Thursday, October 20, 2011

Grape Expectation: This Fruit Has Got It Going On! by Jerry Brainum

  A noted scientist once observed that humans don’t wear out—they rust out. What he meant was that many diseases, as well as the aging process itself, are likely related to out-of-control oxidation reactions in the body. No one argues about the necessity of oxygen for human life. Try breathing without it. Oxygen is necessary to power cellular processes involved in energy production, and without energy, you cannot live.

   The way the body uses oxygen isn’t a perfect process. In the course of it noxious by-products known as free radicals are unavoidably released. Free radicals go by different names, but they’re all unpaired electrons seeking to pair with other electrons. When a free radical finds paired electrons, it locks onto them, creating cellular havoc. Substances prone to oxidation are particularly effective at producing free radicals. Polyunsaturated fats, which play structural roles in various organs and tissues in the body, including cellular membranes and organs that are largely composed of fat, such as the brain, come under that heading. When attacked by free radicals, susceptible structures break down and fail. That, in turn, can lead to myriad diseases, including cardiovascular disease and cancer, the two primary killers.

   Luckily, nature and evolution have created a built-in defense system against free-radical cellular terrorism. It consists of various enzyme systems that neutralize free radicals, often by contributing an electron to stabilize the renegade free radical. Even so, free radicals are voracious in their appetite for pairing with another electron, and thousands of attacks occur at any time. It’s easy for the body to be overwhelmed.

   Once again, nature provides antidotes: dietary antioxidants. Vitamins C and E are the antioxidants familiar to most people, but many other nutrients provide potent protection, including the hundreds of flavonoid chemicals found in various fruits and vegetables. The frequent recommendation to eat at least five servings a day of fruits and vegetables is largely based on their fiber and antioxidant contents, which play definite roles in warding off degenerative diseases.

   The power of antioxidant protection is reflected in what’s known as the French paradox. Although the French habitually eat a considerable amount of saturated fat, the type of fat most linked to cardiovascular disease, they don’t have a high rate of that kind of health problem. Scientists who’ve studied the effect think that their fondness for drinking red wine with most meals is what enables the French to eat saturated fat with impunity.

   Red wine contains flavonoids called polyphenols. They’re potent antioxidants that can protect against cardiovascular disease with a number of mechanisms, including their ability to prevent the internal blood clotting that initiates most heart attacks. Polyphenols also stabilize low-density lipoprotein, the primary cholesterol carrier in the blood. That’s significant because LDL, which is known as the bad cholesterol, is dangerous mainly when oxidized.

   What if you just don’t want to drink wine? Can you get the benefits of its polyphenol content from any other source? A good candidate source is grape-seed extract, which also has powers above and beyond those found in a fine merlot.

Grape-Seed Power

   While common dietary antioxidants such as vitamins C and E do offer potent protective effects, they pale in comparison to grape-seed extract. Studies show that the active components of GSE are 20 times more potent than vitamin C and 50 times more potent than vitamin E in antioxidant activity. The functions of GSE, however, go beyond mere antioxidant protection. For example, it inhibits enzymes that promote the release of histamine from cellular mast cells. Histamine plays a dominant role in the symptoms associated with allergies and inflammation in the body.

   Another name for the active ingredients found in GSE is oligomeric proanthocyanidins. OPCs exist naturally in such fruits as apples, pears and grapes and in chocolate, red wine and tea. In supplement form they’re available as either grape-seed extract or an extract from pine bark known as pycnogenol, which is touted as being the superior source and usually costs nearly twice as much as grape-seed extract.

The truth, however, is that most of the research on the effects of OPCs used grape-seed extract. Even Jacques Masquelier, credited with discovering pycnogenol, says that grape-seed extract is superior. That’s because GSE contains gallic esters not found in pycnogenol that give it greater antioxidant activity. Similar to what happens with another popular antioxidant, lipoic acid, GSE works in both fat and water media, giving it a greater range of protection. In contrast, vitamin C works only in a water medium, while vitamin E functions only in a fat medium.

   Most of the studies showing a beneficial effect, however, were isolated-cell studies, also known as in-vitro, or test-tube, studies. That’s significant because flavonoids tend to be difficult for the human body to absorb. Studies tracking the fate of ingested grape-seed extract found that it was indeed difficult for the body to absorb the active ingredients, but about 25 percent was absorbed, and since they are potent antioxidants, it appears to be enough.

   As noted above, GSE neutralizes many of the problems that lead to cardiovascular disease, including the oxidation of LDL. It also protects vital organs, such as the liver and brain. The OPCs in grape-seed extract have a particular affinity for vascular and connective tissue. They inhibit enzymes that would otherwise degrade those tissues, and in doing so they maintain the integrity of various structural proteins of connective tissue and skin, such as collagen, elastin and hyaluronic acid. When those substances break down in the skin, visible signs of aging, such as wrinkles, appear. One study showed that a topical form of GSE offered protection against the oxidative damage caused by exposure to the sun.

   Pumping Up with GSE

   Nitric oxide has been getting extensive publicity lately. Various supplements have come on the market that increase the effect of nitric oxide synthesis. Among other functions, nitric oxide dilates blood vessels, which would increase the sensation of a muscular pump during training. GSE also increases nitric oxide synthesis, and it does so even more effectively than many of the high-priced supplements currently available. In addition, GSE stimulates vascular endothelial growth factor, which plays a role in wound healing.

   A recent study confirmed the effect of OPCs derived from pycnogenol in helping to alleviate impotence in men.1 The subjects took 120 milligrams a day of either pycnogenol or a placebo for three months in a double-blind protocol, meaning that neither the subjects nor the researchers knew who was taking what. After three months the men who got the pycnogenol showed significant improvement.

   The researchers attributed that result to pycnogenol’s ability to promote nitric oxide synthesis. Nitric oxide is required for the dilation of blood vessels that lead to an erection. Most of today’s so-called impotence drugs, such as Viagra, work through the same mechanism.

   GSE may aid workout recovery by decreasing various chemical initiators of inflammation in the body. Hard training leads to a localized inflammation in muscles, and muscles cannot fully recover until it’s doused. The inflammation is caused by a number of chemicals associated with immune function, such as cytokines, interleukins and tumor necrosis factor-alpha. By neutralizing their excess activity, GSE helps to heal muscle inflammation after intense training, thereby speeding recovery.

GSE: Immunity Booster

   GSE helps protect against various types of cancer. In isolated-cell studies it destroyed several types of cancers, such as those affecting the breasts, lungs and stomach. GSE also reduces the side effects of chemotherapy drugs, which are designed to destroy cancer cells by increasing free-radical production in tumors—an undesirable activity in normal cells. Other research shows that GSE inhibits the virus that causes AIDS, but, once again, the studies involved were test-tube studies.

   A recent study found that GSE may offer benefits in the treatment of advanced prostate cancer, the number-one killer of men.2 Many prostate tumors are initially androgen-sensitive; that is, their growth is stimulated by the presence of testosterone and other androgens. The treatment is to block androgen production, hoping the tumor will recede. In some cases, however, it returns, and this time it’s androgen-independent. Advanced prostate tumors like that are harder to treat and have a greater tendency to metastasize, or spread.

   In the new study GSE strongly inhibited advanced prostate tumors. The researchers believe it accomplished that through at least two mechanisms: It prevents the release of a chemical that enables tumors to spread in the body, and it increases a binding protein for IGF-1, which promotes tumor growth. As a result the tumor winds up killing itself, a process known as apoptosis.

Girlieman Terminator

   Another study found that substances in GSE can inhibit aromatase,3 the ubiquitous enzyme that converts androgens, such as testosterone, into estrogen. From a medical point of view, that means that GSE may help prevent estrogen-related cancer. Inhibiting aromatase in men leads to increased testosterone and lower estrogen—and lower estrogen equals less subcutaneous bodyfat, less water retention and less likelihood that excess-estrogen-related conditions, such as gynecomastia, or male breasts, will occur.

   GSE also exerts insulinlike activity in aiding glucose uptake into cells.4 It appears to lower elevated glucose levels, such as those that occur in people who have diabetes and those who use human growth hormone, as well as increasing the activity of cellular proteins that aid in getting glucose into cells, such as GLUT-4.

   Another interesting isolated-cell study found that a combination of aged garlic and pycnogenol caused a potent release of growth hormone.5 The study used skin cells that had been genetically engineered to react to substances touted as growth hormone releasers. The results showed that pycnogenol is about 1,000 times more potent in its ability to promote GH release than the other substances tested, including amino acids.

   Isolated-cell studies also show that both GSE and pycnogenol inhibit enzymes called lipases, which are required to absorb dietary fat.6,7 Orlistat, a drug that’s currently used to treat obesity, works in the same manner, with the result that about 30 percent less fat is absorbed during a meal. That means fewer fat calories taken in, possibly leading to fat losses.

Safety Issues

What about toxicity? Grape-seed extract is remarkably safe. It shows no mutagenic effects—i.e., links to tumor formation—and has no known interaction with drugs. It does, however, help prevent liver failure if someone takes too much acetaminophen (Tylenol). The best dosage for health effects is about one milligram per kilogram (2.2 pounds) of bodyweight. So someone weighing 200 pounds should take about 100 milligrams of GSE daily. Another method is to begin with a loading dose of 300 milligrams a day in divided doses for about a month, then switch to the one-milligram-per-kilogram-of-bodyweight maintenance dose.


1 Durackova, Z., et al. (2003). Lipid metabolism and erectile function improvement by pycnogenol extract from the bark of Pinus pinaster in patients suffering from erectile dysfunction—a pilot study. Nut Res. 23:1189-98.

2 Singh, R., et al. (2004). Grape-seed extract inhibits advanced human prostate tumor growth and angiogenesis and unregulated insulinlike growth factor binding protein-3. Int J Cancer. 108:733-40.

3 Eng, E.T., et al. (2003). Suppression of estrogen biosynthesis by procyanidin dimers in red wine and grape seeds. Cancer Res. 63:8516-22.

4 Pinent, M., et al. (2004). Grape-seed-derived procyanidins have an antihypoglycemic effect in streptozotocin-induced diabetic rats and insulinomemetic activity in insulin-sensitive cell lines. Endocrinology. In press.

5 Buz’Zard, A., et al. (2002). Kyolic and pycnogenol increase human growth hormone secretion in genetically engineered keratinocytes. Growth hormone and IGF-1 Research. 12:34-40.

6 Moreno, D.A., et al. (2003). Inhibitory effects of grape-seed extract on lipases. Nutrition. 19:876-79.

7 Hasegawa, N. (2000). Inhibition of lipogenesis by pycnogenol. Phytotherapy Res. 14:472-473.

©,2013 Jerry Brainum. Any reprinting in any type of media, including electronic and foreign is expressly prohibited.

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