Protodioscin:Functions,Combination case study and Research findings.......

  seminal trace...Dioscorea gracillima miq extract.Protodioscin.20%,30%40%HPLC.CAS:55056-80-9;60478-69-5.M.F.:C51H84O22.Thinnest Yam extract.Dioscorea spp extract.Hypoglauca yam extract...

 


 Introduction and Basic Source Info of Protodioscin:
 Protodioscin Basic Info:
 Phytochemicals and Constituents of Dioscorea gracillima Miq.:
 Basic Functions and Effects of Protodioscin in Brief:
 Combination and case study:1.Protodioscin and natural acne treatment
 Combination and case study:2.Protodioscin and treatment for Age-Related Sexual Performance Decline:
 Combination and case study:3.Protodioscin and Super Volume Plus:
 Protodioscin Toxicology
 Research Update of Protodioscin related.


   Introduction and Basic Source Info of Protodioscin:

 Botanical Source Latin Name:Dioscorea gracillima Miq.
 English Name:Thinnest Yam
 Family:Dioscoreaceae
 Family Member Botanical Source:  (1).Dioscorea hypoglauca Palib,   (2).Dioscorea collettii Hook.f.;  (3).Dioscorea todoro Mak.;  (4).Dioscorea gracillima Miq.
 Pharmaceutical Names:Rhizoma Dioscoreae Septemlobae;Rhizoma Dioscoreae Tokoro;Rhizoma Dioscoreae Hypoglaucae.
 Habitat: (1).Dioscorea hypoglauca Palib:wide spread from AnHui,ZheJiang,JiangXi,Fujian province etc;(2).Dioscorea collettii Hook.f.:spread growing from Fujian,Taiwan,Sichuan,Yunnan,Guizhou province,etc.(3).Dioscorea todoro Mak.:wide spread at south China.(4).Dioscorea gracillima Miq.:spread from Zhejiang,Jiangxi,Anhui province,etc.

 Rhizome underground column shape,fleshy and plump. Stem column shape, egg shape shoot growing from axil.Leaf shape triangle egg shape to triangle ovum shape,halbert heart shape base.Stamen spike like,no droop,long axis twist like,nearly no flower stem,flower bud triangle egg shape,shorter than perianth,perianth 6 in total,egg shape.female flower shape similar as stamen,germen chapiter split. Capsule fruit has 3 wings,fruit wings have short stems, seed 2 every room,shape egg with wing. Florescence June to August,Fruiting August till October.
 Habitat:widely growing road side and mountain shrubs,prefer sun or growing near farm,spread north and south of China.
 


   Protodioscin Basic Info:

 Name of Product:Protodioscin
 Part of Used:Root and stem of Dioscorea gracillima miq
 Active Ingredients:Protodioscin
 Characteristics:White fine powder
 Specs Available:20%,30%
 Formula C51H84O22
 Mass 1048.5452 (1049.21)
 Synonyms:Protodioscin
 Chemical Name:26-O-Beta-D-glycopyranosyl-22-hydroxyfurost-5-ene-3Beta,26-diol-3-O-Beta-diglucorhamnoside
 CAS: 55056-80-9;60478-69-5
 


    Phytochemicals and Constituents of Dioscorea gracillima Miq.:

 Dioscorea gracillima Miq.Root Rhizoma majorly contains Graceillin and Diosgenin 1.03~2.02%,.Dioscin 2.09 %,yamogenin.some level of Protodioscin.
 Dioscorea todoro Mak. Root Rhizoma majorly contains Dioscin,Graceillin,Dioscorea-sapotozin A,Tokoronin,Yononin,etc.Diosgenin 1.2%(Jiang Su Origin),2.1%(Zhejiang Origin),1.35%(Jiang Su Yinxing Origin);Tokorogenin:0.06%(Jiang Su Origin);0.09%(Zhejiang Origin),0.32%(Jiang Su Yinxing Origin);Yamogenin:0.04%(Jiang Su Origin),0.10%(Zhejiang Origin);Yonogenin,Kogagenin and Igagenin.Some level of 25D-Spirosta-3,5-diene.

   Basic Functions and Effects of Protodioscin in Brief:

 Protodioscin which classified as a furostanol saponin, is the active ingredient of the plant extract of Dioscorea gracillima miq. Its molecular formula is C51H84O22, and its molecular weight is1049.21 daltons.

   Main Function as following:

  1.  Inhibition of cancer cell growth,antiproliferative against human tumor cell lines.
  2.  Improve sexual desire:Dramatically and safely increases sex drive/libido in both men and women.
 Protodioscin can acts as a natural precursor to sex hormones, and is converted into its final forms by the body's own natural enzymes.
  3.  Testosterone enhancement: Increase testosterone by 30% without side effects shown in study in males taking 750mgs per day for 5 days.
 Protodioscin is the remarkable compound shown to enhance the production of luteinizing hormone (LH), which in turn, raises testosterone levels. Studies have also shown that protodioscin works to help stimulate protein synthesis, the major component for lean mass gains. Protodioscin increases the secretion of a hormone regulating the flow of testosterone in the body.
  4.  Regulate the body's androgen levels and may help in preventing hair loss due to the overproduction of the androgen DHT.
  5.  Decreased cholesterol in plasma and liver,Reduces cholesterol and high blood pressure in clinical trials.
  6.   Provide a natural relief for menopause of woman.Alleviation of symptoms of sexual frigidity in women
  7.  Help maintain optimal cell health:This function useful to help treatment for acne.
 The active ingredient in the herb Tribulus terrestris, protodioscin has been clinically proven to help maintain optimal cell health by maintaining the proper balance of natural metabolites and hormones in your body.
  8.  Dramatically speeds muscle and energy recovery, increases strength levels. Ideal, safe non-hormonal sports nutrition supplement. ( No side-effects from harmful steroids )
 


   Combination and case study:1.Protodioscin and natural acne treatment

 PotatoClear is a natural acne treatment that will help you get rid of acne, including whiteheads, blackheads, red spots, body acne and adult acne, fast! With PotatoClear, you can have blemish-free, clear complexion, and healthy skin naturally.
 PotatoClear contains only natural ingredients with antiseptic and antibacterial properties to help clear up acne breakouts and prevent future breakouts. It also has the essential vitamins and herbal nutrients to help you keep acne at bay! PotatoClear contains:

  Tea Tree Oil:  Tea tree oil is a natural antibacterial and antifungal solution derived from the leaves of the Melaleuca tree (tea tree plant). This natural ingredient has been clinically shown to be as effective as chemical acne treatments in eliminating acne breakouts and preventing future acne. Unlike chemical acne treatments, however, tea tree oil does not have unwanted side effects and will not dry out your skin.

  Zinc:  Zinc is a natural element that is essential for skin health. It has been shown to be effective for acne treatments, especially for the elimination of red spots often left by acne.

  Vitamin A:  Besides its famous function for good vision health, vitamin A is also necessary to maintain healthy skin, eliminate age spots and blemishes, as well as fight acne breakouts.

  Vitamin B1, B5 & B6:  Vitamin B1 is a soluble vitamin is necessary for normal protein metabolism for the maintenance of proper skin cell growth. Vitamin B5 has been shown to have beneficial effects in helping counteract stress and promote metabolism, build new skin cells, and maintain normal cell growth. Vitamin B5 is a great vitamin that helps protect skin against the signs of aging. Vitamin B6 forms a variety of functions in your body and is essential to health. It is essential for protein metabolism, cell growth, and the immune systems.

  Vitamin E:  A powerful antioxidant, vitamin E helps maintain healthy skin cells by eliminating harmful free radicals generated in the course of cellular metabolism. Studies have also indicated that vitamin E may help skin recover from acne scarring and reduce the appearance of scars left by acne.

  Protodioscin:  The active ingredient in the herb Tribulus terrestris, protodioscin has been clinically proven to help maintain optimal cell health by maintaining the proper balance of natural metabolites and hormones in your body.

 Simply a Better Choice for Acne Treatment:PotatoClear is scientifically formulated to act in two synergistic ways to give you healthy skin and a clear complexion.

 First, with its natural antiseptic ingredients, PotatoClear gets rid of existing acne breakouts naturally and helps eliminate the red spots left by acne. Second, PotatoClear's vitamins and herbal nutrients help nourish your skin to keep it healthy and to prevent future breakouts.

 When used regularly, PotatoClear will:

 Clear up acne breakouts fast - within only 2 to 4 days for most people
 Treat red spots and blemishes
 Work for body acne and adult acne, as well as regular acne breakouts
 Help prevent future acne breakouts
 Achieve & maintain healthy skin and clear complexion naturally
 


   Combination and case study:2.Protodioscin and treatment for Age-Related Sexual Performance Decline:

   Age-Related Decline in Male Sexual Performance:

 One of the most common complaints of aging men is the decline in their sexual performance. Men's sexual peak usually occurs at around the age of 18. For most, it's usually downhill from there - for some, significant declines in sexual performance can occur as early as in their late 20s. Aging is usually correlated with a longer time to achieve full erection, a less firm erection, lower libido or sex drive, a decline in sexual stamina, inadequate sensation, and unsatisfactory ejaculation.

   Aging and Decline in Testosterone Level:

 As men age, their production of DHEA, as well as testosterone and other androgens or sex hormones decline. It's been estimated that for every year over the age of forty, men's testosterone level drops by one percent1. About twenty percent of men in their sixties and fifty percent of men in their eighties have significantly reduced testosterone levels.
 As testosterone is a key hormone in men's sexual functions, aging-related decline in testosterone levels has a negative impact on men's sexual performance.
 

   Other Factors that Contribute to Poor Sexual Performance:

 For some men, the effect of aging on the decline in their sexual performance is further complicated with other factors, such as pain and fatigue. Pain caused by age-related diseases, such as arthritis and diabetes, can make sex less enjoyable. Likewise, fatigue and muscle soreness can impair men's sex drive.
 As sexual performance is closely related to men's overall health, factors that affect general health, such as anxiety, stress, and psychological factors, can also affect sexual performance. Fortunately, any decline associated with these factors is usually reversed once the underlying factors are resolved.
 Other causes of poor sexual performance include cigarette smoking and tobacco chewing, as well as alcohol and drug abuse.

   Reversing the Decline in Sexual Performance:

 The good news is that much of the aging-related decline in men's sexual performance can be reversed. First, men should aim for a healthy, stress-free, and active lifestyle. Quitting smoking, alcohol, and drug use - if they are a factor - can contribute not only to better sexual performance, but also overall health.
 Age-related decline in testosterone level can also be medically treated by testosterone replacement therapy. Here, the purpose of the therapy is to increase serum level of this hormone by oral administration, injection, or transdermal delivery of testosterone.
 Although generally safe, testosterone replacement therapy may not be suitable for all candidates and can carry substantial health risks and side effects. In addition to requiring close monitoring of serum androgen levels, testosterone replacement therapy should only be administered by qualified physicians.

   Protodioscin for Age-Related Sexual Performance Decline:

 An herbal extract has been shown by clinical studies to be promising in reversing this age-related decline in men's sexual performance. Protodioscin, the main active ingredient in the herbal plant Tribulus terrestris, have been shown by clinical studies to increase the level of DHEA and testosterone in men.
 A clinical study on fifteen men with decreased sexual performance showed that nearly 90% of men treated with protodioscin (in form of Libilov Supplement) at 500mg 3x daily for 60 days experienced improved libido, erection, ejaculation, and orgasm as compared to before the treatment.
 Here, protodioscin treatment resulted in significantly increased sex drive 33% of men after 30 days and in 80% of men after 60 days. Similarly, arousal improved in 53% of men after 30 days and 87% of men after 60 days. Orgasm sensation and ejaculate quality also improved significantly in 40% and 87% of men after 30 and 60 days, respectively.
 In another clinical study, 60 non-diabetic men with and without erectile dysfunctions and 15 diabetic men with sexual performance problems were given protodioscin (Libilov) at 3 x 250 mg per day for 3 weeks. The study found that in addition to increased DHEA levels in the treated group, the frequency of successful intercourse increased by 60%.
 In addition, an improved sense of well-being, improved sensation, erection, ejaculation, and orgasm were also reported by the treated men In these and other clinical studies on Tribulus terrestris' protodioscin, no unwanted side effects or contraindications were found.
 


   Combination and case study:3.Protodioscin and Super Volume Plus:

 Super Volume Plus has been developed with a unique "Plus" potency formula, medically backed to bring you results quickly and effectively.

 The completely natural formula triggers sexual desire by increasing the flow of blood to the penis.
 
 As you can see from the diagrams in a flaccid state the penis acts like any other part of the body, receiving the same flow of blood as the rest of the body.

 However, in erect state blood rushes to the penis and is absorbed in the Caverosa and Spongiosum. Super Volume Plus by Lativio works by increasing the flow of blood and therefore erections become harder, longer and more satisfying.
 The second part of the system works towards increasing the amount of ejaculate that you produce. Super Volume Plus is specifically formulated to increase semen production. This all natural solution can also increase sperm production and mobility.
 

 As you can see Super Volume Plus Formula provides you with the right ingredients to bring you the best possible results.
 We understand that there are many products out there on the market. However, only Super Volume with the new "Plus" formula offers you the most effective results
 

 Solidilin:  One component in the Solidilin compound has shown in numerous studies to improve sexual quality and motivation. In one study by the School of Pharmaceutical Sciences (University of Science Malaysia) results showed a significant enhancement in the sexual qualities of middle-aged rats. The compound also contains L-Dopa, the precursor to dopamine, which is the pleasure-giving neurotransmitter in the brain.
 

 Xi lan rou gui and Hong hua fen:  Xi lan rou gui and Hong hua fen are both vasodilators, meaning they open up the blood vessels to encourage more blood flow. In other words, they can increase blood flow to the penis, causing an erection to occur. This expansion of the vascular spaces of the penis reduce blood outflow, thus sustaining the length of an erection. In addition, Hong hua fen contains omega 3 fatty acids which have been shown to reduce the chances of heart disease.
 

 Ku Gua:  Along with existing as an incredible aid to those with diabetes and indigestion, Ku Gua has also been shown to reduce body fat thereby increasing body testosterone levels. A high level of testosterone is essential to increased semen production and sexual desire. It's a fantastic source of Vitamin C and in studies in rats; it has been shown to promote antispermatogenesis. Additionally, Chinese researchers have found that it contains proteins which show promise in promoting anti-HIV activity.
 

 4', 5, 7- Trihydroxyflavone and Embilica officinalis:   4', 5, 7- Trihydroxyflavone is a citrus bioflavonoid used primarily in the prevention and treatment of cancer. Embilica officinalis is the world's richest source of Vitamin C. Bioflavonoids, such as 4', 5, 7- Trihydroxyflavone, are thought to work synergistically with Vitamin C in the maintenance of blood vessel health. This pairing works to keep your sexual organ healthy and functioning properly over the long term.
 

 San guo mu:  Used mainly in cardiovascular health, San guo mu is an important component of a healthy sexual lifestyle. Regulating blood pressure and heart rate, this herb works to pace the body, which has been seen to be an incredibly beneficial trait during sex.
 

 Dong Chong Xia Cao:  This agent increases testosterone production, thus aiding tremendously in your enhancement efforts. In a study of mice given Dong Chong Xia Cao, plasma testosterone levels were significantly induces in both 3-day and 7-day trials. Testosterone is directly responsible for the development and maintenance of sex drive in males.
 

 Zinc Oxide:  Zinc aids in sperm motility and quality. It is also is very important in the metabolism of testosterone. Zinc, in the form of zinc gluconate, is more easily tolerated than other forms. Studies have shown Zinc supplements to be essential in replenishing Zinc levels absent in many modern diets. Zinc is also very important in increasing fertility and sexual vigour.
 

 Ling Zhi:  Ling Zhi is recorded to increase stamina and energy. Also boasting anti-allergic, anti-inflammatory, anti-viral, anti-bacterial, and antioxidant properties, reishi is known to lift the mood and increase one's sense of spirit and vitality. The benefits of reishi translate perfectly to the bedroom.
 

 Xian Mao:  Found in the South-Eastern part of China, Xian Mao is a safe and natural aphrodisiac used in Chinese traditional medicine and Ayurvedic medicine. It has been touted by some as a natural alternative to Viagra and is hailed for its many beneficial qualities.
 

 Tian Men Dong:  Acting as a full system tonic, Shatarvi has also been shown to aid males suffering from sexual debility and impotence. Overall, it has a calming affect on the body, stabilizing body weight, decreasing nervousness and promoting healthy sleep.
 

 Drilizen:  Drilizen is known to increase nitric oxide release, which prolongs erections through coronary vasodilatation. Nitric oxide also relaxes vascular smooth muscle via parasympathetic stimulation, which allows blood to flow to the penis and reach erection rapidly. Drilizen contains a protein amino acid that is the precursor to nitric oxide in the body.
 Drilizen increases testosterone production, in that it also contains an active ingredient known as protodioscin. Protodioscin increases the secretion of luteinizing hormone (also known as interstitial cell-stimulating hormone.) This hormone, in turn regulates the secretion of testosterone from the Leydig (interstitial) cells in the testes.
 

 Fucus Vesiculosus:  A type of seaweed found on the Atlantic and Pacific coasts, Fucus Vesiculosus promotes thyroid health and is also used in cases of high cholesterol, arteriosclerosis, overweight, and exhaustion. A healthy thyroid streamlines the metabolism making it more efficient and effective. Healthy metabolism is an integral part of both penis enhancement and sexual health.


   Protodioscin Toxicology:G.Tanev, S.Zarkova, 1980.

   Acute toxicity.:

 The acute toxicity of protodioscin was studied after intraperitoneal and oral application to albino mice, H line (18 - 20 mg body mass) and albino rats (160 - 180 g body mass). LD50 was also studied. It was concluded that the product can be included in the group of practically nontoxic substances. LD50 was 1942 mg/kg body mass with intraperitoneal application to mice and over 10,000 mg/kg body mass - with oral administration. The mean lethal dose of protodioscin with intraperitoneal application to rats was 750 (375 +/- 1,500 ) mg body mass, and after oral administration - over 10,000 mg/kg.

   Subacute toxicity.:

 The protodioscin was administered orally to albino Wistar rats for 30 and 90 days in the following doses: 75 mg/kg, 150 mg/kg, 225 mg/kg and 300 mg/kg body mass. No increased lethality was observed, nor a change in the behavior of the animals. No significant changes were observed in the routine clinical-laboratory and biochemical indices, nor morphological changes in the internal organs.

   Chronic toxicity.:

 Protodioscin was administered orally to albino rats for 6 months in doses of 75 mg/kg and 150 mg/kg body mass, as well as in 75 mg/kg body mass for 180 days to beagle dogs. The following toxic symptoms were looked for: changes in behavior, changes in the hematological, biochemical, functional and morphological parameters. No significant changes were found both in the behavior and in the reflexes of the animals. No increased lethality was observed. No pathological deviations from the physiological values were found in all hematological and clinical-chemical indices studied. No pathological changes in the structure of the internal organs, related to the toxic effect of the preparation, were detected.
 Teratological and embryotoxic studies were simultaneously performed, as well as some experiments to follow the pre- and postnatal development (Z.Ilieva, 1980).
 No teratogenic and embryotoxic action, nor deleterious effect on the development of the first generation after its littering, were found after the oral administration of the product in a dose of 750 mg/kg body mass to pregnant Wistar rats.
 Studies were carried out to exclude the possible carcinogenic potential of protodioscin during a long-term treatment of rats (Gendzhev, 1981).
 Increased incidence of neoplasms compared to the control animals was not observed with daily doses of 50 and 150 mg/kg body weight, administered orally for 23 months. No toxic damage was found morphologically in the rat organs.

   Research Update:Protodioscin

   Protodioscin for Hair loss treatment::

 The active ingredient of the herb Tribulus terrestris L., protodioscin has been proven by many clinical studies to help regulate the body's androgen levels and may help in preventing hair loss due to the overproduction of the androgen DHT.

   Structural identification of methyl protodioscin metabolites in rats' urine and their antiproliferative activities against human tumor cell lines.:

 Methyl protodioscin (MPD), a furostanol saponin, is a preclinical drug shown potent antiproliferative activities against most cell lines from leukemia and solid tumors. The metabolites of MPD in rats' urine after single oral doses of 80 mg/kg were investigated in this research. Ten metabolites were isolated and purified by liquid-liquid extraction, open-column chromatography, medium-pressure liquid chromatography, and preparative high-performance liquid chromatography. The structural identification of the metabolites was carried out by high resolution mass spectra, NMR spectroscopic methods including (1)H NMR, (13)C NMR and 2D NMR, as well as chemical ways. The 10 metabolites were elucidated to be dioscin (M-1), pregna-5,16-dien-3beta-ol-20-one-O-alpha-l-rhamnopyranosyl-(1-->2)-[alpha-l-rhamnopyranosyl-(1-->4)]-beta-d-glucopyranoside (M-2), diosgenin (M-3), protobioside (M-4), methyl protobioside (M-5), 26-O-beta-d-glucopyrannosyl(25R)-furan-5-ene-3beta, 22alpha, 26-trihydroxy-3-O-alpha-l-rhamnopyranosyl-(1-->4)-beta-d-glucopyranoside(M-6),26-O-beta-d-glucopyranosyl(25R)-furan-5-ene-3beta,26-dihydroxy-22-methoxy-3-O-alpha-l-rhamnopyranosyl-(1-->4)-beta-d-glucopyranoside (M-7), prosapogenin A of dioscin (M-8), prosapogenin B of dioscin (M-9), and diosgenin-3-O-beta-d-glucopyranoside (M-10), respectively. M-1 was the main urinary metabolite of MPD in rats. Some metabolites showed potent antiproliferative activities against HepG2, NCI-H460, MCF-7 and HeLa cell lines in vitro.

   Facile conversion of spirostan saponin into furostan saponin: synthesis of methyl protodioscin and its 26-thio-analogue.:

 A facile approach for the conversion of a spirostan saponin into its furostan counterpart, as illustrated by the transformation of dioscin to methyl protodioscin (and its 26-thio-analogue), has been developed.

   Microbial metabolism of methyl protodioscin by Aspergillus niger culture-A new androstenedione producing way from steroid.:

 Methyl protodioscin, a natural furostanol biglycoside steroid, was a preclinical anticancer drug, which showed potent activity against most cell lines from leukemia and solid tumors in the National Cancer Institute's (NCI) human cancer panel. Metabolism of methyl protodioscin by Aspergillus niger was investigated. Seven metabolites were isolated and identified. Two main metabolites were pregnane glycosides and four were furostanol glycosides, together with the aglycone. It was found that steroidal saponin skeleton could be converted to pregnenolone skeleton only using microbial methods, which must have chemical procedures in the reported literatures. The proposed biosynthetic pathways of the microbial conversion products of methyl protodioscin were drawn. The found enriched the reaction types of microbial bioconversion and provided a new producing way of androstenedione from steroid. Most metabolites showed strong cytotoxic activities against HepG2, NCI-H460, HeLa, and MCF-7 cell lines.
 

   Methyl protodioscin induces G2/M cell cycle arrest and apoptosis in HepG2 liver cancer cells.:

 Methyl protodioscin (NSC-698790) is one of the main bioactive components in the traditional Chinese medicine Dioscorea collettii var. hypoglauca (Dioscoreaceae). In this study, we investigated the anti-proliferative effect of methyl protodioscin on the HepG2 cells and the mechanism of the induced cytotoxicity. Treatment of methyl protodioscin resulted in G2/M arrest and apoptosis in HepG2 cells. These effects were attributed to down-regulation of Cyclin B1 and the signaling pathways leading to up-regulation of Bax and down-regulation of BCL2, suggesting that methyl protodioscin may be a novel anti-mitotic agent.

   A new steroidal saponin from Dioscorea cayenensis.:

 The new 26-O-beta-D-glucopyranosyl-3beta,26-dihydroxy-20,22-seco-25(R)-furost-5-en-20,22-dione-3-O-alpha-L-rhamnopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-(1-->4)-[alpha-L-rhamnopyranosyl-(1-->2)]-beta-D-glucopyranoside (1), along with the known methyl protodioscin (2), asperoside (3) and prosapogenin A of dioscin (4) were isolated from the rhizomes of Dioscorea cayenensis LAM.-HOLL (Dioscoreaceae). Their structures were established mainly on the basis of 600 MHz 2D-NMR spectral data. 4 exhibited antifungal activity against the human pathogenic yeasts Candida albicans, C. glabrata and C. tropicalis (MICs of 20.8, 6.25, 25 microg/ml, respectively), whereas saponins 1-3 were inactive.

   Steroidal saponins from Dioscorea panthaica and their cytotoxic activity.:

 A new steroidal saponin, dioscoreside E (1), and a known compound, protodioscin (2), were isolated from an ethanol extract of the rhizomes of Dioscorea panthaica. The structure of 1 was established as 3-O-[bis-alpha-L-rhamnopyranosyl-(1 --> 2 and 1 --> 4)-beta-D-glucopyranosyl]-26-O-beta-D-glucopyranosyl-20(R)-methoxy-25(R)-furosta-5,22(23)-diene-3beta,26-diol, on the basis of spectral and chemical evidence. Compounds 1 and 2 showed cytotoxic activity against a panel of tumor cell lines.

   Quantification of protodioscin and rutin in asparagus shoots by LC/MS and HPLC methods.:

 A liquid chromatography/mass spectrometry (LC/MS) method with selected ion monitoring was developed and validated to analyze the contents of protodioscin and rutin in asparagus. The distribution of rutin and protodioscin within the shoots was found to vary by location, with the tissue closest to the rhizome found to be a rich source of protodioscin, at an average level of 0.025% tissue fresh weight in the three tested lines, while the upper youngest shoot tissue contained the highest amount of rutin at levels of 0.03-0.06% tissue fresh weight. The lower portions of the asparagus shoots that are discarded during grading and processing should instead be considered a promising source of a new value-added nutraceutical product.

   Protodioscin (NSC-698 796): its spectrum of cytotoxicity against sixty human cancer cell lines in an anticancer drug screen panel.:

 Protodioscin (NSC-698 796) is a furostanol saponin isolated from the rhizome of Dioscorea collettii var. hypoglauca (Dioscoreaceae), a Chinese herbal remedy for the treatment of cervical carcinoma, carcinoma of urinary bladder and renal tumor for centuries. To systematically evaluate its potential anticancer activity, protodioscin was tested for cytotoxicity in vitro against 60 human cancer cell lines in the NCI's (National Cancer Institute, USA) anticancer drug screen. As a result, protodioscin was cytotoxic against most cell lines from leukemia and solid tumors in the NCI's human cancer panel, especially selectively against one leukemia line (MOLT-4), one NSCLC line (A549/ATCC), two colon cancer lines (HCT-116 and SW-620), one CNS cancer line (SNB-75), one melanoma line (LOX IMVI), and one renal cancer line (786 - 0) with GI50 < or = 2.0 microM. In the general view of mean graphs, leukemia, colon cancer and prostate cancer are the most sensitive subpanels, while ovarian cancer is the least sensitive subpanel. Based on an analysis of COMPARE computer program with protodioscin as a seed compound, no compounds in the NCI's anticancer drug screen database have cytotoxicity patterns (mean graphs) similar to those of protodioscin, indicating that a potential novel mechanism of anticancer action is involved.

   Determination of steroidal saponins in Tribulus terrestris by reversed-phase high-performance liquid chromatography and evaporative light scattering detection.:

 This paper describes the first analytical method suitable for the determination of steroidal saponins in Tribulus terrestris. A separation by high performance liquid chromatography (HPLC) was achieved by using a reversed-phase (RP-18) column, evaporative light scattering (ELS) detection, and a water/acetonitrile gradient as the mobile phase. The marker compound, protodioscin, was detected at a concentration as low as 10.0 microg/mL. Several different samples of plant material were successfully analyzed, and depending on origin and plant part used for extraction, significant differences in the composition of the saponins were observed. The analysis of market products showed considerable variations of 0.17 to 6.49% in the protodioscin content.

   Aphrodisiac properties of Tribulus Terrestris extract (Protodioscin) in normal and castrated rats.:Gauthaman K , Adaikan PG , Prasad RN.Source:Life Sci, 71(12): 1385-96 2002

 Tribulus terrestris (TT) has long been used in the traditional Chinese and Indian systems of medicine for the treatment of various ailments and is popularly claimed to improve sexual functions in man. Sexual behaviour and intracavernous pressure (ICP) were studied in both normal and castrated rats to further understand the role of TT containing protodioscin (PTN) as an aphrodisiac. Adult Sprague-Dawley rats were divided into five groups of 8 each that included distilled water treated (normal and castrated), testosterone treated (normal and castrated, 10 mg/kg body weight, subcutaneously, bi-weekly) and TT treated (castrated, 5 mg/kg body weight, orally once daily). Decreases in body weight, prostate weight and ICP were observed among the castrated groups of rats compared to the intact group. There was an overall reduction in the sexual behaviour parameters in the castrated groups of rats as reflected by decrease in mount and intromission frequencies (MF and IF) and increase in mount, intromission, ejaculation latencies (ML, IL, EL) as well as post-ejaculatory interval (PEI). Compared to the castrated control, treatment of castrated rats (with either testosterone or TT extract) showed increase in prostate weight and ICP that were statistically significant. There was also a mild to moderate improvement of the sexual behaviour parameters as evidenced by increase in MF and IF; decrease in ML, IL and PEI. These results were statistically significant. It is concluded that TT extract appears to possess aphrodisiac activity probably due to androgen increasing property of TT (observed in our earlier study on primates).

   Proerectile pharmacological effects of Tribulus terrestris extract on the rabbit corpus cavernosum.:Adaikan PG , Gauthaman K , Prasad RN , Ng SC.Source:Ann Acad Med Singapore, 29(1): 22-6 2000

 INTRODUCTION: The objective of the present study was to investigate the effect of oral treatment of Tribulus terrestris (TT) extract on the isolated corpus cavernosal tissue of New Zealand white (NZW) rabbits and to determine the mechanism by which protodioscin (PTN), a constituent of the TT, exerts its pharmacological effects. MATERIALS AND METHODS: Twenty-four NZW rabbits were randomly assigned to 4 experimental groups of 6 each. Group I served as control. Groups II to IV were treated with the extract at different dose levels, i.e. 2.5 mg/kg, 5 mg/kg and 10 mg/kg body weight, respectively. The TT extract was administered orally, once daily, for a period of 8 weeks. The rabbits were then sacrificed and their penile tissue isolated to evaluate the responses to both contracting and relaxing pharmacological agents and electrical field stimulation (EFS). RESULTS: PTN on its own had no effect on the isolated corpus cavernosal strips. The relaxant responses to EFS, acetylcholine and nitroglycerin in noradrenaline precontracted tissues from treated groups showed an increase in relaxation of a concentration dependent nature compared to that of the tissues from control group. However, the contractile, anti-erectile response of corpus cavernosal tissue to noradrenaline and histamine showed no significant change between the treatment and the control groups. CONCLUSIONS: The relaxant responses to acetylcholine, nitroglycerin and EFS by more than 10%, 24% and 10% respectively compared to their control values and the lack of such effect on the contractile response to noradrenaline and histamine indicate that PTN has a proerectile activity. The enhanced relaxant effect observed is probably due to increase in the release of nitric oxide from the endothelium and nitrergic nerve endings, which may account for its claims as an aphrodisiac. However, further study is needed to clarify the precise mechanism of its action.

   Phytochemicals and the breakthrough of traditional herbs in the management of sexual dysfunctions.:Adimoelja A.Source:Int J Androl, 23 Suppl 2(): 82-4 2000

 Traditional herbs have been a revolutionary breakthrough in the management of erectile dysfunction and have become known world-wide as an 'instant' treatment. The modern view of the management of erectile dysfunction subscribes to a single etiology, i.e. the mechanism of erection. A large number of pharmacological agents are orally consumed and vasoactive agents inserted intraurethrally or injected intrapenially to regain good erection. Modern phytochemicals have developed from traditional herbs. Phytochemicals focus their mechanism of healing action to the root cause, i.e. the inability to control the proper function of the whole body system. Hence phytochemicals manage erectile dysfunction in the frame of sexual dysfunction as a whole entity. Protodioscin is a phytochemical agent derived from Tribulus terrestris L plant, which has been clinically proven to improve sexual desire and enhance erection via the conversion of protodioscine to DHEA (De-Hydro-Epi-Androsterone). Preliminary observations suggest that Tribulus terrestris L grown on different soils does not consistently produce the active component Protodioscin. Further photochemical studies of many other herbal plants are needed to explain the inconsistent results found with other herbal plants, such as in diversities of Ginseng, Eurycoma longifolia, Pimpinella pruacen, Muara puama, Ginkgo biloba, Yohimbe etc.

   Protodioscin (NSC-698 796): its spectrum of cytotoxicity against sixty human cancer cell lines in an anticancer drug screen panel.:Hu K , Yao X.Source:Planta Med, 68(4): 297-301 2002

 Protodioscin (NSC-698 796) is a furostanol saponin isolated from the rhizome of Dioscorea collettii var. hypoglauca (Dioscoreaceae), a Chinese herbal remedy for the treatment of cervical carcinoma, carcinoma of urinary bladder and renal tumor for centuries. To systematically evaluate its potential anticancer activity, protodioscin was tested for cytotoxicity in vitro against 60 human cancer cell lines in the NCI's (National Cancer Institute, USA) anticancer drug screen. As a result, protodioscin was cytotoxic against most cell lines from leukemia and solid tumors in the NCI's human cancer panel, especially selectively against one leukemia line (MOLT-4), one NSCLC line (A549/ATCC), two colon cancer lines (HCT-116 and SW-620), one CNS cancer line (SNB-75), one melanoma line (LOX IMVI), and one renal cancer line (786 - 0) with GI50 < or = 2.0 microM. In the general view of mean graphs, leukemia, colon cancer and prostate cancer are the most sensitive subpanels, while ovarian cancer is the least sensitive subpanel. Based on an analysis of COMPARE computer program with protodioscin as a seed compound, no compounds in the NCI's anticancer drug screen database have cytotoxicity patterns (mean graphs) similar to those of protodioscin, indicating that a potential novel mechanism of anticancer action is involved.

   Determination of steroidal saponins in Tribulus terrestris by reversed-phase high-performance liquid chromatography and evaporative light scattering detection.:Ganzera M , Bedir E , Khan IA.Source:J Pharm Sci, 90(11): 1752-8 2001

 This paper describes the first analytical method suitable for the determination of steroidal saponins in Tribulus terrestris. A separation by high performance liquid chromatography (HPLC) was achieved by using a reversed-phase (RP-18) column, evaporative light scattering (ELS) detection, and a water/acetonitrile gradient as the mobile phase. The marker compound, protodioscin, was detected at a concentration as low as 10.0 microg/mL. Several different samples of plant material were successfully analyzed, and depending on origin and plant part used for extraction, significant differences in the composition of the saponins were observed. The analysis of market products showed considerable variations of 0.17 to 6.49% in the protodioscin content.

   Two new sulfated furostanol saponins from Tribulus terrestris.:Kostova I , Dinchev D , Rentsch GH , Dimitrov V , Ivanova A;Source:Z Naturforsch [C], 57(1-2): 33-8 0

 The known furostanol saponins methylprotodioscin and protodioscin and two new sulfated saponins, sodium salt of 26-O-beta-glucopyranosyl-22alpha-methoxy-(25R)-furost-5-ene-3beta,26-diol-3-O-alpha-rhamnopyranosyl-(1-->2)-beta-4-O-sulfo-glucopyranoside (methylprototribestin) and sodium salt of 26-O-beta-glucopyranosyl-22alpha-hydroxy-(25R)-furost-5-ene-3beta,26-diol-3-O-alpha-rhamnopyranosyl-(1-->2)-beta-4-O-sulfo-glucopyranoside (prototribestin) have been isolated from the aerial parts of Tribulus terrestris L. growing in Bulgaria. The structures of the new compounds were elucidated on the basis of 1D and 2D (DQF-COSY, TOCSY, HSQC-TOCSY, HSQC, HMBC, ROESY) NMR data, ESI mass spectra and chemical transformation.

   Phytochemicals and the breakthrough of traditional herbs in the management of sexual dysfunctions.:Adimoelja A,Source:Int J Androl, 23 Suppl 2(): 82-4 2000

 Traditional herbs have been a revolutionary breakthrough in the management of erectile dysfunction and have become known world-wide as an 'instant' treatment. The modern view of the management of erectile dysfunction subscribes to a single etiology, i.e. the mechanism of erection. A large number of pharmacological agents are orally consumed and vasoactive agents inserted intraurethrally or injected intrapenially to regain good erection. Modern phytochemicals have developed from traditional herbs. Phytochemicals focus their mechanism of healing action to the root cause, i.e. the inability to control the proper function of the whole body system. Hence phytochemicals manage erectile dysfunction in the frame of sexual dysfunction as a whole entity. Protodioscin is a phytochemical agent derived from Tribulus terrestris L plant, which has been clinically proven to improve sexual desire and enhance erection via the conversion of protodioscine to DHEA (De-Hydro-Epi-Androsterone). Preliminary observations suggest that Tribulus terrestris L grown on different soils does not consistently produce the active component Protodioscin. Further photochemical studies of many other herbal plants are needed to explain the inconsistent results found with other herbal plants, such as in diversities of Ginseng, Eurycoma longifolia, Pimpinella pruacen, Muara puama, Ginkgo biloba, Yohimbe etc.


  Scientific References:

  1.Dioscorea gracillima miq extract and Protodioscin:Functions,Combination case study and Research findings.......
  2.Pharmacological, pharmacokinetic, toxicological and clinical studies on protodioscin.I. Viktorov, E. Bozadjieva, M. Protich, et al. Higher Medical Institute; Medical Academy Institute of Endocrinology, Gerontology and Geriatrics; Medical Academy Institute of Obstetrics and Gynecology, Bulgaria IIMS Therapeutic Focus (1994)