Summary: Red wine extract is an alcohol-free solid powder, rich in polyphenol antioxidants, including oligomeric proanthocyanidins (OPC), anthocyanins, quercetin, myricetin, resveratrol, etc. Red wine extract is one of the OPC 3 ingredients in FrenchGlory® isotonic OPC 3 antioxidants. Natural “French Paradox” is about French red wine extract polyphenols, which contribute to the French heart health & longevity and fight nutritional deficiency due to imbalanced diet. We use ExGrape ® TOTAL PE, a red wine grape extract made in GRAP'SUD, - a native French company specialized in the manufacture of grape by-products including red wine extract polyphenols from red wine grapes since 1969.
Red wine for OPC red wine extract
Wine as an alcoholic beverage containing rich antioxidants, has a history dated back to around 6,000 BC, originated in the Middle East. Wine appeared in Europe at about 4,500 BC in what is now Bulgaria, and Greece. Several ancient Greek philosophers had the interest in praising wine for wonderful health benefits. Wine appeared to be very common in ancient Greece, Thrace and Rome. Wine was also used by early Minoan and Etruscan civilizations. Roman army introduced the rootstocks and winemaking throughout Europe as Roman Empire was expanded. After the Bible was written about 2,000 years ago, Christian churches started to use wine for sacramental purpose, which further stimulated or maintained the wine industry after the fall of the Roman Empire.
Wine can be made from many plants including fruits and rice, etc. Grape wine is made by fermentation of crushed grapes (or grape juice) using various types of yeast. Grapes are rich in natural nutritional chemicals, and the fermentation is conducted without addition of sugars, acids, enzymes or other nutrients. Yeast converts the grape sugars into alcohol. Different varieties of grapes and strains of yeasts are used depending on the type of wine to be produced. Red and white wines are both made from grapes. They have similarities and differences. The differences are less known among the general population.
Red wine is made from red grapes and other dark-colored grapes, which have red coloring pigments such as anthocyanins of a variety of health benefits. In the preparation of red wine, whole grapes are mashed for fermentation without removal of skins and seeds. Among the most notable substances are natural chemicals called oligomeric proanthocyanidins (OPC), their monomers, gallate esters, anthocyanins, and resveratrol. Consequently, red wine contains rich natural phytochemicals including OPC, contributed from 3 parts of grape: skin, seed and the middle section between seed and skin. Red wine exhibits super antioxidant activity.
White wine can be made from either white grapes or red grapes. In either case, the grape seeds are removed before fermentation. Skins and pulp have also to be removed if red grapes are used in making white wine. Consequently, white wine contains fewer beneficial natural products and less concentrated OPC than red wine, and is free of anthocyanins and resveratrol. White wine has much lower antioxidant activity than red wine.
Traditionally, the nutritional benefits of wine as antioxidant recognized in many cultures are limited to people who enjoy alcohol. Many people, who do not like the alcoholic taste of this wonderful gift of red wine from nature, are left out from the nutritional benefits of the antioxidants in it. On the other hand, although occasional red wine consumption benefits the human body due to OPCs and other polyphenols such as anthocyanins, resveratrol, too much alcohol causes damages to the human body. Drinking red wine limits health benefits that human can get from OPCs, anthocyanins, resveratrol, and other polyphenol antioxidants.
From OPC grape seed extract to OPC red wine extract
The grape seed extract contains richer OPCs than any other plants and parts. This OPC discovery by a famous French OPC Professor Masquelier in 1970 stimulated the interests of European scientists to dig deeply into all parts of grapes for the nutritional treasures using modern scientific approaches. One of the approached used for the OPC biological studies 3 decades ago was to cultivate the grape plant in the C-14 isotope labeled carbon dioxide (CO2) microphytotron. This cultivation allowed the C-14 labeled OPC extract, which was used in the investigation of the OPC’s bioavailability and metabolism pathways.
About 20 years later, after the discovery of the grape seed extract OPCs, an epidemiological theory of “French paradox” emerged, which hypothesizes that regular consumption of red wines prevents occurrence of a higher disease rate (cardiovascular diseases, diabetes) in French citizens on high-fat diets, as red wines contain rich proanthocyanidins (OPC), anthocyanins, resveratrol, and other polyphenols and flavonoids. This hypothesis of French Paradox was broadcast in 1991 by CBS’s 60 minutes, while the term “French Paradox” was coined in 1992 by Dr Serge Renaud from Bordeaux University in France. This pattern of relatively high-fat diet, wine consumption, and the low incidence of heart disease and obesity among the French, stimulated the public interests in red wine extract of the nutritional components including OPC, resveratrol, and other polyphenols. The goal was to make alcohol-free red wine extract so that every adult can take the advantage of the rich nutrient OPCs present in red wine, without having to consume an alcohol beverage. Indeed the red wine extract, made from red wine, has been studied using the modern biological technologies and has been demonstrated many health benefits based on cellular, animal, and human clinical studies.
Components in OPC red wine extract
Oligomeric proanthocyanidins (OPC), including dimeric, trimeric, tetrameric and pentameric procyanidins are the major, but not the only components in a red wine extract. There are a plenty of catechin derivatives, flavanols, flavonoids such as anthocyanins, quercetin, resveratrol and apigenin that provide high antioxidant and free radical scarvenging benefits. A variety of proteins (leucine, arginine, cystine, phenylalanine, valine), tannins, lipids (palmitic, stearic, oleic, linoleic acids), sitosterol, phosphatidylserine, lecithin and vitamins C, A and E are found in OPC red wine extract.
Characteristics of red wine extract OPC
Red wine extract is relatively economical, and less technologically demanding than grape seed extract and pine bark extract. The compositions in red wine extract distinguish red wine extract from other OPC extracts such as grape seed extract and pine bark extract. Red wine extract contains less concentrated OPC and more diverse antioxidant natural products. There are many red wine extracts in the market that only contain 30-50% total polyphenols and 5-15% OPCs. Many red wine extract manufacturers do not give the information of OPC content at all in their papers of ingredient specifications. The higher grade red wine extracts contain 90-95% polyphenols, including OPC in 15-30%. The overall antioxidant activity of red wine extract is close to that of grape seed OPC extract or pine bark OPC extract.
1. Anthocyanins - flavonoids
One class of the unique natural products abundant in the red wine extract, but not in grape seed extract and pine bark extract is anthocyanins, which are completely water-soluble vacuolar pigments. Anthocyanins are not a part of OPC but polyphenols or bio-flavonoids, and may make about 3-10% of a red wine extract. Anthocyanins are especially rich in bilberry extract.
Anthocyanins may give different colors - red, purple, or blue according to pH. They are odorless and nearly flavorless, even though they taste slightly astringent. The core chemical structure in anthocyanin is anthocyanidin, based on the flavylium ion or 2-phenylchromenylium (chromenylium is referred also to as benzopyrylium). Anthocyanidins and anthocyanins are actually salt derivatives of such as 2-phenylchromenylium cation, or flavylium cation. The counterion of the flavylium cation is mostly chloride. Due to this positive charge, anthocyanins change the color in different pH conditions, differing from flavanol OPCs.
2. Resveratrol
The other well-known compound in red wine extract is resveratrol, a strong antioxidant polyphenol. Resveratrol (trans-resveratrol) is a phytoalexin natural product, produced as a defense chemical against pathogens such as bacteria or fungi by several plants. It is a polyphenol antioxidant, and not an OPC molecule. Resveratrol antioxidant is rich in Japanese knotweed (or Chinese polygonum cuspidatum, or Huzhang). Huzhang is a native plant in China, and has been used as a famous Chinese herbal medicine for more than 2,000 years. A low concentration of resveratrol in grape skins is also present in red wine and red wine extract, and may contribute to a tiny part of “French Paradox” in our opinion. OPCs are several orders more abundant than resveratrol in a red wine extract. Resveratrol is also reportedly detected in the grape seed extract and pine bark extract in even lower concentrations.
Controversies of resveratrol
Emergence of “French Paradox” theory in the early 1990s stimulated the search for other single molecules (other than OPCs) in the red wine extract and could bring miracles to human heart health and longevity. OPCs contain many antioxidant molecules instead of a single one, and the health benefits of OPCs had been known well. Anyway, scientists have the spirit to explore new things. Resveratrol was the one attracting the attention of some scientists since the early 1990s. In 2003, David Sinclair and his team from Harvard published in Nature that resveratrol increased the survival of yeast cells. The following published studies of resveratrol in nematode worms, fruit flies, fish, and mice have linked resveratrol to longer lives with super antioxidant activity. Resveratrol has been demonstrated anti-cancer and anti-inflammatory activities by cellular and animal model studies. Resveratrol appears to offer considerable health benefits. Resveratrol was said to be “one of the most promising molecules on the planet”.
Despite resveratrol's "anti-aging effects" have been touted extensively in the media, many scientists published controversial articles and questioned the reliabilities of some published heath benefit claims of resveratrol. The controversies include the effects of resveratrol on the lifespan of many model organisms, with uncertain effects in fruit flies, nematode worms, and short-lived fishes.
Blood-sugar-lowering and other beneficial cardiovascular effects of resveratrol have been reported with animal model studies, while OPC has been demonstrated almost exactly the same benefits. A positive human clinical trial indicates that resveratrol in extremely high doses (3–5 g) is required to significantly lower blood sugar. In contrast to these giant dosages, as many are suspicious, so low content of resveratrol in red wine or red wine extract can really contribute to French Paradox theory at all. The rich polyphenol components including OPCs, on the other hands, are well recognized nutritional components in red wine extracts without controversy.
One glass of wine may contain up to 3 micrograms of resveratrol. “Even if you take resveratrol with doses of 30 to 150 mg this is still not enough to achieve the quantities that produced the wonderful effects in test animals,” as claimed by a renowned scientist.
The resveratrol concentration in the red wine extract is usually about 1% or far less, even from the best French red or purple grapes, at about a 100th of the OPC content. There are 3 cheap ways to make a larger quantity of resveratrol in red wine extract. Unlike OPC and other polyphenols such as anthocyanins, resveratrol is a single chemical compound that can be easily synthesized in a chemical lab. The chemical synthesized resveratrol is widely sold in the market. Other 2 cheap ways to add a large quantity of resveratrol are from Chinese polygonum cuspidatum and Japanese knotweed extracts.
Based on some of these considerations, our Ph.D. scientists specialized in OPC natural product chemistry and medicinal chemistry wish to emphasize the nutritional values of OPCs and related polyphenols in red wine extract as natural nutritional supplements. “French Paradox” really means the red wine extract as a whole system with the predominance of OPCs. Resveratrol is of nutritional values as an antioxidant. Its natural concentration in red wine extract can serve for this purpose as a cocktail with other polyphenols including OPCs. A red wine extract of diverse OPCs and other polyphenols has the better nutritional benefits than a single compound resveratrol alone.
There are compiling studies indicating that several components in the red wine extract other than resveratrol have stronger biological activities and are more beneficial to human health than resveratrol. In addition to OPC, one of other polyphenols has just published in Mol Nutr Food Res. (2010 May 3) with a title: “The red wine extract-induced activation of endothelial nitric oxide synthase is mediated by a great variety of polyphenolic compounds.” Another example is a paper in Ann N Y Acad Sci. (August 2009; 1171: 170-5) with a title: “Protective effects of red wine flavonols on 4-hydroxynonenal-induced apoptosis in PC12 cells.”
Resveratrol, when used as a single molecule, has several issues of stability, solubility, and bioavailability, which may limit its use in foods and supplements. The data for bioavailability of resveratrol in human body essentially do not exist as the end of 2009. While OPC has been well demonstrated to be safe, the safety is even the more concern when resveratrol is used in large quantities (30-100 mg doses) as a single compound in human bodies. High doses of resveratrol could be harmful for a long term use. Resveratrol is a chelator of copper - a mineral used by our red blood cells and collagen. As reported by NUTRA INGREDIENTS, USA on May 6, 2010, “a phase 2 human trial investigating the effectiveness of resveratrol for treating multiple myeloma patients has been suspended after 20 percent of the trial’s subjects developed kidney damage.” There are un-clarified risks to take resveratrol in large quantities as dietary supplement.
A good and safe use of resveratrol is probably as a potential topical agent, in combination with OPC grape seed extract, for skin cancer. A recent study using SENCAR mice skin cancer model indicates that resveratrol is effective as a topical agent, and even more effective when combined with grape seed extract OPC against skin cancer [Cancer Prevention Research (Philadelphia, Pa.). Feb 2010, 3(2):170-8]. But this published study is very preliminary, and resveratrol and red wine extract have neither been approved for treatment of skin cancer according to FDA regulations on dietary supplements.
Eastern Cultures and FrenchGlory isotonic OPCs
“One may not have a good thing too much,” according to a general philosophy of the Easter traditional herbal medicine such as in China, India and Japan. Balance and harmony from a variety of different natural products are the better choice for the purpose of dietary supplement. A single substance like resveratrol, acting along in large doses, would cause damage one way or the other in the long run, as predicted in the Eastern cultures. This is not about resveratrol, but a general philosophy. French red wine extract of OPCs and a variety of other polyphenols from the Western modern nutritional science meets this balance and harmony requirement of ancient wisdoms from the Eastern cultures. On the other hand, many other people believe that resveratrol natural concentration in the red wine extract could have very significant anti-aging effect, as resveratrol works coordinately with OPCs, other polyphenols and a list of rich antioxidants in the red wine extract. This coordinated team work of antioxidants involving resveratrol, OPCs and other polyphenols contributes to “French Paradox” theory. Without resveratrol, a red wine extract would not be a red wine extract any more. The added resveratrol or resveratrol taken alone in large doses could harm human bodies in the long run, regardless of its nutritional benefits. The Eastern philosophy of herbal medicine advice: try to avoid a single chemical such as resveratrol for general health maintenance unless it is necessary as the only choice for special medical conditions.
FrenchGlory ® isotonic OPC, -3 antioxidant products contain a red wine grape extract of natural resveratrol concentration, as well as OPCs from grape seed extract and pine bark extract. The diverse sources of a variety of polyphenols include bilberry extract and citrus extract bio-flavonoids.
and Treat Your Body with the World-best ® Antioxidants!
It Is Your Body! It Is Your Choice!
Easy ways to produce red wine extract containing OPCs
The goal to make red wine extract is to preserve the nutritional OPC antioxidants, resveratrol, anthocyanins and other bioactive polyphenols, and to remove alcohol and sugars. Red wine extract can be more easily made for this purpose, compared to grape seed extraction and pine bark extraction. Red wine mainly contains small polyphenol molecules such as small OPCs, catechin derivatives, catechin, resveratrol, and other flavonoids (quercetin, apigenin), etc. A red wine extract from fermented whole grapes contains very little amount of polymeric proanthocyanidins. Polymeric proanthocyanidins, often present in grape seed extract and pine bark extract, make the OPC extraction from grape seeds and pine bark more challenging.
Red wine polyphenols including OPCs, anthocyanins, resveratrol, etc. can be directly extracted from red wine grapes without going through the fermentation process. Such a thought was tested by many companies in order to lower the costs, and make the OPC ingredient of the same nutritional values. The purpose of fermentation is just to convert grape sugars to ethanol, while OPC nutrients are supposedly preserved. If this fermentation is skipped, OPCs and related polyphenols can be extracted by removing grape sugars instead of ethanol.
The OPC red wine extract obtained this way without fermentation was investigated in many different ways from strict OPC characterization in analytical chemistry laboratories to OPC bio-activity evaluations using modern biological technologies. The OPC chemical analyses indicate that the red wine grape extract without the fermentation has higher OPC concentration than the red wine extract from the fermented grapes. It is further found that the red wine extract from the fermented grapes contains more of the monomers - catechin and epicatechin. It is likely that OPC oligomers degrade in some degree during the fermentation. As OPC oligomers have been shown to be more beneficial to human health than monomers - catechin and epicatechin, a red wine grape extract without fermentation is expected to be more potent nutritional ingredient due to its higher content OPCs.
These findings stimulate the biological tests for the red wine grape extracts without fermentation. For example, a proprietary red wine grape extract (ExGrape TOTAL) was used in the studies with cholesterol-fed hamsters and to investigate possible operating mechanisms. This red wine grape extract (ExGrape TOTAL) and other 2 OPC grape seed extracts (GSE1, GSE2) fed hamsters at a moderate dose mimicking two glasses of red wine per meal reduced plasma cholesterol (−11% on average). The extracts prevented the development of aortic atherosclerosis by 68% (GSE1), 63% (ExGrape TOTAL), and 34% (GSE2). Elsewhere, in an ex vivo experiment using rat aortic rings, GSE1 (7 μg/mL) induced 77% endothelium-dependent relaxation, whereas ExGrape TOTAL and GSE2 (30 μg/mL) induced 84 and 72%, respectively. These results suggest that phenolic extracts from grape seeds and marc are beneficial in inhibiting atherosclerosis by indirect mechanism(s).
ExGrape ® TOTAL is an OPC ingredient extracted from grape marc in a ratio of 500:1. As comparison, Vitaflavan ® OPC is extracted from grape seeds in a ratio of 150:1, and Oligopin ® OPC from pine bark in a ratio of 1000:1.
Red wine extract is neither resveratrol nor grape seed extract
We wish to emphasize that red wine extract is NOT grape seed extract, although both have the similarity of rich OPCs and other polyphenol antioxidants. Several OPC consumer products on the market labeled as red wine extract do not actually contain a red wine extract or red wine polyphenols, but only the OPC grape seed extract and some added resveratrol, while resveratrol could be made by chemical synthesis, or from an extract of Chinese polygonum cuspidatum.
Red wine extract does not mean resveratrol either. Many sellers call their resveratrol, wherever it is from, as red wine extract. It is very confusing and misleading. “French Paradox” really means red wine extract OPC and other polyphenols as a whole system of balanced antioxidants. “French Paradox” originated from complex polyphenol antioxidants of natural concentrations. The basis of “French Paradox” is balanced, harmonic, and coordinated effects of many antioxidant natural products. We wish to use the term “OPC red wine extract” to distinguish from any other red wine extract with added resveratrol from chemical synthesis or from polygonum cuspidatum resveratrol.
Health benefits of OPC red wine extract †
The heart health benefits of OPC red wine extract were well recognized by epidemiological studies of red wine consumption in France, leading to the French Paradox theory in the early 1990s. A long-term ongoing intake of alcohol-free red wine extract may prevent nutrition-deficient health problems, leading to longevity. Antioxidant deficiency is among the major nutritional deficiencies caused by imbalanced diet. Extensive scientific investigations have been conduted on both the whole red wine extract and individual polyphenol components. The antioxidant activity of polyphenols (mainly OPCs) in the red wine extract occupies the center stage of the interests. OPC red wine extract polyphenols as antioxidants in vitro and in vivo studies indicate the nitritional benefits for oxidative stress related diseases - cardiovascular diseases, cancer, or chronic inflammatory processes.† It should be emphasized that red wine extract is under investigations as a possible drug in treating a variety of diseases. But its current commercial use is limited to as dietary supplement, not intended to treat, prevent, cure, or diagnose any diseases.
Red wine extract polyphenols including OPCs have been demonstragted the ability of helping reduce platelet aggregation and clotting in the blood, therefore, can help reduce the risk of arteriosclerosis, stroke and heart attacks. Studies show that the levels of high-density lipoproteins (HDLs - good cholesterol) in the blood were increased, while the low-density lipoproteins (LDLs, - bad cholesterol) were decreased by regular consumption of red wine extract polyphenols. This means better blood circulation in the body, from and to the heart. Anthocyanins, quercetin, myricetin, resveratrol, etc. as the minor components, and OPCs as the major antioxidants may both assist in increasing nitric oxide levels, which helps relax artery walls, thus also help maintain good blood flow and improved circulation.†
Despite resveratrol is a very minor component in red wine extract, resveratrol may contribute to the nutritional benefit for Alzheimer's disease. A study from UCLA and Mt. Sinai Schools of Medicine indicates that red wine extract polyphenols containing resveratrol can be protective in cases of Alzheimer's disease in animal models by preventing the buildup of beta amyloid, the feature of Alzheimer disease. The red wine polyphenol extract containing resveratrol blocked precursor proteins from aggregating to form the toxic beta amyloid protein. Red wine extract may significantly improve blood circulation for better cardiac and cerebral function. Red wine extract OPCs are able to cross the blood-brain barrier, and OPCs are, therefore, expected to protect the brain and spinal nerves against free radical damage. OPCs and other polyphenol antioxidants in red wine extracts help as a dietary supplement for Alzheimer's disease and dementia.†
Red wine extract OPCs were demonstrated to improve peripheral blood circulation and to relieve pain and swelling in arms, ankles and legs. Other nutritional uses of red wine extract may be extended for varicose veins, numbness, and tingling. OPCs in red wine extract show the strengthening effects on collagen and elastin, and may be useful supplement for edema and swelling.†
Red wine extract OPCs can potentially help tissue regeneration, strengthen and repair connective tissues, stimulate collagen production, slow down and revitalize aging skin and enhance tissue elasticity. These anti-aging effects of OPCs have been widely recognized due to OPCs’ ability to deactivate harmful free radicals in human bodies. OPC red wine extract has the major function of cytoprotection, enhancing the development of normal cells as a free radical scavenger. Other than the ability to combat free radicals, red wine extract OPC and related polyphenols may even stimulate cell renewal by interfering with mucosal proteins. Further, red wine extract OPCs can inhibit abnormal cell growth, and were found to stimulate apoptosis of leukemia cells. In fact, there have been many other studies indicating that red wine extract OPCs have the inhibitory effects on cancer cells of skin, breast, bowel, lung, stomach and prostate, in test tubes or by animal models.†
OPC red wine extract has been demonstrated the role of regulating human immune system by suppressing histamine production, and adjusting allergic and inflammatory responses. Therefore, OPC red wine extract as a dietary supplement may help allergy sufferers. But its use as a drug has not been validated in treating/preventing inflammatory diseases.
Red wine extract OPCs as an antioxidant supplement are studied to help relieve the side effect of acetaminophen (a non prescription pain killer) and protect liver from its toxicity. OPCs are found to protect liver from toxicity damages in general in several studies. Other protective effects of red wine extract OPCs under investigations include those against osteoarthritis, pancreatitis, diabetic kidney disease and risk of stroke. †
Possible contraindications
There are no reports of side effects for taking red wine extracts. No drug interaction has been established or reported. But do not take an OPC supplement of red wine extract, grape seed extract or pine bark extract if you take blood-thinning medication such as aspirin, Coumadin, etc. unless advised by a health care professional. Do not take an OPC supplement if you have anemia or take iron supplement. Do not take OPCs together with a mineral supplement, and take them at two separate times of at least 2 -3 hours apart in the day.
Generally, other adults, healthy or sick, may take OPC red wine extract as a dietary supplement. Always consult your health care professional for any questions related to your medical conditions.
Preparation of red wine extract antioxidants
Most consumer products labeled as “red wine extract” contain added resveratrol, which is from two possible sources - chemical synthesis or an extract of Chinese polygonum cuspidatum. Some consumer products labeled as “red wine extract resveratrol” are very misleading for OPC consumers. A large quantity of the added resveratrol can no way be made from red wine or red wine extract.
OPC red wine extract is one of the 3 OPC ingredients in our FrenchGlory ® isotonic OPC antioxidants. In the other words, a red wine extract containing resveratrol of natural concentration is made as isotonic drink with a very yummy taste for high and efficient absorption. Our 3 isotonic OPC products use the highest quality ingredients of French red wine extract, French grape seed extract, and French pine bark extract to provide diverse OPC antioxidants of natural concentration.
ExGrape ® TOTAL, a commercial ingredient of our red wine grape extract polyphenols contain high and natural contents of OPCs, anthocyanins, and resveratrol. The natural resveratrol content is standardized and the typical resveratrol concentration is 300-350 ppm in the red wine extract powder (300-350 mg / kg). This red wine extract ingredient is certified in a native French manufacture with renowned credibility.
“Natural” French Paradox is our choice. It is your body! It is your choice!
and Treat Your Body with the World-best ® Antioxidants!
† These statements have not been evaluated by the US Food & Drug Administration.
FrenchGlory ® isotonic OPC antioxidants are nutritional supplements, not intended to diagnose, treat, care or prevent any diseases.
Reference outlines on OPC red wine extract
This is a section of information on OPC research related to red wine extract and red wine grape extract. The published research articles are critically summarized by our OPC experts - 3 PhD scientists in natural product and medicinal chemistry. All the writings are original and are based on our critical reading and understanding of the original scientific papers. All copyrights are reserved.
WARNING: The published scientific studies are very preliminary and red wine extract has not been approved for treating, curing or preventing any diseases, according to the US FDA regulations on drug and dietary supplement. Red wine extract is officially recognized to be safe and has a variety of nutritional benefits for nutritional deficiency-related health problems.
1. Cytotoxic Effect of Wine Polyphenolic Extracts and Resveratrol Against Human Carcinoma Cells and Normal Peripheral Blood Mononuclear Cells. J Med Food. May 18, 2010.
An OPC red wine extract was among the 3 materials, including white wine extract and resveratrol, was investigated for the cytotoxic activities against different cancer cell lines, including human cervix adenocarcinoma HeLa, human breast adenocarcinoma MDA-MB-361, human breast carcinoma MDA-MB-453 and normal human peripheral blood mononuclear cells (PBMCs). The OPC red wine extract, white wine extract polyphenol and resveratrol exhibited higher cytotoxic activities against HeLa and MDA-MB-453 cells than their activities against MDA-MB-361 cells and unstimulated and stimulated PBMCs. Surprisingly, white wine polyphenol extract was found to have significantly stronger antiproliferative activity on cancer cell lines than red wine extract. The morphological signs of apoptosis was indicated by condensed or fragmented nuclei in HeLa cells, pretreated with white wine extract polyphenols and stained with a mixture of acridine orange and ethidium bromide. The late stages of apoptosis or secondary necrosis of HeLa cells were observed. These results support that OPC and polyphenolic extracts from red and white wine may have nutritional benefits of anticarcinogenic potential.
2. The red wine extract-induced activation of endothelial nitric oxide synthase is mediated by a great variety of polyphenolic compounds. Mol Nutr Food Res. 2010 May 3.
In this study, red wine extract polyphenol OPC was found to induce nitric oxide (NO)-mediated vasoprotective effects, mainly by causing the PI3-kinase/Akt-dependent activation of endothelial NO synthase (eNOS). The red wine extract polyphenols contain several hundreds of phenolic antioxidants including proanthocyanidins (OPC). In order to identify polyphenol compounds as antioxidants in red wine extract capable of activating eNOS in endothelial cells, multi-step fractionation was conducted. The red wine extract OPC and polyphenols were fractionated using Sephadex LH-20 and preparative reverse phase HPLC. The phosphorylation levels of Akt and eNOS caused by different polyphenol fractions were assessed by Western blot analysis, and NO formation was determined by electron spin resonance spectroscopy. MALDI-TOF and HPLC-MS techniques were used for the identity assignments of phenolic compounds in fractions. The 9 fractions (Fractions A to I) of red wine extract were obtained from Sephadex LH-20. Significant eNOS activations were observed from fractions F, G, H and I. The further analyses using semi-preparative RP-HPLC techniques indicated that the active fractions and subfractions contained mainly OPCs and anthocyanins.
3. Red wine extract polyphenols cause growth inhibition and apoptosis in acute lymphoblastic leukaemia cells by inducing a redox-sensitive up-regulation of p73 and down-regulation of UHRF1. European Journal of Cancer. Mar 2010; 46(5): 983-94.
Red wine extract contains rich polyphenol antioxidants including proanthocyanidins (OPCs). In this study, red wine extract OPCs and other polyphenols (2.9g/L) were investigated for the effect on the proliferation of human lymphoblastic leukaemia cells (Jurkat cells). Red wine extract OPCs and other polyphenols suppressed the proliferation of Jurkat cells and caused G0/G1 cell cycle to arrest, depending on the concentration of OPC red wine extract. OPC red wine extract increased levels of the pro-apoptotic protein p73 and the active caspase-3 by increasing their expression. Consequently, the OPC red wine extract led to apoptosis of the leukaemia cells, as confirmed by DNA fragmentation analysis. The OPC red wine extract also down-regulated the antiapoptotic protein UHRF1. The formation of reactive oxygen species (ROS) was largely increased, as stimulated by red wine extract OPCs and other polyphenols. Formation of ROS and apoptosis induced by the red wine extract polyphenols including OPC were prevented by the 3 intracellular scavengers of superoxide anions (MnTMPyP, MnTBAP, PEG-SOD), but not by native extracellular superoxide dismutase (SOD). MnTMPyP also offset the effects of OPC red wine extract and related polyphenols on the expression levels of p73, active caspase-3 and UHRF1. Therefore, red wine extract OPCs and other polyphenols can induce the intracellular formation of superoxide anions, up-regulation of p73 and down-regulation of UHRF1 in Jurkat cells. This redox-sensitive mechanism accounts for the consequent apoptosis of Jurkat cells induced by the OPC red wine extract.
4. In vitro hemorheological effects of red wine and alcohol-free red wine extract. Clin Hemorheol Microcirc. 2010; 44(3): 227-36.
Red wine and OPC red wine extract were evaluated for their abilities to induce changes of 3 hemorheological factors, which impact the pathophysiology of the French paradox related to the cardiovascular health benefits. OPC-containing red wine was mixed with blood samples of healthy volunteers in 3 different alcohol concentrations of 0.1%, 0.3 % and 1% respectively. The OPC red wine extract in the 3 equivalent amounts or physiological saline was also added to different blood samples for the investigation by comparison. These blood samples, pretreated with red wine, OPC red wine extract or saline, were then treated with the free radical generator phenazine methosulfate (PMS). PMS is known to cause impairment of deformability of erythrocytes in absence of an added antioxidant such as OPC red wine extract. The 3 bioassay parameters, erythrocyte aggregation (Myrenne and LORCA), deformability (LORCA) and platelet aggregation (Carat TX4) were measured. Red wine and OPC red wine extract at all the 3 different concentrations (0.1%, 0.3% and 1%) significantly inhibited erythrocyte aggregation using Myrenne aggregometer, as compared to the saline control samples. LORCA aggregation index and threshold shear rate showed the significant inhibition by red wine and OPC red wine extract only at the highest concentration of 1%. Red wine and OPC red wine extract did not affect erythrocyte deformability significantly for all the 3 different concentrations. The OPC red wine extract at 3 per thousand concentration significantly prevented erythrocytes from PMS-induced impairment of deformability (p < 0.05). Platelet aggregation was significantly suppressed only by the highest concentration (1%) of OPC red wine extract (p < 0.05). This study supports that red wine and OPC red wine extract have significant impact on hemorheological parameters, and therefore, contribute to the phenomenon described by the “French Paradox” theory.
5. Estrogen receptor alpha as a key target of red wine extract polyphenols action on the endothelium. PLoS One. Jan 1, 2010; 5(1): e8554.
Diet rich in polyphenol antioxidants such as OPCs contributes to benefits for cardiovascular health and vascular protection. Molecular targets for OPCs’ and other polyphenols’ effects need to be investigated further. There is a structural similarity between estrogens and polyphenols including OPCs known as phytoestrogens, as they also have similar vascular effects. The alpha isoform of estrogen receptor (ERa) was investigated for possible involvement in the transduction of the vascular benefits of OPC and polyphenols. ERa deficient mice were used to investigate endothelium-dependent vasorelaxation induced either by OPC red wine extract, delphinidin (an anthocyanin), or ERa agonists (17-beta-estradiol) and PPT. The OPC red wine extract, delphinidin and the 2 ERa agonists activated nitric oxide (NO) pathway in endothelial cells in ERa Wild-Typ, leading to endothelial vasodilatation in aorta from ERa Wild-Type but not from Knock-Out mice. Binding assay and docking were conducted and indicated a direct interaction between delphinidin and ERa activator site. The decreased serotonin response and increased sensitivity of the endothelium-dependent relaxation to acetylcholine were observed by a short term feeding with OPC red wine extract. Concomitantly, the NO production was increased and the production of superoxide anions was decreased, by the OPC red wine extract. These events were completely blunted in ERa deficient mice. The endothelial benefits of red wine extract polyphenols and delphinidin involve a molecular mechanism of ERa activation. This study provides a new and valuable insight of the potential therapeutic use of OPC red win extract and other polyphenols such as anthocyanins against cardiovascular pathologies.
6. Protective effects of resveratrol and quercetin against MPP+ -induced oxidative stress act by modulating markers of apoptotic death in dopaminergic neurons. Cell Mol Neurobiol. Dec. 2009; 29(8): 1169-80.
OPC and related polyphenol antioxidants such as resveratrol and quercetin may protect dopamine neurons from apoptotic death by regulating reactive oxygen species produced by oxidative stress, benefiting patients of Parkinson's disease. 1-Methyl-4-phenylpyridinium ion (MPPI) is a Parkinsonian toxin and causes the selective degeneration of dopaminergic neurons. This study was to investigate the effects of resveratrol, isolated from an OPC red wine extract, and quercetin on the MPPI induced apoptotic cascade. The MPPI-induced apoptotic neuronal PC12 death was found significantly reduced by a pre-treatment for 3 h with resveratrol or quercetin before MPPI administration. mRNA levels and protein expression of Bax, a pro-apoptotic gene, and Bcl-2, an anti-apoptotic gene were down-regulated by resveratrol or quercetin. Overall, resveratrol and quercetin exhibited the activities in regulating the expression of pro- and anti-apoptotic genes, resulting in diminished apoptotic neuronal cell death. These and other related natural polyphenols such as OPC, resveratrol and quercetin have nutritional values for patients of neurodegenerative diseases caused by oxidative stress and apoptosis.
7. Protective effects of red wine flavonols on 4-hydroxynonenal-induced apoptosis in PC12 cells. Ann N Y Acad Sci. Aug 2009; 1171: 170-5.
“French Paradox” is a theory that a moderate consumption of red wine has health benefits, such as the inhibition of neurodegenerative diseases. Resveratrol is just a very minor component among many others in a red wine extract. The protective mechanisms for French Paradox and the active substances in red wine extract remain unclear. This study was to investigate whether and how OPC red wine extract and red wine flavonols quercetin and myricetin inhibited 4-hydroxynonenal (HNE)-induced apoptosis of rat pheochromocytoma PC12 cells. HNE-induced PC12 cell death was attenuated by the treatment with OPC red wine extract in a concentration-dependent manner. The OPC red wine extract exhibited 3 effects. 1) The OPC red wine extract prevented HNE-induced cleavage of poly(ADP-ribose) polymerase, a key enzyme involved in DNA repair in the nucleus. 2) The OPC red wine extract inhibited HNE-induced nuclear condensation in PC12 cells. 3) The OPC red wine extract protected against apoptosis of PC12 cells by attenuating intracellular reactive oxygen species, as indicated by data of 2',7'-dichlorofluorescin diacetate. The cytoprotective effects of OPC red wine extract were separately evaluated for 3 components in it: quercetin, myricetin and resveratrol. Quercetin and myricetin exhibited significantly stronger protective effects on HNE-induced cell death than resveratrol. Quercetin and myricetin decreased HNE-induced nuclear condensation more than resveratrol. Therefore, flavonols such as OPC, Quercetin and myricetin in the red wine extract are the major contributors to the neuroprotective potential other than resveratrol.
8. Activation of phosphatidylinositol 3-kinase is required for tumor necrosis factor-alpha-induced upregulation of matrix metalloproteinase-9: its direct inhibition by quercetin. Int J Biochem Cell Biol. Jul 2009; 41(7): 1592-600.
An OPC red wine extract was investigated among 3 materials in this study for possible inhibitory effects on tumor necrosis factor (TNF)-alpha-induced upregulation of matrix metalloproteinase-9 (MMP-9) and on the migratory phenotype of JB6 P+ mouse epidermal (JB6 P+) cells. It was found that the TNF-alpha-induced up-regulation of MMP-9 and cell migration were inhibited significantly by either OPC red wine extract or quercetin, but not by resveratrol. Western blotting and luciferase assays indicated that the OPC red wine extract and quercetin suppressed the phosphorylation of Akt and the transactivation of activator protein-1 and nuclear factor-kappaB. Akt was the only MAP-kinase affected by quercetin. The OPC red wine extract and quercetin inhibited phosphatidylinositol 3-kinase (PI3K) activity, as shown by direct kinase assay data. A direct binding between OPC red wine extract (or quercetin) and PI3K was indicated by direct and cell-based pull-down assays, while the PI3K-dependent Akt pathway was involved in TNF-alpha-induced MMP-9 upregulation and migration in JB6 P+ cells. In conclusion, the OPC red wine extract and quercetin inhibited TNF-alpha-induced MMP-9 up-regulation and the migratory phenotype by inhibiting and direct binding with the PI3K/Akt pathway. This study demonstrated that the potential nutritional benefits of the OPC red wine extract and quercetin for various skin disorders, including photoaging, dermatitis, and tumorigenesis, as TNF-alpha is a key proinflammatory cytokine that acts to provoke inflammation, proliferation, and tumorigenesis.
9. Red wine anthocyanins are rapidly absorbed in humans and affect monocyte chemoattractant protein 1 levels and antioxidant capacity of plasma. J Nutr Biochem. Jul 2009; 20(7): 521-9.
French Paradox as an epidemiological theory suggests that a moderate consumption of anthocyanins-containing red wine OPC and polyphenols may be associated with protection against coronary heart disease. Dietary anthocyanins contain a mixture of diverse molecules. A red wine OPC and several 3-monoglucosides (anthocyanins) were evaluated in this study for their absorption and metabolism in humans. The 3-monoglucosides include delphinidin, cyanidin, petunidin, peonidin and malvidin. The effects of an OPC red wine extract on plasma antioxidant level and on monocyte chemo-attractant protein 1 production in healthy human volunteers were also investigated. An anthocyanin extract of 12 g was supplied to 7 healthy volunteers by meal after a 12-h overnight fast. 13 Blood samples were collected within the 24 h following the supplementation meal. Urine was also collected within this 24-h period.
Both plasma and urine samples contain the intact form of anthocyanins. Several other anthocyanin metabolites were detected in plasma and urine, and 2 chemical structures of the metabolites were assigned as those for glucuronides of peonidin and malvidin.
Anthocyanins and their metabolites did not appear in plasma until about 30 min later after the supplementation meal, and their maximum levels were reached about 1.6 h later for glucosides and 2.5 h for glucuronides. The red wine extract anthocyanins caused an increase in the antioxidant capacity and a decrease in MCP-1 circulating levels in plasma. About 0.05% of the total supplemented anthocyanins were detected in the excreted urine within 24 h. About 94% of the total anthocyanin excretion took place within 6 h.
10. Red wine polyphenols prevent metabolic and cardiovascular alterations associated with obesity in Zucker fatty rats (Fa/Fa). PLoS One. 2009; 4(5): e5557.
“French Paradox” is an epidemiological theory that an inverse correlation between dietary polyphenol consumption and mortality from cardiovascular diseases. This study was an investigation that OPC red wine extract as a dietary supplement might exert beneficial effects on obesity-associated metabolic disorders and cardiovascular functions in Zucker fatty (ZF) rats. ZF rats or their lean littermates were fed with diet containing OPC red wine extract supplementation for 8 weeks, as compared with a control group that received only normal diet without OPC red wine extract supplementation. The OPC red wine extract improved glucose metabolism by lowering plasma glucose and fructosamine levels in ZF rats. The OPC red wine extract also exhibited the following 3 effects. 1) The OPC red wine extract reduced circulating triglycerides and total cholesterol as well as LDL-cholesterol in ZF rats. 2) The OPC red wine extract improved cardiac performance as evidenced by an increase in left ventricular fractional shortening and cardiac output associated with decreased peripheral arterial resistances in ZF rats, as shown by echocardiography measurements. 3) The OPC red wine extract corrected endothelial dysfunction in aortas from ZF rats by improving endothelium-dependent relaxation in response to acetylcholine (Ach). Further, the OPC red wine extract enhanced endothelial NO-synthase (eNOS) activity and reduced superoxide anion release via decreased expression of NADPH oxidase membrane sub-unit, Nox-1. Consequently, bioavailability of NO resulting from increased nitric oxide (NO) production was enhanced by the OPC red wine extract. It was concluded that the red wine extract OPC and other associated polyphenols might have the nutritional benefits for prevention of cardiovascular and metabolic alterations associated with obesity.
11. Grape seed and red wine polyphenol extracts inhibit cellular cholesterol uptake, cell proliferation, and 5-lipoxygenase activity. Nutr Res. Dec. 2008; 28(12): 842-50.
Polyphenol OPC grape seed and red wine extracts possess a variety of biological activities and are used as dietary supplements for inflammatory-mediated disease such as cardiovascular disease and cancer. The OPC extracts were investigated in this study for 3 possible activities: 1) inhibition of cholesterol uptake; 2) inhibition of cell proliferation; 3) inhibition of 5-lipoxygenase (5-LOX), a target of the inflammatory process. An OPC extract of these 3 activities would contribute to the reported pleiotropic effects for several OPC extracts such as OPC grape seed extract or OPC red wine extract. The 3 corresponding results: 1) It was found that [(3)H]cholesterol uptake was inhibited by up to 66% by an OPC grape seed extract or OPC red wine extract, when they were added as supplementation for incubation of HT29, Caco2, HepG2, or HuTu80 cells in a medium containing [(3)H]cholesterol. The IC(50) values were estimated to be 60 and 83 microg/mL for an OPC grape seed extract or OPC red wine extract, respectively. Uptake of the fluorescent cholesterol analogue NBD cholesterol was also inhibited. The antioxidative potency difference between the OPC grape seed extract and OPC red wine extract did not make any difference on the cholesterol uptake inhibition. 2) HT29 colon adenocarcinoma cell proliferation was inhibited by OPC red wine extract and OPC grape seed extract dose dependently, which induced an increase in apoptosis. 3) The 5-LOX activity was inhibited by the OPC red wine extract and OPC grape seed extract with IC(50) values of 35 and 13 microg/mL, respectively. These results indicate the nutritional benefits of OPC grape seed extract and OPC red wine extract and related polyphenols as dietary supplements for chronic degenerative diseases such as cardiovascular diseases and cancers.
12. Raf and MEK protein kinases are direct molecular targets for the chemopreventive effect of quercetin, a major flavonol in red wine. Cancer Res. Feb 1, 2008; 8(3): 46-55.
The health-promoting effects of OPC red wine extract and its nonflavonoid polyphenol compound resveratrol have been recognized. However, the underlying molecular mechanisms and molecular target(s) of red wine OPCs or other polyphenols need to be investigated. In this study, an OPC red wine extract and quercetin - a red wine flavonoid were studied for inhibition of 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced transformation of JB6 promotion-sensitive mouse skin epidermal (JB6 P+) cells. OPC red wine extract and quercetin inhibited the TPA-induced activation of activator protein-1 and nuclear factor-kappaB dose-dependently. The OPC red wine extract and quercetin inhibited signal transduction pathways involving 3 protein kinases: mitogen-activated protein kinase/extracellular signal-regulated kinase (ERK) kinase (MEK) 1 and Raf1 kinase, as indicated by Western blot and kinase assay data. Consequently, TPA-induced phosphorylation of ERK/p90 ribosomal S6 kinase was suppressed. The OPC red wine extract and quercetin inhibited MEK1 activity even more effectively than they inhibited Raf1 kinase activity. Quercetin exhibited stronger inhibition than a well-known pharmacologic inhibitor of MEK - PD098059. Neither MEK1 nor Raf1 kinase activity was affected by resveratrol. The direct binding of either OPC red wine extract or quercetin (but not resveratrol) with either MEK1 or Raf1 was implicated by pull-down assays. Computational modeling study indicated that quercetin formed a hydrogen bond with the backbone amide group of Ser(212), stabilizing the inactive conformation of the activation loop of MEK1, while resveratrol could not form the same hydrogen bond.
13. Myricetin down-regulates phorbol ester-induced cyclooxygenase-2 expression in mouse epidermal cells by blocking activation of nuclear factor kappa B. J Agric Food Chem. Nov. 14, 2007; 55(23): 9678-84.
OPC red wine extract contains a variety of flavonoid polyphenols and a non-flavonoid polyphenols such as resveratrol, which exert chemopreventive effects against cancer by preventing abnormal expression of cyclooxygenase-2 (COX-2). Other phytochemicals from OPC red wine extract might also contribute to the cancer-preventive activities. One of the major flavonols in the OPC red wine extract is 3,3',4',5,5',7-hexahydroxyflavone (myricetin). This study was to investigate whether 12-O-tetradecanoylphorbol-13-acetate (phorbol ester)-induced COX-2 expression could be inhibited by myricetin in JB6 P+ mouse epidermal (JB6 P+) cells by suppressing activation of nuclear factor kappa B (NF-kappaB). It was found that myricetin at 10 and 20 microM exhibited inhibitory effect on phorbol ester-induced upregulation of COX-2 protein. Resveratrol did not show this activity at the same concentrations. Myricetin suppressed the phorbol ester-induced production of prostaglandin E 2 and inhibited both COX-2 and NF-kappaB transactivation in phorbol ester-treated JB6 P+ cells. An electrophoretic mobility shift assay shows myricetin blocked the phorbol ester-stimulated binding of NF-kappaB with DNA. The OPC red wine extract inhibited phorbol ester-induced COX-2 expression and NF-kappaB transactivation in JB6 P+ cells. In conclusion, this study demonstrated the chemopreventive effects of myricetin in OPC red wine extract by inhibiting COX-2 expression via blocking the activation of NF-kappaB. Resveratrol was found inactive on the same target at the same concentrations.
14. Oenology: Red wine procyanidins and vascular health. Nature. November 30, 2006; 444: 566.
This short paper is about an investigation of 165 different wines for their procyanidin (OPC) contents. Consumptions of European red wines from certain areas are correlated with heart health and longevity in those regions, leading to reduced risks of coronary heart disease and to lower overall mortality. The highest procyanidins (OPC) are found in wines from the Tannat grape, grown in southwest France, an area with increased longevity in the population. Procyanidins (OPC) were found as the principal vasoactive polyphenols in red wines.
15. Red wine extract prevents neuronal apoptosis in vitro and reduces mortality of transgenic mice. Ann N Y Acad Sci. Nov 2006; 1089: 88-97.
A nutritional antioxidant - OPC red wine extract, was studied as antidegenerative agents on glutamate-induced apoptosis in primary cultures of cerebellar granule neurons (CGNs). Glutamate was known to interact with several intracellular factors associated with apoptosis of neurons, including intracellular [Ca(2+)]i overload, generation of reactive oxygen species (ROS), depression of cell energy metabolism, cytochrome c release, and increase in caspase-3 activity. Ascorbic acid (30 microM) and OPC red wine extract (5 microg/mL) were used to treat the cell culture 3 h earlier before the glutamate. It was found that glutamate-induced apoptosis in CGNs was prevented by the OPC and ascorbic acid. This in vitro effect of OPC red wine extract was tested using transgenic mice expressing the human mutated Cu, Zn superoxide dismutase (SOD1) G93A (mSOD1(G93A)). It was found mice fed with alcohol free-red wine concentrate survived in a significantly higher rate as compared to mice without the treatment using red wine concentrate. Therefore, the red wine OPC and related polyphenols may have nutritional benefit in protecting neurons from apoptosis.
16. Wine constituents inhibit thrombosis but not atherogenesis in C57BL/6 apolipoprotein E-deficient mice. Br J Nutr. Aug 2006; 96(2): 290-8.
“French Paradox” says that regular and moderate wine consumption is correlated with the lower cardiovascular risks in France, as compared with other industrialized countries. In this study, alcohol alone and OPC red wine extract were studied for possible reduction of plaque size and/or attenuation of thrombotic reactivity at the site of advanced atherosclerotic lesions. Each of the 3 materials including OPC red wine extract, purified (+)-catechin with alcohol and alcohol alone, was supplied in the drinking water of apoE-deficient (apoE(-/-)) C57BL/6 mice and wild-type counterparts for 12 weeks. It was found that blood thrombotic reactivity in the apoE(-/-) mice was significantly inhibited by the OPC red wine extract or (+)-catechin (P<0.05). A cylindrical perfusion chamber model of experimental thrombosis showed that area reductions in cross-sectional surface of the ex vivo thrombus were 64% and 63%, respectively, by the OPC red wine extract and (+)-catechin. All alcohol-containing mixtures were correlated to a larger size of aortic atherosclerotic lesions. While the OPC red wine extract and (+)-catechin exhibited a tend to reduce thrombogenicity in the wild-type mice, but at much less extent than in the apoE(-/-) mice. Therefore, a moderate and regular consumption of red wine or an OPC red wine extract may affect thrombogenic response and consequently reduce clinical cardiovascular risks, while red wine or an OPC red wine extract does not affect on the development of atherosclerotic lesions significantly. Red wine or the OPC red wine extract of the direct antithrombotic effect may also regulate the abnormally high thrombogenic responsiveness in apoE(-/-) mice.
17. The red wine phenolics piceatannol and myricetin act as agonists for estrogen receptor in human breast cancer cells. J Mol Endocr. 2005; 35: 269-281.
“French Paradox” has been a well-known term about moderate red wine consumption-associated heart health and longevity in France, originated from certain polyphenol components such as OPC, anthocyanins, resveratrol, etc. Further, previous epidemiological reports have suggested estrogen-like activity of red wine intake. Estrogens have a variety of other activities. When estrogens bind to and trans-activate estrogen receptor (ER), estrogens affect the proliferation of hormone-dependent breast cancer cells, causing responsive DNA sequences located within the promoter region of target genes. This study was to further investigate the health-beneficial effects of active phytochemical constituents in OPC red wine extract on the incidence of breast carcinoma in postmenopausal women. The estrogenic properties of piceatannol and myricetin, two abundant compounds in OPC red wine extract were studied using model systems of the hormone-sensitive MCF7 and the endocrine-independent SKBR3 breast cancer cells. Piceatannol and myricetin in the OPC red wine extract were demonstrated in this study to have a variety of estrogen-like activities including the following 3. 1) Piceatannol and myricetin transactivated endogenous ER. 2) Piceatannol and myricetin activated AF-2 (the agonist-dependent activation function 2) of ER and ER-beta in the context of the Gal4 chimeric proteins. 3) Piceatannol and myricetin rapidly induced the nuclear immunodetection of ER. 4) Piceatannol and myricetin affected the expression of diverse estrogen target genes. 5) Piceatannol and myricetin bound to ER and ER-beta by competing with 17beta-estradiol. 6) Consequently, piceatannol and myricetin stimulated the proliferation of MCF7 cells. Therefore, the estrogenic activity of OPC red wine extract is at least partially contributed from piceatannol and myricetin for the nutritional benefits, particularly in postmenopausal women of breast tumors.
18. Red wine and red wine polyphenolic compounds but not alcohol inhibit ADP-induced platelet aggregation. Eur J Intern Med. Oct 2003;14(6): 361-366.
OPC red wine extract and related polyphenols were investigated in reducing the risk of cardiovascular diseases, particularly coronary heart disease (CHD). The effects of alcohol and OPC red wine extract on platelet aggregation were directly compared. Each of the 3 tested materials including whole red wine, an OPC red wine extract and alcohol, was added in different concentrations to blood samples of standardized blood platelets. Two minutes later, different concentrations of ADP were added to induce aggregation. The results included the following 3 observations: 1) The ADP-induced platelet aggregation was not affected by alcohol in concentrations up to 0.24 percent in vitro. 2) The OPC red wine extract inhibited aggregation concentration-dependently and the significance started from concentrations of 45 mg/l and above. 3) Red wine only inhibited platelet aggregation at very high concentrations (approximately 0.24 and 0.48 alcohol %). Therefore, red wine has an inhibitory effect on platelet aggregation. The inhibition was caused by OPC and other polyphenolic compounds in the wine. A direct inhibitory effect of alcohol within a range up to 0.24 percent was not observed, but only at very high concentrations. It is unlikely that alcohol has any clinical relevance in a moderate drinking pattern to reach such a high alcohol concentration in blood. That is, alcohol may not exert the direct inhibitory effect on platelet aggregation in vivo. This could not, however, exclude the possibility that alcohol consumption could still exert platelet inhibition via metabolic changes.
19. Comparison of red wine extract and polyphenol constituents on endothelin-1 synthesis by cultured endothelial cells. Clin Sci (Lond). Aug 2002; 103 Suppl 48: 72S-75S.
The health benefits of red wine have been well recognized in the popular “French Paradox” theory. This observation has been attributed to the anti-thrombotic effects of ethanol, and to the antioxidant properties of polyphenolic compounds present in red wine, such as OPC, anthocyanins, quercetin, resveratrol, etc. An OPC red wine extract was studied in this paper for the effect on reduction of mortality from coronary heart disease. It was found that that OPC red wine extract inhibited endothelin-1 synthesis, concentration-dependently in the culture of bovine aortic endothelial cells. OPC red wine extract induced modifications in phosphotyrosine staining. The active OPC and other polyphenol components of red wine extract exhibited the role in regulating tyrosine kinase signalling. By inhibiting endothelin-1 synthesis, OPC red wine extract may provide the nutritional benefit as a dietary supplement in preventing the development of atherosclerosis, and hence decreasing the risk of coronary heart disease.
20. Nonalcoholic red wine extract and quercetin inhibit LDL oxidation without affecting plasma antioxidant vitamin and carotenoid concentrations. Clin Chem. Aug 2000; 46(8 Pt 1): 1162-70.
Red wine extract contains a variety of polyphenolic antioxidants, including OPC, anthocyanins, catechins, resveratrol, phenolic acids, and the flavonols quercetin and myricetin. Supplementation of an OPC red wine extract is expected to increase resistance of LDL to oxidation and hence reduce its atherogenicity. In the present study, an OPC red wine extract and quercetin were investigated for possible in vivo effects on the oxidative resistance of LDL, and on other antioxidative micronutrients present in the blood. Male volunteers were divided into 3 groups. Group 1 (n=10) were supplied with quercetin (30 mg/day) for 2 weeks; Group 2 (n=11) were supplied with OPC red wine extract (1 g/day) for 2 weeks; Group 3 as the control, supplied with a placebo drink without supplementation of either of OPC red wine extract or quercetin. All 3 groups were then followed by a 5-week washout period. The ex vivo copper-initiated oxidation of LDL was measured by lag phase (mean +/- SD). In Group 1, quercetin significantly increased the lag phase of the ex vivo copper-initiated LDL oxidation from 44 +/- 11 and 40 +/- 5 min for the baseline and placebo, respectively, to 51 +/- 7 min [P <0.05 compared with placebo and washout (41 +/- 9 min)] after supplementation. In Group 2, the OPC red wine extract significantly increased the lag phase from 40 +/- 11 min at the baseline, to 47 +/- 6 min [P <0.05 compared with placebo (38 +/- 4 min) and the washout values (40 +/- 5 min)]. The OPC red wine extract and quercetin did not affect plasma lipids (triglycerides, total cholesterol, LDL- and HDL-cholesterol) during the study period. The plasma levels of vitamin C and E, retinol, and carotenoid concentrations were not affected either by OPC red wine extract and quercetin. Therefore, the OPC red wine extract and quercetin inhibit LDL oxidation in vivo. The OPC red wine extract may have the nutritional effects as dietary supplement for the risk reduction of cardiovascular disease.
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French Red Wine Extract Containing Resveratrol & Anthocyanins Flavonois Is Related to French Paradox Theory
