Resveratrol-Grape Skin Extract

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Resveratrol-Grape Skin Extract
Posting date : Dec 05, 2008
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Resveratrol (trans-3,5,4'-trihydroxystilbene), belongs to a class of polyphenolic compounds called stilbenes , found largely in the skins of red grapes and root of Polygonum cuspidatum Sieb. et Zucc ( Japanese knotweed), is a component of Ko-jo-kon, an oriental medicine used to treat diseases of the blood vessels, heart and live.. Resveratrol is a fat-soluble compound that occurs in a trans and a cis configuration (see figure 1). Both cis- and trans-resveratrol also occur as glucosides (bound to a glucose molecule). Resveratrol-3-O-beta-glucoside is also called piceid. Function: Cardiovascular Effects Many studies suggest that consuming alcohol (especially red wine) may reduce the incidence of coronary heart disease (CHD). Several studies have demonstrated that resveratrol is an effective antioxidant. It inhibits lipid peroxidation of low-density lipoprotein (LDL), prevents the cytotoxicity of oxidized LDL, and protects cells against lipid peroxidation. It is thought that because it contains highly hydrophilic and lipophilic properties, it can provide more effective protection than other well-known antioxidants, such as vitamins C and E. On the other hand, it is less effective than the antioxidants quercetin and epicatechin found in red wine. Reduced platelet aggregation has also been demonstrated in studies on resveratrol, further contributing to its prevention of atherosclerosis. To date, most of the research on resveratrol's antioxidant and anti-platelet properties has been done in vitro (in an artificial environment using test-tube or tissue-culture preparations). Further studies in animals and humans are necessary to determine whether resveratrol supplementation makes sense. Cancer-Related Effects Resveratrol is being studied to see how it affects the initiation, promotion, and progression of cancer. With regard to tumor initiation, it has been shown to act as an antioxidant by inhibiting free radical formation, and as an anti-mutagen in rat models. Resveratrol appears to decrease tumor promotion activity by inhibiting cyclooxygenase-1 (COX-1), an enzyme that converts arachidonic acid to pro-inflammatory substances that stimulate tumor-cell growth . Studies related to progression have found that resveratrol induced human promyelocytic leukemia cell differentiation and inhibited ribonucleotide reductase, an enzyme needed for DNA synthesis in proliferating cells . One appealing characteristic of resveratrol's anti-cancer potential is its minimal toxicity to blood-forming cells . More studies using both cellular and animal models are needed before any such data would be applicable to human use. The similarity in structure between resveratrol and diethylstilbestrol (a synthetic estrogen) has prompted investigations into resveratrol's potential as a phytoestrogen (a plant compound that produces estrogen-like effects). However, these properties also stimulate the growth of human breast cancer cells . This finding seems contrary to its other anticancer activities, and is a cause for concern. The Natural Products Association was cited in an article regarding a new dietary supplement that contains resveratrol, a substance researchers believe may help protect human cells from diseases such as cancer and arthritis. Direct Antioxidant Activity In the test tube, resveratrol effectively scavenges (neutralizes) free radicals and other oxidants and inhibits low density lipoprotein (LDL) oxidation . However, there is little evidence that resveratrol is an important antioxidant in vivo . After oral consumption of resveratrol, circulating and intracellular levels of resveratrol in humans are likely to be much lower than that of other important antioxidants, such as vitamin C, vitamin E and glutathione. Moreover, the antioxidant activity of resveratrol metabolites, which comprise most of the circulating resveratrol, may be lower than that of resveratrol. Inhibition of Vascular Smooth Muscle Cell Proliferation The proliferation of vascular smooth muscle cells plays an important role in the progression of atherosclerosis . Resveratrol has been found to inhibit the proliferation of vascular smooth muscle cells in culture . Inhibition of Platelet Aggregation Platelet aggregation is one of the first steps in the formation of a blood clot that can occlude a coronary or cerebral artery, resulting in myocardial infarction or stroke. Resveratrol has been found to inhibit platelet aggregation in vitro. Safety & Adverse Effects Resveratrol is not known to be toxic or cause adverse effects in humans, but there have been few controlled clinical trials. In rats, daily oral administration of trans-resveratrol at doses up to 300 mg/kg of body weight for 4 weeks resulted in no apparent adverse effects . Pregnancy and Lactation The safety of resveratrol-containing supplements during pregnancy and lactation has not been established. Since no safe level of alcohol consumption has been established at any stage of pregnancy, pregnant women should avoid consuming wine as a source of resveratrol. Estrogen-sensitive Cancers Until more is known about the estrogenic activity of resveratrol in humans, women with a history of estrogen-sensitive cancers, such as breast, ovarian and uterine cancers, should avoid resveratrol supplements (see Estrogenic and Anti-estrogenic Activities above). Drug Interactions Anticoagulant and Antiplatelet Drugs Resveratrol has been found to inhibit human platelet aggregation in vitro (42, 84). Theoretically, high intakes of resveratrol (e.g., from supplements) could increase the risk of bleeding when taken with anticoagulant drugs, such as warfarin (Coumadin), and antiplatelet drugs, such as clopidogrel (Plavix), dipyridamole (Persantine), non-steroidal anti-inflamatory drugs (NSAIDs), aspirin and others.

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