagonist nifedipine in a statistically significant manner. The intake of Pycnogenol decreased endothelin-1 concentrations significantly compared to placebo while concentrations of 6-keto prostaglandin F1a in plasma were significantly higher compared to placebo. Values for nitric oxide (NO) in plasma increased in both groups, but the differences were not significant. Angiotensin II concentrations in plasma were lowered in the placebo group to a larger extent than in the Pycnogenol group. Heart rate, electrolytes and blood urea nitrogen were not changed during treatment in both groups of patients. Unwanted effects observed in both groups were of mild and transient nature, such as gastrointestinal problems, vertigo, headache and nausea. Differences in rate of side effects were not statistically significant between the two groups. Study results support a supplementation with Pycnogenol for mildly hypertensive patients.
Antidiabetic effect of Pycnogenol French maritime pine bark extract in patients with diabetes type II.:
Life Sci. 2004; 75(21):2505-13 (ISSN: 0024-3205).Liu X; Wei J; Tan F; Zhou S; W??rthwein G; Rohdewald P.Guang An Men Hospital of Chinese Medical Science Research Institute, Beijing, PR China.
A double-blind, placebo-controlled, randomized, multi-center study was performed with 77 diabetes type II patients to investigate anti-diabetic effects of the French maritime pine bark extract, Pynogenol. Supplementation with 100 mg Pycnogenol for 12 weeks, during which a standard anti-diabetic treatment was continued, significantly lowered plasma glucose levels as compared to placebo. HbA1(c) was also lowered; however, the difference as compared to placebo was statistically significant only for the first month. In the Pycnogenol-group endothelin-1 was significantly decreased, while 6-ketoprostaglandin F(1a) in plasma was elevated compared to placebo. Nitric oxide levels in plasma increased during treatment in both groups, but, differences did not reach statistical significance. Pycnogenol was well-tolerated with ECG, electrolytes, creatinine and blood urea nitrogen remaining unchanged in both groups. Mild and transient unwanted effects were reported for both groups without significant differences. Supplementation of Pycnogenol to conventional diabetes treatment lowers glucose levels and improves endothelial function.
The effect of polyphenolic extract from pine bark, Pycnogenol on the level of glutathione in children suffering from attention deficit hyperactivity disorder (ADHD).:
Redox Rep. 2006; 11(4):163-72 (ISSN: 1743-2928).Dvor??kov?? M; Sivonov?? M; Trebatick?? J; Skod??cek I; Waczulikov?? I; Muchov?? J; Durackov?? Z.Department of Medical Chemistry, Biochemistry and Clinical Biochemistry, Faculty of Medicine, Comenius University, Bratislava, Slovak Republic.
Attention deficit hyperactivity disorder (ADHD) belongs to the neurodevelopmental disorders characterized by impulsivity, distractibility and hyperactivity. In the pathogenesis of ADHD genetic and non-genetic factors play an important role. It is assumed that one of non-genetic factors should be oxidative stress. Pycnogenol, an extract from the pine bark, consists of bioflavonoids, catechins, procyanidins and phenolic acids. Pycnogenol acts as powerful antioxidant, chelating agent; it stimulates the activities of some enzymes, like SOD, eNOS, and exhibits other biological activities. AIM: The aim of this randomized, double-blind, placebo-controlled trial was to investigate the influence of administered Pycnogenol or placebo on the level of reduced (GSH) and oxidized (GSSG) glutathione in children suffering from ADHD and on total antioxidant status (TAS). This is the first investigation of the redox glutathione state in relation to ADHD. RESULTS: One month of Pycnogenol administration (1 mg/kg body weight/day) caused a significant decrease in GSSG and a highly significant increase in GSH levels as well as improvement of GSH/GSSG ratio in comparison to a group of patients taking a placebo. TAS in children with ADHD was decreased in comparison with reference values. Pycnogenol administration normalizes TAS of ADHD children.
Antioxidant activity and inhibition of matrix metalloproteinases by metabolites of maritime pine bark extract (pycnogenol).:
Free Radic Biol Med. 2004; 36(6):811-22 (ISSN: 0891-5849).Grimm T; Sch??fer A; H??gger P.Institut f??r Pharmazie und Lebensmittelchemie, Bayerische Julius-Maximilians-Universit??t, W??rzburg, Germany.
The procyanidin-rich maritime pine bark extract Pycnogenol has well-documented antioxidant and anti-inflammatory activity. After oral administration of Pycnogenol two major metabolites are formed in vivo, delta-(3,4-dihydroxyphenyl)-gamma-valerolactone (M1) and delta-(3-methoxy-4-hydroxyphenyl)-gamma-valerolactone (M2). We elucidated the effects of these metabolites on matrix metalloproteinases (MMPs) and determined their antioxidant activity to understand their contribution to the effects of maritime pine bark extract. We discovered strong inhibitory effects of M1 and M2 toward the activity of MMP-1, MMP-2, and MMP-9. On a microgram-per-milliliter basis both metabolites appeared more active than Pycnogenol. The metabolites were more effective than their metabolic precursor (+)-catechin in MMP inhibition. On a cellular level, we detected highly potent prevention of MMP-9 release by both metabolites, with concentrations of 0.5 microM resulting in about 50% inhibition of MMP-9 secretion. M1 was significantly more effective in superoxide scavenging than (+)-catechin, ascorbic acid, and trolox, while M2 displayed no scavenging activity. Both metabolites exhibited antioxidant activities in a redox-linked colorimetric assay, with M1 being significantly more potent than all other compounds tested. Thus, our data contribute to the comprehension of Pycnogenol effects and provide a rational basis for its use in prophylaxis and therapy of disorders related to imbalanced or excessive MMP activity.
Urinary metabolites of French maritime pine bark extract in humans.:
Pharmazie. 2000; 55(5):364-8 (ISSN: 0031-7144).D??weler KG; Rohdewald P.Institut f??r Pharmazeutische Chemie, Westf??lischen Wilhelms-Universit??t, M??nster, Germany.
After oral administration of 5.28 g and 1.06 g of French maritime pine bark extract to a human volunteer, metabolites of some of the components of the extract could be detected. Ferulic acid and taxifolin, conjugated as glucuronide/sulphate, were excreted within 18 h. The peak urinary excretion was observed approximately 2-3 h after intake. Recovery of ferulic acid in urine was 36-43% and 7-8% for taxifolin. Two further metabolites could be identified as delta-(3,4-dihydroxy-phenyl)-gamma-valerolactone and delta-(3-methoxy-4-hydroxyphenyl)-gamma-valerolactone conjugated with glucuronic acid/sulphate. These metabolites could also be detected after intake of 960 mg of a procyanidin fraction of French maritime pine bark extract. Thus, it was shown that procyanidins are metabolised by humans. Both metabolites show maximal urinary excretion 8-12 h after intake and are excreted within 28-34 h.
Analgesic efficacy of French maritime pine bark extract in dysmenorrhea: an open clinical trial.:
J Reprod Med. 2004; 49(10):828-32 (ISSN: 0024-7758)
OBJECTIVE: To clarify the effect of Pycnogenol (Horphag Research, Switzerland), French maritime pine bark extract, on menstrual pain. STUDY DESIGN: We treated 47 patients with menstrual pain, aged 21-45 years, with Pycnogenol at 30 mg (2 capsules) orally twice a dysmenorrl day. The administration of Pycnogenol began on the eighth day of the first menstrual cycle and continued until the seventh day of the third menstrual cycle. Improvement was evaluated by measuring scores of symptoms during the first and second, and first and third menstrual cycle using the Wilcoxon rank sum test. RESULTS: Treatment with Pycnogenol lowered the pain scores for abdominal pain significantly (p < 0.05) as compared to pretreatment values. Pain relief in the second cycle of treatment was better as compared to the first cycle of treatment, as indicated by a higher level of significance (p < 0.01) and lower median pain score. The number of days with abdominal pain showed a trend toward fewer days with pain; however, the difference failed to reach significance. Relief of back pain was not that pronounced during the first cycle treated with Pycnogenol; the pain scores were not significantly different from those in the pretreatment period. However, continuation of treatment during the second cycle produced significant pain relief (p < 0.01). The number of days with back pain decreased. The number of days with pain was significantly lower (p < 0.01) in the second cycle of treatment with Pycnogenol. CONCLUSION: Pycnogenol has a potential analgesic effect on menstrual pain.
Pine bark extract pycnogenol downregulates IFN-gamma-induced adhesion of T cells to human keratinocytes by inhibiting inducible ICAM-1 expression.:
Free Radic Biol Med. 2000; 28(2):219-27 (ISSN: 0891-5849).Bito T; Roy S; Sen CK; Packer L.Department of Molecular and Cell Biology, University of California, Berkeley 94720-3200, USA
Expression of intercellular adhesion molecule-1 (ICAM-1) is necessary for leukocyte/keratinocyte interactions. Upregulation of ICAM-1 expression in keratinocytes has been observed in several inflammatory dermatoses, such as psoriasis, atopic dermatitis, and lupus erythematosus. Inflammatory cytokines, such as interferon-gamma (IFN-gamma), upregulate ICAM-1 expression in keratinocytes. Because of potent antioxidant and anti-inflammatory properties of the French maritime pine bark extract, Pycnogenol (Horphag Research, Geneva, Switzerland), its effects were investigated on the interaction of T cells with keratinocytes after activation with IFN-gamma and the molecular mechanisms involved in such interactions. Studies were performed using a human keratinocyte cell line, HaCaT. Cell adhesion in the presence of IFN-gamma was studied using a coculture assay. Treatment of HaCaT cells with 20 U/ml IFN-gamma for 24 h markedly induced adherence of Jurkat T cells to HaCaT cells. PYC pretreatment (50 microg/ml, 12 h) significantly inhibited IFN-gamma induced adherence of T cells to HaCaT cells (p < .01). ICAM-1 plays a major role in the IFN-gamma-induced adherence of T cells to keratinocytes. Thus, the effect of PYC on IFN-gamma-induced ICAM-1 expression was investigated as well. Pretreatment of HaCaT cells with PYC significantly inhibited IFN-gamma-induced expression of ICAM-1 expression in HaCaT cells. The downregulation of inducible ICAM-1 expression by PYC was both dose and time dependent. A 50 microg/ml dose of PYC and a 12 h pretreatment time (i.e., before activation with IFN-gamma) provided maximal (approximately 70%) inhibition of inducible ICAM-1 expression in HaCaT cells. Gamma-activated sequence present on the ICAM-1 gene confers IFN-gamma responsiveness in selected cells of epithelial origin (e.g., keratinocytes) that are known to express ICAM-1 on activation with IFN-gamma. Gel-shift assays revealed that PYC inhibits IFN-gamma-mediated activation of Stat1, thus suggesting a transcriptional regulation of inducible ICAM-1 expression by PYC. These results indicate the therapeutic potential of PYC in patients with inflammatory skin disorders.
A review of the French maritime pine bark extract (Pycnogenol), a herbal medication with a diverse clinical pharmacology.:
Int J Clin Pharmacol Ther. 2002; 40(4):158-68 (ISSN: 0946-1965)Rohdewald P.Institute Pharmaceutical Chemistry, Westf??lische Wilhelms-Universit??t M??nster, Germany. rohdewa@uni-muenster.de
OBJECTIVES: An increasing body of evidence indicates that Pycnogenol (PYC), a standardized extract of French maritime pine bark, has favorable pharmacological properties. This is a review of studies with both PYC and components of the preparation, that have helped to elucidate target sites and possible mechanisms for activity in men.
METHODS: Studies appearing in peer reviewed literature, as well as results presented at international meetings not yet available as published papers, are included in this review. Additional data from published sources in German and French languages that are not widely available are also included.
RESULTS: Chemical identification studies showed that PYC is primarily composed of procyanidins and phenolic acids. Procyanidins are biopolymers of catechin and epicatechin subunits which are recognized as important constituents in human nutrition. PYC contains a wide variety of procyanidins that range from the monomeric catechin and taxifolin to oligomers with 7 or more flavonoid subunits. The phenolic acids are derivatives of benzoic and cinnamic acids. The ferulic acid and taxifolin components are rapidly absorbed and excreted as glucuronides or sulphates in men, whereas procyanidins are absorbed slowly and metabolized to valerolactones which are excreted as glucuronides. PYC has low acute and chronic toxicity with mild unwanted effects occurring in a small percentage of patients following oral administration. Clinical studies indicate that PYC is effective in the treatment of chronic venous insufficiency and retinal micro-hemorrhages. PYC protects against oxidative stress in several cell systems by doubling the intracellular synthesis of anti-oxidative enzymes and by acting as a potent scavenger of free radicals. Other anti-oxidant effects involve a role in the regeneration and protection of vitamin C and E. Anti-inflammatory activity has been demonstrated in vitro and in vivo in animals. Protection against UV-radiation-induced erythema was found in a clinical study following oral intake of PYC. In asthma patients symptom scores and circulating leukotrienes are reduced and lung function is improved. Immunomodulation has been observed in both animal models as well as in patients with Lupus erythematosus. PYC antagonizes the vasoconstriction caused by epinephrine and norepinephrine by increasing the activity of endothelial nitric oxide synthase. Dilation of the small blood vessels has been observed in patients with cardiovascular disease, whereas in smokers, PYC prevents smoking-induced platelet aggregation and reduces the concentration of thromboxane. The ability to inhibit angiotensin-converting enzyme is associated with a mild antihypertensive effect. PYC relieves premenstrual symptoms, including abdominal pain and this action may be associated with the spasmolytic action of some phenolic acids. An improvement in cognitive function has been observed in controlled animal experiments and these findings support anecdotal reports of improvement in ADHD patients taking PYC supplements.
CONCLUSIONS: There is much evidence showing that PYC has beneficial effects on physiological functions. Results from ongoing clinical research are required to confirm and extend previous observations.
Enzyme inhibition and protein-binding action of the procyanidin-rich french maritime pine bark extract, pycnogenol: effect on xanthine oxidase.:
J Agric Food Chem. 2000; 48(11):5630-9 (ISSN: 0021-8561).Moini H; Guo Q; Packer LDepartment of Molecular and Cell Biology, 251 Life Sciences Addition, University of California at Berkeley, Berkeley, California 94720-3200, USA.
Pycnogenol, an extract from French maritime pine bark (PBE), is a complex mixture of bioflavonoids with reported protective effects against disease. PBE is an effective scavenger of reactive oxygen species, and its main constituents are procyanidins of various chain lengths. To find out the biochemical basis of action of PBE on enzyme activity, involvement of its redox activity and direct binding to the enzyme in its subsequent action on enzyme activity have been investigated. PBE dose-dependently inhibited the activities of xanthine oxidase, xanthine dehydrogenase, horseradish peroxidase, and lipoxygenase, but it did not affect the activities of glucose oxidase, ascorbate oxidase, or elastase. To characterize the mechanism of PBE action, studies were focused on xanthine oxidase and glucose oxidase. Under non-denaturing conditions, PBE changed the electrophoretic mobility of xanthine oxidase but not of glucose oxidase. Gel filtration chromatography confirmed higher molecular weight complexes of xanthine oxidase and xanthine dehydrogenase in the presence of PBE. It was found that hydrophobic bonding might be the dominant mode of interaction between PBE and xanthine oxidase. The importance of the binding in the effect of PBE on enzyme activity was supported by the observation that PBE binds to and inhibits catalase, but not superoxide dismutase. However, no correlation was found between superoxide/hydroxyl radical scavenging activity and the inhibitory effect on xanthine oxidase activity of PBE, various purified flavonoids, or other complex mixtures of bioflavonoids. The results indicate that PBE selectively inhibits xanthine oxidase through binding to the enzyme rather than by the redox activity.
The antioxidative effect of procyanidins from pine bark in vitro.:
Zhong Yao Cai. 2001; 24(12):882-4 (ISSN: 1001-4454).Lin C; Jiang J; Wu M; Yan Y; Zhou Y.Medical College of Jinan University, Guangzhou 510632.
OBJECTIVE: To assess the antioxidative effect of procyanidins from pine bark on free radical damage. METHODS: Hemolysis, Malonaldehyde(MDA) level of mice liver homogenates, the conformation changes of irradiated plasmid PUC18 were used as indexes. RESULTS: Procyanidins could reduce the hemolysis degree of human RBC induced by H2O2 significantly(P < 0.01), reduce the MDA level of mice liver homogenate initiated by VitC/Fe2+ remarkably(P < 0.01), and reduce the degree of single-strain break of plamid PUC18 induced by 60Co gamma significantly(P < 0.01). CONCLUSION: Procyanidins had good antioxidative function. It can prevent RBC membrane, plasmid DNA suffering from oxygen free radical damage in vitro.
Supplementation with a pine bark extract rich in polyphenols increases plasma antioxidant capacity and alters the plasma lipoprotein profile.:
Lipids. 2002; 37(10):931-4 (ISSN: 0024-4201).Devaraj S; Vega-L??pez S; Kaul N; Sch??nlau F; Rohdewald P; Jialal I.Laboratory for Atherosclerosis and Metabolic Research, University of California, Davis, Medical Center, Sacramento, California 95817, USA.
Pycnogenol (PYC), an extract of French maritime pine bark (Pinus pinaster), is a potent antioxidant with potential health benefits. Its bioavailabilty has previously been shown by urinary excretion studies of constituents and metabolites of PYC. The aim of this study was to test the effect of PYC supplementation on measures of oxidative stress and the lipid profile in humans. Twenty-five healthy subjects received PYC (150 mg/d) for 6 wk. Fasting blood was collected at baseline, after 3 and 6 wk of supplementation, and again after a 4-wk washout period. After 6 wk of supplementation with PYC, a significant increase in plasma polyphenol levels was detectable, which was reversed after the 4-wk washout phase. The antioxidant effect of PYC was demonstrated by a significant increase in oxygen radical absorbance capacity (ORAC) in plasma throughout the supplementation period (P < 0.05). The ORAC value returned to baseline after the 4-wk washout period. Moreover, in addition to its antioxidant effects, PYC significantly reduced LDL-cholesterol levels and increased HDL-cholesterol levels in plasma of two-thirds of the subjects. While the LDL changes reversed during washout, the HDL increase did not. There was no significant difference in LDL oxidizability or plasma lipid peroxides following PYC supplementation. Hence, following oral supplementation in humans, PYC significantly increases antioxidant capacity of plasma, as determined by ORAC, and exerts favorable effects on the lipid profile.
From ancient remedies to modern therapeutics: pine bark uses in skin disorders revisited.:
Phytother Res. 2001; 15(1):76-8 (ISSN: 0951-418X).Rihn B; Saliou C; Bottin MC; Keith G; Packer L.Membrane Bioenergetics Group, Department of Molecular and Cell Biology, University of California, Berkeley, CA 94720-3200, USA. rihn@inrs.fr
The effect of French maritime pine bark extract (PBE) on the gene expression profile of HaCaT human keratinocytes was studied using high density filter arrays. The expression profile of both control and PBE-treated cells was determined. Interestingly, PBE was shown to downregulate both calgranulin A and B genes which are known to be upregulated in psoriasis and various dermatoses. Thus, PBE could be considered in human dermatoses.
A novel alpha-glucosidase inhibitor from pine bark.:
Carbohydr Res. 2004; 339(3):715-7 (ISSN: 0008-6215).Kim YM; Wang MH; Rhee HI.Division of Biotechnology, Kangwon National University, Chunchon 200-701, South Korea.
Inhibitors of carbohydrate-hydrolysing enzymes play an important role for the treatment of diabetes. To our knowledge, a number of inhibitors such as, 1-deoxynojirimycin, acarbose and voglibose have been identified as a result of screening of secondary metabolites up to now. In this note, we report the inhibitory effect on carbohydrate hydrolysis of ethanol extracts from more than 1400 species of plants with the aim of identifying a potential antihyperglycemic drug. Pinus densiflora bark extracts showed the highest inhibition activity against several carbohydrate-hydrolysing enzymes.
French maritime pine bark extract Pycnogenol dose-dependently lowers glucose in type 2 diabetic patients.:
Phenolic extractives from the bark of Pinus sylvestris L. and their effects on inflammatory mediators nitric oxide and prostaglandin E2.:
J Agric Food Chem. 2004; 52(25):7532-40 (ISSN: 0021-8561)Karonen M; H??m??l??inen M; Nieminen R; Klika KD; Loponen J; Ovcharenko VV; Moilanen E; Pihlaja K.Environmental Chemistry and Structural Chemistry Group, Department of Chemistry, University of Turku, Vatselankatu 2, FIN-20014 Turku, Finland.
The anti-inflammatory properties of phenolic pine (Pinus sylvestris L.) bark extract were studied. The pine bark extract was fractionated by liquid-liquid extractions and semipreparative high-performance liquid chromatography to reveal the most potent constituents. The phenolic compositions of three pine bark samples obtained, a crude extract, a chloroform fraction, and a semipreparative fraction, were analyzed using high-performance liquid chromatography with UV diode array detection and/or electrospray ionization mass spectrometry. In addition, eight compounds were isolated and identified by NMR and MS techniques. In total 28 phenolic compounds were identified. The effects of the three pine bark samples on the synthesis of two proinflammatory mediators, nitric oxide and prostaglandin E(2), were measured. It was shown that pine bark contains compounds that inhibit the production of these proinflammatory mediators.
Antioxidant potential of six pine species.:
Phytother Res. 2006; 20(4):263-6 (ISSN: 0951-418X).Guri A; Kefalas P; Roussis V.Mediterranean Agronomic, Institute of Chania, Alsyllion Agrokepion, P.O. Box 85, GR 73100, Chania, Crete, Greece
The aim of the study was to evaluate the antioxidant efficacy of extracts obtained from six Pinus species (P. pinea, P. brutia, P. radiata, P. halepensis, P. attenuata, P. nigra) growing in natural forests in Southern Greece. Specimens of fresh, dry needles and pine bark were extracted and fractionated with a variety of organic solvents and the efficient concentration and their radical scavenging activity was evaluated by the Co(II)/EDTA induced luminol plateau chemiluminescence assay.
Comparative study of Venostasin and Pycnogenol in chronic venous insufficiency.:
Phytother Res. 2002; 16 Suppl 1:S1-5 (ISSN: 0951-418X).Koch R.Wolfsschlucht 6a, 34117 Kassel, Germany.
The aim of this study was to compare the efficacy of Venostasin (horse chestnut seed extract) and Pycnogenol (French maritime pine bark extract) in the treatment of chronic venous insufficiency (CVI). In an open, controlled comparative study 40 patients with diagnosed CVI were treated either with 600 mg chestnut seed extract per day or 360 mg Pycnogenol per day over a period of 4 weeks. The following parameters were investigated before the start of treatment and after 2 and 4 weeks of treatment: circumference of the lower legs and rating of subjective symptoms (scores) of pain, cramps, night-time swelling, feeling of "heaviness", and reddening of the skin. In addition, blood levels of cholesterol LDL and HDL were determined before and at the end of treatment. Pycnogenol significantly reduced the circumference of the lower limbs and significantly improved subjective symptoms. Furthermore, Pycnogenol significantly decreased cholesterol and LDL values in the blood, whereas HDL remained unaffected. Venostasin only moderately but not significantly, reduced the circumference of the lower limbs and marginally improved symptoms. Venostasin had no influence on the determined lipid values. Both medications were equally well tolerated. In conclusion, Pycnogenol was found to be more efficacious than Venostasin for the treatment of CVI.
Pycnogenol inhibits the release of histamine from mast cells.:
Phytother Res. 2003; 17(1):66-9 (ISSN: 0951-418X).Sharma SC; Sharma S; Gulati OP.Department of Pharmacology and Therapeutics, Trinity College, Dublin-2, Ireland. ssharma@tcd.ie
Oxygen derived free radicals are now increasingly regarded as a primary force of tissue destruction and also have the ability to release histamine from mast cells. Pycnogenol is an extract of the bark of French maritime pine (Pinus pinaster) containing bioflavonoids with a potent ability to scavenge free radicals. Therefore Pycnogenol was investigated for inhibition of histamine release from rat peritoneal mast cells. In addition, its effects were compared with sodium cromoglycate, a known inhibitor of histamine release from the mast cell. Rat peritoneal mast cells were isolated and purified by differential centrifugation and cells pooled from 3-4 animals were suspended at approximately 10(6) cells/mL buffered salt solution. Histamine release was induced by compound 48/80 or the calcium ionophore A-23187 and estimated from supernatant following extraction and by fluorimetric methods. Pycnogenol produced a concentration dependent inhibition of histamine release induced by the two secretagogues. Its inhibitory effect on mast cell histamine release was favourably comparable to sodium cromoglycate.
Pycnogenol prevents haemolytic injury in G6PD deficient human erythrocytes.:
Phytother Res. 2003; 17(6):671-4 (ISSN: 0951-418X).Sharma SC; Sharma S; Gulati OP.Department of Pharmacology and Therapeutics, Trinity College, Dublin-2 Ireland. ssharma@tcd.ie
Glucose6 phosphate dehydrogenase (G6PD) deficiency is the most common X-linked disorder of human erythrocytes where cells have inadequate capacity to destroy peroxides and high susceptibility towards haemolytic changes. Pycnogenol is a proprietary dry extract of the French Maritime pine (Pinus pinaster) bark with high ability to scavenge free radicals. In the present study we have investigated if Pycnogenol can protect G6PD deficient erythrocytes against haemolytic cell damage. Venous blood samples were obtained from six subject of Mediterranean origin with known G6PD deficiency which was also confirmed with standard techniques. Erythrocyte haemolysis in the presence and absence of Pycnogenol was induced either with tert-butylhydroperoxide (t-BHP) or quinine and the haemoglobin release in the supernatant was determined by recording the optical density at 540 nm in a Shimadzu spectrophotometer. Our results have shown that Pycnogenol has protective action against a Xenobiotic chemical induced haemolysis in G6PD deficient human erythrocytes.
Antimicrobial and antioxidant activities of natural extracts in vitro and in ground beef.:
J Food Prot. 2004; 67(1):148-55 (ISSN: 0362-028X).Ahn J; Gr??n IU; Mustapha A.Department of Food Science, 256 William Stringer Wing, Eckles Hall, University of Missouri, Columbia, Missouri 65211, USA.
Inhibition of Escherichia coli O157:H7, Salmonella Typhimurium, and Listeria monocytogenes by grape seed extract (ActiVin) and pine bark extract (Pycnogenol) and the effect of these natural extracts on the oxidative stability of raw ground beef were studied. In an agar dilution test, the MICs of ActiVin and Pycnogenol were determined to be 4.0 mg/ml for 4.43 log CFU per plate of E. coli O157:H7 and 4.0 mg/ml for 4.38 log CFU per plate of L. monocytogenes. In an inhibition curve test, populations of E. coli O157:H7, Salmonella Typhimurium, and L. monocytogenes fell to below the detection limit (10 CFU/ml) after 16 h of incubation. The numbers of E. coli O157:H7, L. monocytogenes, and Salmonella Typhimurium declined by 1.08, 1.24, and 1.33 log CFU/g, respectively, in raw ground beef treated with 1% Pycnogenol after 9 days of refrigerated storage. ActiVin (1%) and oleoresin rosemary (1%) resulted in an approximately 1-log CFU/g reduction in the populations of all three pathogens after 9 days. The addition of 1% ActiVin and Pycnogenol contributed to the maintenance of an acidic pH of 5.80 and 5.58, respectively, in raw ground beef. Compared to the control, all treatments increased in L* (lightness), with the exception of ActiVin. ActiVin and oleoresin rosemary had the highest a* (redness) and b* (yellowness) values, respectively. ActiVin most effectively retarded lipid oxidation, followed by Pycnogenol. The results suggest that these natural extracts have potential to be used with other preservative methods to reduce pathogenic numbers, lipid oxidation, and color degradation in ground beef.
Comparative efficacy of oligonol, catechin and (-)-epigallocatechin 3-O-gallate in modulating the potassium bromate-induced renal toxicity in rats.:
Toxicology. 2006; 226(2-3):181-7 (ISSN: 0300-483X)
Potassium bromate (KBrO(3)) is a by-product from ozonation of high-bromide surface water for production of drinking water and is a rodent carcinogen. Oligonol is a product emanating from the oligomerization of polyphenols, typically proanthocyanidin from a variety of fruits (grapes, apples, persimmons, etc.) and contains catechin-type monomers and proanthocyanidin oligomers. In this study, the ability of oligonol derived from grape seeds, grape seeds extracts (Product A, containing biologically active flavonoids and the oligomeric proanthocyanidin) and pine bark extracts (Product B, composed of flavan-3-ol derivatives) to modulate the KBrO(3)-induced renal toxicity was compared with (+) catechin and (-)-epigallocatechin 3-O-gallate (EGCG). In the Trolox equivalent antioxidant capacity (TEAC) assay, the order of the antioxidant activity was EGCG>catechin>oligonol>Product A>Product B. However, oligonol elicits the strongest antioxidant capacity following in vivo supplementation to rats, with the order of efficacy of oligonol>Product A> or =Product B>EGCG>catechin. Blood levels of lipid peroxidation products (LPO), urea nitrogen (BUN) and creatinine were elevated by KBrO(3) treatment. Oligonol significantly restored LPO to the level in the untreated rats and had the strongest potency when compared with the effects of Products A and B. The five materials lowered KBrO(3)-induced BUN level, but this was not statistically significant. Oligonol significantly reduced the increased level of the creatinine, seconded by Product A, Product B and EGCG. Catechin had the lowest effect in both the BUN and creatinine levels. That oligonol was able to modulate KBrO(3)-induced lipid peroxidation and the levels of blood urea nitrogen and creatinine suggests potential chemopreventive function and application in mitigating toxicity due to long-term exposure to KBrO(3) in public drinking water.
Effect of polyphenolic extract, Pycnogenol, on the level of 8-oxoguanine in children suffering from attention deficit/hyperactivity disorder.:
Free Radic Res. 2006; 40(9):1003-10 (ISSN: 1071-5762).Chovanov?? Z; Muchov?? J; Sivonov?? M; Dvor??kov?? M; Zitnanov?? I; Waczul??kov?? I; Trebatick?? J; Skod??cek I; Durackov?? Z.Department of Medical Chemistry, Biochemistry and Clinical Biochemistry, Faculty of Medicine, Comenius University, Sasinkova, Bratislava, Slovak Republic.
The purpose of this randomized, double-blind and placebo controlled study was to test the effect of polyphenolic extract of pine bark Pycnogenol (Pyc) on the level of oxidized purines represented by 8-oxo-7,8-dihydroguanine (8-oxoG) and on the total antioxidant status (TAS) in children with attention deficit/hyperactivity disorder (ADHD).We have found significantly increased damage to DNA in ADHD children when compared to controls. 8-oxoG was significantly lower after 1 month of Pyc administration in comparison to the beginning state and to placebo group. TAS in ADHD children was lower in comparison to controls. After Pyc administration, TAS was elevated but statistically significant increase was recorded after 1 month of termination of Pyc application. Improvement of DNA damage and TAS after Pyc administration is associated with the improvement of attention in ADHD children.In conclusion, Pycnogenol(R) administration reduces oxidative damage to DNA, normalizes TAS and improves attention of ADHD children. Explanation of mutual relation between oxidative damage to DNA, TAS and symptoms of ADHD and mechanism of Pyc's action needs further investigations.
Effects of pycnogenol treatment on oxidative stress in streptozotocin-induced diabetic rats.:
J Biochem Mol Toxicol. 2003; 17(3):193-9 (ISSN: 1095-6670).Maritim A; Dene BA; Sanders RA; Watkins JB.Moi University Faculty of Health Sciences, Eldoret, Kenya.
Free radicals and oxidative stress have been implicated in the etiology of diabetes and its complications. This in vivo study has examined whether subacute administration of pycnogenol, a French pine bark extract containing procyanidins that have strong antioxidant potential, alters biomarkers of oxidative stress in normal and diabetic rats. Diabetes was induced in female Sprague-Dawley rats by a single injection of streptozotocin (90 mg/kg body weight, ip), resulting (after 30 days) in subnormal body weight, increased serum glucose concentrations, and an increase in liver weight, liver/body weight ratios, total and glycated hemoglobin, and serum aspartate aminotransferase activity. Normal and diabetic rats were treated with pycnogenol (10 mg/kg body weight/day, ip) for 14 days. Pycnogenol treatment significantly reduced blood glucose concentrations in diabetic rats. Biochemical markers for oxidative stress were assessed in the liver, kidney, and heart. Elevated hepatic catalase activity in diabetic rats was restored to normal levels after pycnogenol treatment. Additionally, diabetic rats treated with pycnogenol had significantly elevated levels of reduced glutathione and glutathione redox enzyme activities. The results demonstrate that pycnogenol alters intracellular antioxidant defense mechanisms in streptozotocin-induced diabetic rats.
Effect of procyanidins from Pinus maritima on glutathione levels in endothelial cells challenged by 3-morpholinosydnonimine or activated macrophages.:
Redox Rep. 1999; 4(4):171-7 (ISSN: 1351-0002).Rimbach G; Virgili F; Park YC; Packer L.Department of Molecular and Cell Biology, University of California, Berkeley 94720-3200, USA.
The effects of reactive nitrogen species on glutathione homeostasis in human endothelial ECV 304 cells challenged by 3-morpholinosydnonimine-N-ethylcarbamide (SIN-1) on RAW 264.7 activated macrophages using a co-culture model were investigated. SIN-1 or macrophages activated by lipopolysaccharide plus interferon-gamma induced a significant glutathione decrease in ECV 304 cells. Pre-incubation of ECV 304 cells with French maritime pine bark extract containing mainly oligomeric procyanidins protected endothelial cells from activated macrophage-induced glutathione depletion. Data demonstrate that reactive nitrogen species generated with different kinetics and mechanisms impair glutathione levels in endothelial cells, and that pine bark extract significantly enhances antioxidant defenses.
Antifugal susceptibility testing and antifugal traditional Chinese medicines screening of oral Candida isolated from head and neck cancer patients treated with radiotherapy or chemotherapy.:
Hua Xi Kou Qiang Yi Xue Za Zhi. 2006; 24(2):131-4 (ISSN: 1000-1182).Zhao M; Zhou ZT; Zhang WD.Dept. of Oral Medicine, The Ninth Affiliated Hospital of Shanghai Second Medical University, Shanghai 200011, China.
OBJECTIVE: To evaluate the sensitivity and resistance of pathogenic oral Candida spp. isolated from head and neck cancer patients treated with radiotherapy or chemotherapy to antifungal agents. To screen antifugal agents from Chinese traditional and herbal drugs by NCCLS M27-A2 method. METHODS: Using YBC Test Kit to identify 20 clinical oral Candida isolated from head and neck cancer patients treated with radiotherapy or chemotherapy. The in vitro susceptibilities of 20 oral Candida spp. to 5-flucytosine (5-FC), itraconazole (ITR), fluconazole (FLU), the extracts of 6 Chinese traditional and herbal drugs (caltrop, honeysuckle flower, dandelion, green tea, pine bark, red trefoil) and utility componets of 7 Chinese traditional and herbal drugs (sophorcarpidine, aloperine, archin, glycyrrhizic acid, glycosides of white peony root, glycosides of baikal skullcap root, hydrochloric berberine) were determined by NCCLS M27-A2 method. RESULTS: The proportion of no-C. albicans in all Candida spp. were 25%. All strains were sensitive to 5-flucytosine, 25% stains were resistant to fluconazole and 40% stains were resistant to itraconazole. In all agents from Chinese traditional and herbal drugs, glycosides of white peony root and hydrochloric berberine (C20H18CINO4) exhibited antifungal activity, especially to C. glabrates. CONCLUSION: The proportion of no-C. albicans in all oral Candida spp. isolated from head and neck cancer patients treated with radiotherapy or chemotherapy was pretty high. NCCLS M27-A2 micro-dilution method is a reliable and reproducible method and can be used to screen antifugal agents from Chinese traditional and herbal drugs.
Does pycnogenol intensify the efficacy of acetylsalicylic acid in the inhibition of platelet function? In vitro experience.:
Postepy Hig Med Dosw (Online). 2006; 60:316-21 (ISSN: 1732-2693).Gola??ski J; Muchova J; Gola??ski R; Durackova Z; Markuszewski L; Wata??a C.Department of Hemostasis and Hemostatic Disorders, Medical University Hospital No. 2, Medical University of ????d??, ????d??, Poland.
INTRODUCTION: Some compounds of herbal origin, such as Pycnogenol (PYC), have been considered as an aid in antiplatelet therapy. Pycnogenol, a French maritime pine bark extract, is a complex mixture of polyphenols that has the ability to reduce human smoking-induced platelet aggregation. The aim of this study was to evaluate the in vitro ability of PYC to improve the efficacy of acetylsalicylic acid (ASA) in the inhibition of platelet function. MATERIAL/METHODS: Whole blood, anticoagulated with hirudin, was drawn from 38 volunteers (40.4+/-13.8 years old) and incubated with PYC (10, 50, 100 microg/ml) or/and ASA (25, 100 micromol/l) for 20 min at RT.PYC was dissolved in water (water-PYC group, n=20) or ethanol (ethanol-PYC group, n=18). To investigate platelet functions, PFA-100 closure-time determination, whole-blood electrical aggregation (WBEA), and PRP aggregation were employed. Collagen (1 microg/ml) and ADP (5 micromol/l) were used as platelet agonists. RESULTS: A compounding effect of ASA and PYC to inhibit platelet function recorded in collagen-induced aggregation in PRP was observed, but only when ethanol-dissolved PYC was used. The inhibitory effect of PYC (alone) was most profound in platelets activated with ADP. At all concentrations, PYC significantly inhibited platelet aggregation only in the ethanol-PYC group. CONCLUSIONS: It was found that under in vitro conditions, ethanol-dissolved PYC deepened the efficacy of ASA to inhibit platelet function. This study confirmed the direct and compounding (with ASA) inhibitory effect of PYC on platelets. These observations encourage the concept that the combined use of ASA and PYC may be beneficial in patients with impaired response to ASA therapy.
Effect of plant phenolics on protein and lipid oxidation in cooked pork meat patties.:
J Agric Food Chem. 2005; 53(22):8492-7 (ISSN: 0021-8561)Vuorela S; Salminen H; M??kel?? M; Kivikari R; Karonen M; Heinonen M.Department of Applied Chemistry and Microbiology, Division of Food Chemistry, University of Helsinki, P.O. Box 27, 00014 University of Helsinki, Finland. satu.vuorela@helsinki.fi
Rapeseed and pine bark are rich sources of phenolic compounds that have in previous studies been shown to exhibit antioxidant and anti-inflammatory properties. In this study, the antioxidant effect of rapeseed and pine bark phenolics in inhibiting the oxidation of lipids and proteins in meat was tested as a possible functional food application. The cooked pork meat with added plant material was oxidized for 9 days at 5 degrees C under light. The suitable level of plant material addition was first screened by following lipid oxidation only. For further investigations plant materials were added at a level preventing lipid oxidation by >80%. The oxidation was followed by measuring the formation of hexanal by headspace gas chromatography and the formation of protein carbonyls by converting them to 2,4-dinitrophenylhydrazones and measured by spectrophotometer. It was shown that rapeseed and pine bark were excellent antioxidants toward protein oxidation (inhibitions between 42 and 64%). These results indicate that rapeseed and pine bark could be potential sources of antioxidants in meat products.
Hydroxyl and superoxide anion radical scavenging activities of natural source antioxidants using the computerized JES-FR30 ESR spectrometer system.:
Biochem Mol Biol Int. 1997; 42(1):35-44 (ISSN: 1039-9712).Noda Y; Anzai K; Mori A; Kohno M; Shinmei M; Packer L.Department of Molecular and Cell Biology, University of California at Berkeley 94720-3200, USA
Free radical scavenging activities of water-soluble extracts from some natural sources, health foods, and antioxidant substances were measured using the JES-FR30 JEOL spectrometer. The objective was to develop a standardized method whereby comparison could be made between the radical scavenging activities of complex mixtures. Scavenging of hydroxyl radical was determined using DMPO. Activity was calibrated using a standard material, L-ascorbic acid 2-[3,4-dihydro-2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-2H -1- benzopyran-6yl-hydrogen phosphate] potassium salt (EPC-K1), an analog of vitamin C and vitamin E which is water soluble and stable at room temperature. The order of greatest hydroxyl radical scavenging activity was green tea extract, pine bark extract (Pycnogenol), Ginkgo Biloba extract (EGb 761), a flavonoid blend of several fruit and vegetable extracts (GNLD), and Bio-Normalizer (Sun-O Corp). Activity was determined after treatment of samples with ascorbic acid oxidase. This treatment revealed the presence of ascorbate in some natural extracts and commercial preparations. The pine bark extract was the most heat resistant and had ascorbate-like activity in the preparations. Scavenging of superoxide anion was determined using the spin trap, 5,5-dimethyl-1-pyrroline-N-oxide (DMPO), and analyzed by comparison with a standard curve made with superoxide dismutase. Comparison of the water solubilized components of natural source antioxidants showed that filtrates fractionated using centrifuge type Millipore filter tubes (M.W. < 100,000; M.W. < 10,000) also had almost the same SOD-like activity. Samples were also treated with ascorbate oxidase or by heating (100 degrees C for 10 min). The order of activity, from greatest to least, was Ginkgo biloba extract EGb 761, pycnogenol, beta-catechin, tea and BioNormalizer.
Analysis of condensed and hydrolysable tannins from commercial plant extracts.:
J Pharm Biomed Anal. 2006; 41(2):415-20 (ISSN: 0731-7085).Romani A; Ieri F; Turchetti B; Mulinacci N; Vincieri FF; Buzzini P.University of Florence, Department of Pharmaceutical Science, Via Ugo Schiff 6, I-50019 Sesto Fiorentino, Florence, Italy. annalisa.romani@unifi.it
High performance liquid chromatography (HPLC)/DAD and MS qualitative and quantitative analyses of polyphenols, hydrolysable and condensed tannins from Pinus maritima L. and tannic acid (TA) extracts were performed using normal and reverse phase. Normal-phase HPLC was more suitable for pine bark (PBE) and tannic acid extracts analysis. The chromatographic profile revealed that P. maritima L. extract was mainly composed by polymeric flavanols (containing from two to seven units) and tannic acid (characterized by a mixture of glucose gallates containing from three to seven units of gallic acid). Concerning their antimycotic properties, P. maritima L. extract exhibited a broad activity towards yeast strains of the genera Candida, Cryptococcus, Filobasidiella, Issatchenkia, Saccharomyces: MICs from 200 to 4000 microg/ml (corresponding to 140-2800 microg/ml of active polyphenols) were determined. Conversely, no activity of tannic acid was observed over the same target microorganisms. Taken into consideration the above results of HPLC analysis and on the basis of the current literature, we may conclude that only 70.2% of polyphenols (recognized as condensed tannins) occurring in P. maritima L. extract can be apparently considered responsible for its antimycotic activity.
Activity of monomeric, dimeric, and trimeric flavonoids on NO production, TNF-alpha secretion, and NF-kappaB-dependent gene expression in RAW 264.7 macrophages.:
FEBS Lett. 2000; 465(2-3):93-7 (ISSN: 0014-5793).Park YC; Rimbach G; Saliou C; Valacchi G; Packer L.Department of Molecular and Cell Biology, 251 Life Sciences Addition, University of California, Berkeley, CA 94720-3200, USA.
Flavonoids are potent antioxidants and have been associated with lowering the risk of cardiovascular diseases. In this study, the effect of flavonoids (monomers, dimers and a trimer) as well as French maritime pine bark extract, Pycnogenol, on NO production, tumor necrosis factor-alpha (TNF-alpha) secretion and nuclear factor (NF)-kappaB activity was compared. Monomers and dimers repressed NO production, TNF-alpha secretion and NF-kappaB-dependent gene expression induced by interferon gamma, whereas the trimeric procyanidin C2 and Pycnogenol enhanced these parameters. In addition, in unstimulated RAW 264.7 macrophages, both procyanidin C2 and Pycnogenol increased TNF-alpha secretion in a concentration- and time-dependent manner. These results demonstrate that procyanidins act as modulators of the immune response in macrophages.
Pycnogenol in chronic venous insufficiency.:
Fitoterapia. 2000; 71(3):236-44 (ISSN: 0367-326X).Arcangeli P.Professore di Clinica Medica Generale e Terapia Medica, Universit?? degli Studi di Firenze, Via Marsilio Ficino 10, I-50122, Firenze, Italy.
Forty patients with chronic venous insufficiency (CVI) and varices of the legs were selected and double-blindly randomly assigned to a treatment with Pycnogenol (French maritime pine bark extract), 100 mg x 3/day or a placebo for 2 months, according to a double-blind experimental design. The effects of the treatment were evaluated by scoring the symptomatology with a semi-quantitative scale, and the venous blood flow by means of a hand-held Doppler ultrasound. The tolerability was evaluated by recording the adverse effects and by means of hematology and blood chemistry parameters, before and at the end of the treatment. Pycnogenol treatment induced a significant reduction in subcutaneous edema as well as heaviness and pain in the legs, on both after 30 and 60 days, the evaluation time periods. Approximately 60% of patients treated with Pycnogenol(R) experienced a complete disappearance of edema (the most rapidly disappearing symptom) and pain at the end of the treatment, while almost all the patients reported a reduction in leg heaviness which disappeared in approximately 33% of patients. These changes were statistically significant. No effect was observed in the placebo-treated subjects. No effect on the venous blood flow was observed in either of the experimental groups.
Effect of PYCNOGENOL on the toxicity of heart, bone marrow and immune organs as induced by antitumor drugs.:
Phytomedicine. 2002; 9(5):414-8 (ISSN: 0944-7113)Feng WH; Wei HL; Liu GT.Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union of Medical College, Beijing, People's Republic of China.
PYCNOGENOL is a mixture of water-soluble bioflavonoids extracted from the bark of pine trees growing in the southwest coastal region of France. In the present paper the effects of PYCNOGENOL (Pyc) on the toxicity of bone marrow, heart and immune organs induced by anticancer drugs were investigated, in mice. The following results were obtained: 1. Pyc at the orally-administered dose of 200 and 150 mg/kg body wt. markedly prevented the elevation of serum creatine phosphokinase (CPK) activity and the decrease of heart rate in mice treated with doxorubicin (Dox); 2. Pyc at 100 and 150 mg/kg body wt. significantly antagonized the inhibition of DNA synthesis in thymus induced by subcutaneous injection of cyclophosphamide (Cyc); 3. Pyc at 150 and 200 mg/kg body wt. markedly induced increase of erythrocytes and hemoglobin, but had no effect on leukopenia, in Cyc-treated mice; and 4. Pyc has no antagonizing effect on the anticancer activity of Dox and Cyc. All the results suggest that Pyc possesses a protective effect on the cardiotoxicity of Dox and the inhibition of thymus DNA synthesis induced by Cyc in mice.
A comparison of the hydroxyl radical scavenging properties of the shark bile steroid 5 beta-scymnol and plant pycnogenols.:
Biochem Mol Biol Int. 1997; 42(6):1249-60 (ISSN: 1039-9712).Macrides TA; Shihata A; Kalafatis N; Wright PF.Department of Medical Laboratory Science, RMIT-University, Melbourne, Victoria, Australia.
The hydroxyl radical (OH.) quenching abilities of the following compounds were compared in the deoxyribose degradation system (initiated by the ferrous-ascorbate Fenton reaction): (a) 5 beta-scymnol, the hepatoprotective shark bile sterol, and its mono- and di-sulfate esters; (b) three marketed pycnogenol preparations (syn: proanthocyanidin--natural plant-derived polyphenolic bioflavonoids) extracted from pine tree (Pinus maritima) bark and grape (Vitis vinifera) seeds; and (c) two known hydroxyl radical scavengers, dimethyl sulfoxide and mannitol, and the peroxyl radical scavenger Trolox (the alpha-tocopherol analogue). 5 beta-scymnol was a more potent OH. quencher than dimethyl sulfoxide, mannitol and Trolox, and markedly more potent than the pycnogenol preparations. Increased sulfation of 5 beta-scymnol progressively reduced its free radical scavenging activity, thus clearly attributing the potent OH. quenching properties to its novel tri-alcohol-substituted aliphatic side chain. The favourable interaction of these bile steroids with reactive oxygen species in an aqueous environment, makes them attractive candidates for evaluation as protective agents against disorders in which oxidative stress is implicated.
An experimental comparison of Pycnogenol and methylphenidate in adults with Attention-Deficit/Hyperactivity Disorder (ADHD).:
J Atten Disord. 2002; 6(2):49-60 (ISSN: 1087-0547).Tenenbaum S; Paull JC; Sparrow EP; Dodd DK; Green L.The Attention Deficit Center in St. Louis 63141, MO.
Twenty-four adults (24 to 53 years old) with Attention-Deficit/Hyperactivity Disorder (ADHD), Combined Type, were studied in a double-blind, placebo-controlled, crossover study of Pycnogenol and methylphenidate. Pycnogenol is an antioxidant derived from the bark of the French maritime pine tree. Methylphenidate is a standard pharmaceutical intervention for ADHD. Anecdotal reports suggest that Pycnogenol improves concentration in adults with ADHD without adverse side effects. Participants received Pycnogenol, methylphenidate, and placebo, each for three weeks, in a randomized and counterbalanced order. Although ADHD symptoms improved during treatment, neither methylphenidate nor Pycnogenol outperformed the placebo control, as measured by self-report rating scales, rating scales completed by the individual's significant other, and a computerized continuous performance test. The conservative dosage levels and relatively brief length of treatment may have contributed to the absence of significant differences among treatment conditions. Implications for future research are noted.
Scientific References:
1.Pine Bark Extract Proanthocyanidins and Pine Bark logogriph.
2.Research update of Pine Bark Extract Proanthocyanidins related.
Claims & Warning:
Claims: Information this web site presented is meant for Nutritional Benefit and as an educational starting point only, for use in maintenance and promotion good health in cooperation with a common knowledge base reference...Furthermore,it based solely on the traditional and historic use or legend of a given herb from the garden of Adonis. Although every effort has been made to ensure its accurate, please note that some info may be outdated by more recent scientific developments......
Pharmakon Warning: The order of knowledge is not the transparent order of forms and ideas,as one might be tempted retrospectively to interpret it; it is the antidote....(Dissemination,Plato's Pharmacy,II.The Ingredients:Phantasms,Festivals,and Paints;138cf. Jacques Derrida.).
And as it happens,the technique of imitation,along with the production of the simulacrum,has always been in Plato's eyes manifestly magical,thaumaturgical:......and the same things appear bent and straight to those who view them in water and out,or concave and convex,owing to similar errors of vision about colors, and there is obviously every confusion of this sort in our souls.And so scene painting (skiagraphia) in its exploitation of this weakness of four nature falls nothing short of witchcraft (thaumatopoia), and so do jugglery and many other such contrivances.(Republic X,602c-d;cf.also 607c).
seminal trace...French Marine Pine Bark Extract, French Maritime Pine Bark Extract, Leucoanthocyanidins, OPC, Oligomeric Proanthocyanidins, PCO, Pinus maritima, Pinus pinaster, Procyandiol Oligomers, Procyanodolic Oligomers, Pycnogenol, Pygenol.Pine Bark Extract.Proanthocyanidins.CAS.NO:90082-77-2.M.F.C30H26O12.Pinus Strobus Bark extract.Proanthocyanidins,Proanthocyanidin B2.Pinetree extract.CAS.NO.000000-14-0...
Phytochemical info of Pine Bark Extract:
Phlebotonics for venous insufficiency.:MJ Martinez
Scientific References:
Claims & Warning:
