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Resveratrol (trans-3,5,4'-trihydroxystilbene), a compound found largely in the skins of red grapes, is a component of Ko-jo-kon, an oriental medicine used to treat diseases of the blood vessels, heart and liver . It is a naturally occurring, powerful polyphenol (plant-derived) compound that has some significant antioxidant properties, which allow it to neutralize the gaggle of free radicals that intend to wreak havoc on critical cellular functions. It came to scientific attention during the mid-1990s as a possible explanation for the "French Paradox"—the low incidence of heart disease among the French people, who eat a relatively high-fat diet. Since then, it has been touted by manufacturers and examined by scientific researchers as an antioxidant, an anti-cancer agent, and a phytoestrogen. It has also been advertised on the Internet as "The French Paradox in a bottle." One company even markets a red-wine extract antioxidant product called "French Parad'ox." Most research on resveratrol has been done on animals, not in people. Research in mice given resveratrol suggests that the antioxidant might also help protect them from obesity and diabetes, both of which are strong risk factors for heart disease. However, those findings were reported only in mice. In addition, to get the same dose of resveratrol used in the mice studies, a person would have to drink over 60 liters of red wine every day. More research is needed before it's known whether resveratrol was the cause for the reduced risk. A study by John Hopkins University concludes that resveratrol levels may be a key player in protecting the brain during a stroke by elevating specific enzyme levels. Researchers believe resveratrol could extend the human life span, and protect people against a wide range of diseases such as cancer, type II diabetes, Alzheimer’s, and heart disease. The promise of resveratrol has been escalated with research suggesting that it has the capacity to activate a protein called SIRT1 found in mammals. SIRT1 is one of a larger class of proteins called sirtuins that have been shown to extend the life span of yeast, worms, flies and maybe, mice. Old yeast cells live longer when treated with resveratrol. The yeast cell is big and yellow. They've found a new study and published in online by March 7, in the journal Science. In that, they conclusively prove the interaction between resveratrol and SIRT1. Many studies suggest that consuming alcohol (especially red wine) may reduce the incidence of coronary heart disease (CHD). Several studies have demonstrated that resveratrol has antioxidant properties. It is claimed that because it contains highly hydrophilic and lipophilic properties, it may 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. Recent studies in laboratory mice have found increased survival and lower incidence of several diseases and conditions associated with aging, but the results are contradictory. Protective effects have been found in mice fed a high-fat or a low-calorie diet, but one study found that mice fed a standard diet beginning at age 12 months did not live longer. The study, published in the May issue of Cell Metabolism, tested the effects of resveratrol on mice. According to Dr. David Sinclair of Harvard Medical School, resveratrol works by acting on the SIRT1 gene, a gene that is believed to control the function and longevity of cells. Deleting the SIRT1 gene from mice causes developmental defects, but for the latest study, Sinclair and colleagues were able to produce mice without the SIRT1 gene that were healthy enough to be studied. The researchers found that the SIRT1 gene is necessary to enjoy any benefits from resveratrol, regardless of dose. They found that resveratrol, given at moderate doses, targets SIRT1 directly - and at higher doses, hits other targets (Image: http://themeathouseblog.files. wordpress.com).

DRUG DISCOVERY OF THE MONTH

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A perspective on NNRTI: Etravirine

Balasubramanian J, Narayanan N

Etravirine is a second-generation non-nucleoside opposite transcriptase chemical (NNRTI) with the key benefits of in vitro efficiency against many stresses of malware immune to efavirenz and nevirapine, as well as a greater inherited hurdle to level of resistance.

Drug Discovery, 2013, 4(10), 3-4

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FDA APPROVED DRUGS

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FDA approved drugs - February 2013

Brithvi V

Stivarga (regorafenib) is a small molecule inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, and maintenance of the tumor microenvironment.

Drug Discovery, 2013, 4(10), 5-6

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RESEARCH

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Antibacterial activity of certain medicinal plants against opportunistic pathogenic bacteria

Chauhan Divyesh, Bhatt Nikhil, Srinivas Murthy, Nayak Srutikant, Chauhan Paresh

study was conducted to check the efficacy of certain herbal medicinal plants against opportunistic pathogenic bacteria. Plant extracts of Allium sativum, Zingiber officinale, Curcuma longa, Syzigium aromaticum, Trigonella foenam graeaum were extracted out by solvent extraction method .

Drug Discovery, 2013, 4(10), 07-10

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DRUG DISCOVERY OF THE MONTH

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Novel Antimalarial analogue: Quinolone-3-Diarylethers

Brithvi V

The objective for creating new antimalarial medication is to discover a compound that can focus on several levels of the parasite’s life-cycle, thus affecting avoidance, therapy, and transmitting of the illness.

Drug Discovery, 2013, 4(11), 13

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FDA APPROVED DRUGS

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FDA approved drugs - March 2013

Brithvi V

Osphena (ospemifene) is an estrogen agonist/antagonist with tissue selective effects. It binds to estrogen receptors, resulting in the activation of estrogenic pathways in some tissues and the blockade of estrogenic pathways in other tissues.

Drug Discovery, 2013, 4(11), 14

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RESEARCH

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Carbon tetrachloride induced renaltoxicity and the effect of aqueous extract of Gongronema latifolium in Wistar albino rats

Onuoha SC, Chinaka NC

Gongronema latifolium is an important and highly medicinal plant commonly called utazi in Nigeria. It is commonly used as spice, ad vegetable and traditional folk medicine. The kidney by the way is an essential organ and part of the urinary system and serves as natural filter of blood and removal of wastes, among other functions.

Drug Discovery, 2013, 4(11), 15-16

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DRUG DISCOVERY OF THE MONTH

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A novel lead in design for the treatment of major depression: Vortioxetine

Brithvi V

Vortioxetine is an experimental drug currently under development by Lundbeck and Takeda for the treatment of major depressive disorder (MDD) and generalized anxiety disorder (GAD). The most common side effects reported with vortioxetine are nausea, vomiting, diarrhea, headache, and dizziness.

Drug Discovery, 2013, 4(12), 19

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FDA APPROVED DRUGS

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FDA approved drugs - April 2013

Brithvi V

Sitavig (acyclovir) is an antiviral buccal tablet formulated on the company's proprietary Lauriad muco-adhesive technology. It is specifically indicated for the treatment of recurrent herpes labialis in immunocompetent adults. It is supplied as a tablet for oral administration.

Drug Discovery, 2013, 4(12), 20-21

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