Resveratrol: History and Efficacy

The cardio-protective use of resveratrol can be traced back 2,000 years to the cardiac-stimulating mixture "Darakchasava" used in Indian Ayurvedic medicine. Darakchasava, a cardiotonic herbal remedy native to India, contains resveratrol as its major constituent.

Resveratrol is a naturally occurring phytoalexin produced by some plants as a defense against infection by pathogenic microorganisms. Chemically, resveratrol is a stilbene-based compound found in the trans and cis forms. The trans form gets converted to the cis form upon exposure to light and ultra-violet radiation.

In 1940, the pure form of resveratrol was identified in the roots of a Japanese plant called Ko-jo-kon. Recent familiarity with resveratrol, however, stems from its presence in nature as a component of the plant species Vitis vinifera L., more widely known as the common grapevine. As the highest concentration of grapevine resveratrol is located in the grape skin, red wines have a resveratrol concentration ranging anywhere from 0.2 mg/l to 7.0 mg/l, depending upon the wine.

In addition to its cardio-protective effects, resveratrol has been reported to be effective as an anti-viral and anti-bacterial agent. The cancer chemopreventive property of resveratrol was identified in 1997 when a collaboration of research groups reported (Jang et al. Science 275: 218-220, 1997) that resveratrol inhibited the development of carcinogen-induced precancerous lesions in mammary glands and suppressed skin carcinogenesis. It was later reported that resveratrol inhibited carcinogen-induced rat mammary carcinogenesis. Since then, more than 1,000 papers have been published reporting the chemopreventive effects of resveratrol, its molecular mechanisms of action, metabolism and toxicity, as well as the efficacy of resveratrol-derived compounds.

For nearly 4 years, scientists in IITRI's Carcinogenesis and Chemoprevention Division have been evaluating the effects of resveratrol in chemically induced mouse colon and lung carcinogenesis models. The mechanism of action of resveratrol in these targets is studied by using human colon cancer and lung cancer cells. The group has recently identified a new signaling cascade for resveratrol's action in lung cancer cells. Using azoxymethane to induce carcinogenesis, the focus for colon cancer at IITRI is on prevention of aberrant crypt foci, which often develop into colon cancers in both animal and human models.

Overall, resveratrol has become one of the molecules of choice for anti-cancer studies. Besides its chemopreventive effects, its ability to suppress proliferation of human cancer cells suggests that resveratrol may have anti-cancer properties. Reports have shown resveratrol is effective against melanoma and ovarian carcinoma, as well as cancers of the breast, prostate, colon, stomach, pancreas, thyroid, head and neck.