What is Transresveratrol?Basic Information,Super Function and Researches of resveratrol and Polygonum Cuspidatum Extract.Polygonum Cuspidatum Extract.Resveratrol.

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Health Benefits and research of transreveratrol.

Polygonum Cuspidatum Extract Resveratrol CAS.NO 510-36-0 photo picture image Mechanism of Transresveratrol as natural antibiotics and cancer inhibitor.

 Specifically trans-resveratrol can help inhibit all three stages of cancer by:

 Inducing quinone reductase activity, an enzyme that is capable of detoxifying carcinogens.

 Inhibiting cyclo-oxygenase, a substance that causes the production of prostaglandins that stimulate tumor growth, suppress the immune system and activate carcinogens.

 Inducing the expression of nitroblue tetazolium reduction activity, a marker of non-specific acid esterase activity and macrophage formation.

 Furthermore trans-resveratrol can inhibit the development of cardiovascular disease. This is performed through its ability as an antioxidant to inhibit platelet aggregation and eicosaniod synthesis and its ability to modulate lipoprotein metabolism.

 In humans, studies are underway to determine health benefits of resveratrol in cancer and heart disease. Preliminary research results demonstrate that resveratrol may have anti-infective, antioxidant, and anti-inflammatory properties. According to studies involving cancer-prone mice, resveratrol seems to reduce the occurrence of skin tumors. Additional studies suggest that resveratrol is unique because of its ability to battle cancer at all three steps of the cancer process: initiation, promotion, and progression.

 Researchers believe that resveratrol is partially responsible for the cholesterol-lowering effects of red wine. Epidemiologic and clinical studies suggest that high consumption of resveratrol-rich foods may result in reduced cardiovascular disease risk, lowered total cholesterol, and lowered LDL cholesterol. Resveratrol's antioxidant properties may again be the mechanism at work in reducing the oxidation of LDL cholesterol. Currently scientists are exploring additional potential health benefits of resveratrol.

 Resveratrol doses for inhibition, (i.e. assistance in the prevention) of cancer and cardiovascular disease are 5mg or 10mg daily. Doses for the treatment of the same are 15mg to 30mg daily.

 Trans-Resveratrol, the active ingredient that makes up 50 percent of the extract, acts as an antioxidant, anti-mutagenic, and anti-inflammatory by lowering COX-2. It elevates cyclic AMP,which increases metabolic activity in the cell, decreases platelet aggregation, and decreases levels and inhibits oxidation of LDL cholesterol.

 Research shows it to be a powerful phytoestrogen that can help maintain normal estrogen activity, reduce hot flashes, balance mood swings, and promote bone density. Resveratrol promotes cardiovascular health and helps prevent premature aging for both sexes.

 A recent in vitro study with human cells showed Resveratrol was 99.9 percent effective in halting the reproduction of herpes, shingles, and other viruses and inhibited the growth of cancer cells. Research suggests that 20mg per day of Resveratrol may be able to promote longevity by stimulating the human cell-survival enzyme that is known to increase by restricting caloric intake.

 Cancer Chemopreventive Activity and tumor inhibition of Tran-resveratrol from Polygonum cuspidatum extracts:

 Cancer is the largest single cause of death in both men and women, claiming over 6 million lives each year worldwide. Chemoprevention, the prevention of cancer by ingestion of chemical agents that reduce the risk of carcinogenesis, is one of the most direct ways to reduce morbidity and mortality. Cancer chemopreventive agents include nonsteroidal anti-inflammatory drugs (NSAIDs) such as indomethacin, aspirin, piroxicam, and sulindac, all of which inhibit cyclooxygenase (COX) .

 This inhibitory activity is relevant to cancer chemoprevention because COX catalyzes the conversion of arachidonic acid to pro-inflammatory substances such as prostaglandins,which can stimulate tumor cell growth and suppress immune surveillance. In addition, COX can activate carcinogens to forms that damage genetic material.

 The process of chemical carcinogenesis can be divided into three general stages, and chemopreventive agents have been categorized according to the stage that they inhibit.

 Resveratrol has also been shown to have potent anticancer activity. It modulates the expression of the COX-2 enzyme, which is important in promoting tumorigenesis. It does this by suppressing the activation of the COX-2 gene expression, which leads to the inhibition of the protein kinase C signal transduction pathway. Additionally, resveratrol directly inhibits the activity of COX-2 (Subbaramaiah 1998). In human HepG2 hepatoma cells, resveratrol inhibits enzymes which metabolize arylhydrocarbons to genotoxic metabolites and acts as a competitive agonist of the arylhydrocarbon receptor (Ciolino 1998). This is important because this activity can reduce endothelial cell damage caused by environmental toxicants.

 Transresveratrol inhibits cellular events associated with tumor initiation, promotion, and progression. As noted above, the compound was identified on the basis of its ability to inhibit the cyclooxygenase activity of COX-1 (median effective dose ED50 5 15 mM) (Fig. 2A), and this activity correlates with antitumor promotion. Although its inhibitory activity was less than that of certain NSAIDs, such as indomethacin (ED50 5 2.3 mM) (Fig. 2A),it was much greater than that mediated by compounds such as aspirin (ED50 5 880mM). Also, unlike indomethacin and most other NSAIDs, resveratrol inhibited the hydroperoxidase activity of COX-1 (ED50 5 3.7 mM)

 Resveratrol-mediated inhibition was specific for the cyclooxygenase activity of COX-1 because there was no discernable activity when oxygen uptake was assessed with COX-2 (Fig. 2A), an inducible form of the enzyme associated with responses such as inflammation, and inhibition of the hydroperoxidase activity of COX-2 (ED50 5 85 mM) was greatly reduced relative to the activity observed with COX-1.

 On the basis of these results, researchers investigated the anti-inflammatory activity of resveratrol. In the carrageenan-induced model of inflammation in rats, resveratrol significantly reduced pedal edema both in the acute phase (3 to 7 hours) and in the chronic phase (24 to 144 hours). The edema-suppressing activity of resveratrol was greater than that of phenylbutazone and was similar to that of indomethacin.

 Overall, these data demonstrate the potential of resveratrol to inhibit tumor promotion.

 Western research has also discovered potential applications of this herb for cancer -- several compounds have shown possible usefulness, including emodin, resveratrol and chrysophanol. These compounds have shown antitumor, antimetastatic, chemopreventive, chemical carcinogenesis-inhibitive, oncogene signal transduction-inhibitive and immunomodulating properties. One study also demonstrated that Hu Zhang was able to increase white blood cells (WBC's, aka leukocytes) in patients with lowered WBC levels due to radiation treatment.

 In 1997, resveratrol was reported to be one of the most potent chemopreventive agents able to block all three phases of tumor development that includes initiation, promotion, and progression, induced by the aryl hydrocarbon DMBA. How resveratrol exerts its anticarcinogenic effects is only partially understood. This polyphenol has been shown to inhibit the growth of a wide variety of tumor cells, including leukemic, prostate, breast, and endothelial cells. The ability of resveratrol to induce the expression of CD95L (also called FasL), p53, and p21 may contribute to its growth-inhibitory effects. The suppression of cyclooxygenase-2 (COX-2), cytochrome p450, and c-fos expression by resveratrol may account for its ability to inhibit tumor promotion. Recently, the drug was reported to be a phytoestrogen that behaves as superagonist of estrogen receptor and thereby an inducer of tumor cell proliferation. Its structural similarity with estrogen may also account for its cardioprotective effects.

 Because the carcinogenic, inflammatory, and growth-modulatory effects of many chemicals are mediated by NF-B, we hypothesized that the suppression of NF-B activation pathway accounts for resveratrol's activities. Numerous lines of evidence suggest this possibility. For example, various agents that promote tumorigenesis are known to activate NF-B, including phorbol ester, okadaic acid, and TNF. Experiments in TNF-deficient mice showed that TNF is required for tumor promotion. In addition, several genes that are involved in tumorigenesis, metastasis, and inflammation are regulated by NF-B. A critical role for NF-B in cellular transformation has also been reported.

 Most agents that activate NF-B also activate another transcription factor, AP-1. That AP-1 activation mediates tumorigenesis and invasiveness has also been described. The activation of NF-B and AP-1 is regulated by several protein kinases that belong to the mitogen-activated protein kinase (MAPK) family. The activation of NF-B and AP-1 and its associated kinases is in most cases dependent on the production of reactive oxygen species.

 In some recent study, scientists tested the hypothesis that the anti-inflammatory and anticarcinogenic effects of resveratrol are mediated through its modulation of NF-B and AP-1 activation, members of the MAPK, and caspase-mediated apoptosis. We demonstrated that resveratrol was a potent inhibitor of NF-B and AP-1 activation. It also inhibited TNF-induced c-Jun N-terminal protein kinase (JNK) and MAPK kinase (MEK) activation and caspase-induced apoptosis. Both reactive oxygen intermediate (ROI) generation and lipid peroxidation induced by TNF were also suppressed by resveratrol.
 Polygonum Cuspidatum Extract Resveratrol CAS.NO 510-36-0 photo picture image

 Brief Benefits of transresveratrol

 Key points:
 Protects against free radical injury in vivo
 Inhibits hydroxyl and peroxyl radicals
 Increases plasma and LDL polyphenols
 Inhibits brain monoamine oxidase in vivo
 Shown to inhibit the three stages of carcinogenesis and COX-2 activity:
 Normally formulated and combined with following herbs at a proper dosage function as a good COX-2 inhibitor:
 Holy Basil leaf extract (ursolic acid),Green Tea leaf extract,Rosemary leaf extract,Turmeric ethanolic extract,Ginger rhizome extract,Chinese Goldthread root extract,Barberry root extract,Oregano leaf extract,Scutellaria baicalensis root extract,etc.
 Exhibits anti-inflammatory properties.
 Decreases the "stickiness" of blood platelets and assures blood vessels remain open and flexible.
 Helps to support proper immune system health.
 Shown to inhibit LDL cholesterol oxidation.
 Helps to support normal cardiovascular function.
 Shown to exhibit phytoestrogen and cardioprotectant properties.
 Helps prevent the effects of premature aging.

 Medical Functions: anti viral,anti leptospirosis,anti fungal,relaxes the bronchial smooth muscles, expels phlegm, and suppresses asthma and cough,lower blood pressure and lipids,stops bleeding in external injuries,inhibits pain,astringent,anti inflammatory,antibiotic,like: Pseudomonas aeruginosa,Staphylococcus aureaus,Moraxella (Branhamella),catarrhalis,Streptococcal,Escherichia coli.

 Actions and Indications:For jaundice, gall bladder stones, blood stasis with menses stoppage, yeast infection, rheumatoid arthritis, physical injuries from impacts, inflammation of the bronchi, lobar pneumonia, poisonous snake bites, scalding injuries, acute hepatitis, urinary tract infection, boils, stoppage of menses due to heat in the blood, breast cancer, menopausal bleeding disorder.

 And trans:resveratrol also act as good inhibitor,more:
 killing bacteria and antibio:transresveratrol killing bacteria and act as bactericide.
 inhibitor of serum triglyceride synthesis:transresveratrol act as serum triglyceride synthesis inhibitor.
 lipid peroxidation inhibitor:research shows transresveratrol act as good lipid peroxidation inhibitor.
 platelet aggregation inhibitor:transresveratrol show good character of inhibiting platelet aggregation.
 detoxifying carcinogens,carcinogens inhibitor:transresveratrol could act as antidote of carcinogens,carcinogens inhibitor.
 cyclo-oxygenase inhibitor:transresveratrol inhibiting cyclo-oxygenase and act as inhibitor.
 prostaglandins inhibitor:transresveratrol act as prostaglandins inhibitor.
 inhibitor of brain monoamine oxidase:transresveratrol proved as brain monoamine oxidase inhibitor.
 inhibitor of hydroxyl radicals,hydroxyl radicals inhibitor--transresveratrol show super antioxidant property and inhibiting hydroxyl radicals very effectively.
 inhibitor of peroxyl radicals:transresveratrol proved also widely act as peroxyl radicals inhibitor but not only hydroxyl radicals inhibitor.
 cardioprotection in vivo:transresveratrol also showed act as cardioprotection in vivo.
 Inhibition of monoamine oxidase A:transresveratrol act as monoamine oxidase A inhibitor.
 inhibitor of malonaldehyde generation:resveratrol act as malonaldehyde generation inhibitor.
 inhibitor of HIV:transresveratrol also show good character and Anti-HIV Effects.

 Of course transresveratrol has many other good character and wide uses to be explored, so please read on:

 In China.transresveratrol is used as an antioxidant phenol and a potent vasodilator that inhibits serum triglyceride synthesis, lipid peroxidation, and platelet aggregation.

 It is extensively used for treatment of blood vessel disease such as atherosclerosis and hyperlipidemia. In addition,it has anti-virus and anti-inflammatory activity, can treat acute microbial infections and viral hepatitis, ect.

 Transresveratrol reduced oxidative stress in cultured brain cells (PC12 cells) induced by the addition of Fe2+ and t-butyl hydroperoxide, and increased the antioxidant protective effects of vitamins C and E under these same conditions.

 Transresveratrol also protected against free radical injury in cerebral ischemia. Ischemia refers to the obstruction of blood and oxygen flow through an organ, while restoration of blood and oxygen flow is termed reperfusion. Reperfusion induces more oxidative stress and damage to an organ than ischemia does.

 In an ischemia-reperfusion rat brain model, resveratrol glycoside decreased levels of free radicals and lipid peroxidation (as demonstrated by a reduction in malondialdehyde production) and increased the antioxidant activities of antioxidant enzymes such as superoxide dismutase, catalase, and glutathione peroxidase.

 A concentration of 10 milligrams per kilogram body weight had the greatest effect. Resveratrol increased plasma and LDL polyphenols and enhanced antioxidant activity as judged by decreased plasma peroxides. It also increased lag time and decreased LDL lipid peroxides and lipid peroxidation in the copper-catalyzed peroxidation of LDL conjugated dienes.

 Protykin, a natural extract of trans-resveratrol (20 percent) derived from the dried rhizome of Polygonum cuspidatum, scavenged both hydroxyl and peroxyl radicals in vitro, and provided significant cardioprotection in vivo. Supplementation of protykin to rats for three weeks dramatically improved postischemic left ventricular functions and aortic flow as compared to control animals.

 This was further supported by reduced myocardial (heart) infarct size, as measured by a computerized TTC staining method, and reduced malondialdehyde formation, a presumptive marker of oxidative stress. The researchers showed that protykin demonstrated dramatic cardioprotection, presumably by virtue of its potent free radical scavenging ability.

 Peroxidation of the LDL cholesterol from two healthy volunteers was inhibited by 81 percent and 70 percent upon the addition of 10 umol per liter of trans-resveratrol (2.5 mg per liter). In contrast, 10 umol per liter of a-tocopherol (natural vitamin E), which has been associated with a reduced risk of heart disease, had a much lower antioxidant potency than did resveratrol, and inhibited LDL cholesterol oxidation by only 40 percent and 19 percent.

 Inhibition of monoamine oxidase A was seen to be the prime factor responsible for the antioxidant activity of resveratrol. Monoamine oxidase is an enzyme found in most tissues, but especially in the liver and nervous system. It catalyzes the oxidation of a large variety of monoamines, including epinephrine, norepinephrine, and serotonin. Resveratrol and its derivatives induced a significant inhibitory effect on malonaldehyde generation-a marker of lipid per-oxidation and oxidative tissue injury-during thrombininduced platelet aggregation.

 Resveratrol also inhibited brain monoamine oxidase in rats (IC50 of 2 uM), even though lacking the structural features of classic monoamine oxidase inhibitors.

 It is thought that inhibiting monoamine oxidase in the brain may be a way to treat depression.
 Polygonum Cuspidatum Extract Resveratrol CAS.NO 510-36-0 photo picture image

 How is Resveratrol distributed within the body?

 Trans-resveratrol is well-absorbed by humans when taken orally, however its bioavailability is quite low as a result of its rapid metabolism and elimination.

 When human subjects were administered an oral dose of 25 mg of trans-resveratrol, the unchanged resveratrol was only detected in trace amounts in the blood, while resveratrol metabolites: trans-resveratrol-3-O-glucuronide and trans-resveratrol-3 peaked 30-60 minutes after administration at around 2 micromoles/liter. The bioavailability of resveratrol from grape juice, which contains mostly glucosides of resveratrol (piceid) may be even lower than that of trans-resveratrol.

 Information about the bioavailability of resveratrol in humans is still scarce since most of the basic research on resveratrol has been carried out using cultured cells exposed to unmetabolized resveratrol at concentrations that are often 10-100 times greater than peak concentrations observed in human plasma after oral consumption. In the gastro-intestinal tract, cells are exposed to unmetabolized resveratrol, however recent studies suggest that in humans, other tissues are exposed mainly to resveratrol metabolites. Information is still lacking about the biological activity of resveratrol metabolites, and it is unknown whether some tissues are capable of converting resveratrol metabolites back to its original form and what bioactivity that may have on the body.

 Resveratrol and its Metabolism and Bioavailability:

 Although trans-resveratrol appears to be well-absorbed by humans when taken orally, its bioavailability is relatively low due to its rapid metabolism and elimination. When healthy men and women took an oral dose of 25 mg of trans-resveratrol, only traces of the unchanged resveratrol were detected in plasma (blood), while plasma concentrations of resveratrol metabolites peaked 30-60 minutes later at concentrations around 2 micromoles/liter.

 The bioavailability of resveratrol from grape juice, which contains mostly glucosides of resveratrol (piceid) may be even lower than that of trans-resveratrol. Information about the bioavailability or resveratrol in humans is important because much of the basic research on resveratrol has been conducted in cultured cells exposed to unmetabolized resveratrol at concentrations that are often 10-100 times greater than peak concentrations observed in human plasma after oral consumption.

 Although cells that line the digestive tract are exposed to unmetabolized resveratrol, research in humans suggests that other tissues are exposed primarily to resveratrol metabolites. Little is known about the biological activity of resveratrol metabolites, and it is not known whether some tissues are capable of converting resveratrol metabolites back to resveratrol.

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Reference:

citations1.What is Transresveratrol?Basic Information,Super Function and Researches of resveratrol and Polygonum Cuspidatum Extract.Polygonum Cuspidatum Extract.Resveratrol.

last edit date:5th,May.2009.