Grouppe Kurosawa: Natural Medicine - The Extraction of Medicinal Compounds (print)

The Extraction of Medicinal Compounds
from Fruits and Vegetables

Many herbs, medicinal plants, and medicinal vegetables/fruit contain molecules that can prevent, cure or ameliorate the course of various acute and chronic diseases. These molecules are not nutrients. They are true medicinal compounds in the same category as quinine, digitalis and other famous plant-derived compounds. Diets rich in fruits and vegetables are consistently associated with a decreased risk of cancer and other chronic diseases. The US Department of Health and Human Services, in their Healthy People 2000 and Healthy People 2010 campaigns, has advocated the consumption of 5 to 6 servings of fruits and vegetables daily. Although Americans have changed their dietary habits in the last few years, the “5 A Day” message has failed to inform consumers that nutrients and fiber, although beneficial to overall health, are not medicinal compounds. As a consequence, the consumption of medically significant dark green and cruciferous vegetables, plants that contain a high concentration of anti-cancer medicinal compounds, remains low.

Iceberg lettuce, tomatoes, French fried potatoes, bananas and orange juice are the most commonly eaten fruits and vegetables in the American diet, consisting of 30% of all fruits and vegetables consumed. Cruciferous vegetables, such as broccoli, cauliflower, kale, and Brussels sprouts, are only consumed by 3% of Americans. Spinach, a dark green vegetable, is only consumed by 2% of Americans. This is unfortunate because the plants listed above contain, by far, the highest concentrations of medicinally important phytochemicals. Broccoli and Brussels sprouts are not popular foods in America. Former President of the United States George Bush made it very clear that he “didn’t like broccoli” and had no intention of eating it regardless of its health benefits. Kale, an extremely beneficial dark green and cruciferous vegetable, is virtually absent from the American diet, as is soy. Someone once said, “you are what you eat”. This statement is more true than most people realize.

Taste is obviously a significant factor in why people do not consume medicinally important foods. A high fat content hamburger tastes much better and is more psychologically satisfying than steamed broccoli. Unfortunately, hamburger contains a high concentration of arachidonic acid, a polyunsaturated fatty acid that is a direct precursor of inflammation-inducing prostaglandins. It is certainly true that we, as consumers, cannot “eat right” all the time, but this is really an excuse for not “eating right” most of the time. In the final analysis, we eat what we like. Medicinal foods, or foods containing medicinally (so-called phytochemicals)—not nutritionally—important anti-disease compounds, fall into a number of well defined categories. Anti-cancer compounds found in vegetables and fruits include lycopene (tomatoes), lutein and zeaxanthin (corn and leafy greens), anthocyanins (red apples, grapes, berries and wine), beta-carotene (carrots, mangos, apricots, pumpkin, and squash), citris flavonoids (oranges, lemons, grapefruit), glucosinolates (broccoli, Brussels sprouts, kale), and allyl sulfides (onions and garlic). The National Cancer Institute and the American Institute for Cancer Research guidelines recommend 5 to 9 servings of these fruits and vegetables each day. Ain’t ever going to happen! Many important fruits and vegetables are not freely available, especially when traveling. In the home, cooking convenience, smell and taste are the only important factors in the diets of most busy Americans. If you can’t stand the smell of Brussels sprouts, you are not going to cook them in your home, regardless of their medicinal properties. Fortunately, all is not lost. These important phytochemicals can be formulated into a palatable food that anyone, even the most fussy eaters, can enjoy.

One of the problems associated with consuming herbs, plant extracts, or medicinal foods such as soy products is that of bioavailability. Many natural medicinal compounds are not soluble in water. When orally consumed, only a small percentage of the compounds are absorbed by the stomach. Many of compounds that are absorbed are rapidly neutralized in their initial passage through the liver and the intestinal wall. In brief, the oral consumption of natural medicinal compounds is not always an effective means to introduce these important compounds into the body.

Asian women have a dramatically reduced incidence of breast cancer compared to Western women. Many regional variations in cancer incidence have been reported and attributed, in part, to differences in dietary intake. Asian women consume very large amounts of soy isoflavones in their diet. Soy isoflavones are a group of related compounds that have been shown to have dramatic effects on experimental and natural cancers. One soy isoflavone, genistein, is a powerful tyrosine kinase inhibitor that prevents the growth of cancer cells. Genistein is also an estrogen analogue that binds the estrogen receptor, thereby negating the growth of estrogen dependent cancers. Genistein also blocks the ability of estrogenic pesticide compounds from stimulating the growth of normal breast cells. Unfortunately, soy products are a minor component of the Western diet. Soy based products are difficult to find in traditional grocery stores in many areas of the United States. When Asian women migrate to the West, their diets change and their susceptibility to breast and other cancers increase. Adding soy products to the Western diet is a commendable idea, but in reality it is not feasible. In order for genistein, a water insoluble compound, to have an effect on breast cancer, soy products would have to constitute a substantial portion of the diet. This isn’t going to happen in the West.

We have developed a technology for introducing water insoluble medicinal compounds into the body by topically applying them to areas of the body that contain large amounts of subcutaneous fat. Most water insoluble medicinal compounds are soluble in ethanol. Ethanol extracts of herbs and medicinal plants have been available in health food stores for a long time. The process is quite simple. Fresh plant material is ground and soaked in ethanol for a period of days. The ethanol soluble components are poured off and packaged as highly concentrated plant extracts. Gingko bilova, Genseng, Garlic, and many other herbal plants are commonly available as ethanol extracts. These extracts are usually packaged in dropper bottles. The usual protocol is to add 30 or more drops in a glass of water two to three times a day. Unfortunately, many ethanol soluble compounds will immediately precipitate and fall out of solution when added to water. Adding ethanol extracts to water defeats the purpose of preparing ethanol extracts—to dissolve previously insoluble compounds so they can be more readily absorbed by the body. We have developed a method for directly introducing these ethanol extracts into the body by adding them to a proprietary mixture of oils. The oil is rubbed into fat deposits, such as the thighs, buttox or abdomen for one minute. Within five minutes, many of the compounds cross the epidermis and dermis and can be found in the blood and lymphatic fluid. This simple procedure allows important medicinal compounds to be introduced into the body at concentrations not attainable by oral ingestion.

Many natural medicinal compounds have been found to be effective against the HIV virus and numerous cancers. In the laboratory, these compounds are dissolved in ethanol or DMSO and carefully diluted into tissue culture solutions. In an artificial environment, such as a tissue culture dish, very small concentrations of natural products have proven very effective in killing cancer cells or blocking the proliferation of viruses such as HIV. Unfortunately, these compounds rapidly precipitate out of solution when injected at high concentrations into the blood. Most natural compounds are poorly soluble in water and very sensitive to immediate changes in pH. The blood is buffered to approximately 7.4. Many medicinal compounds, such as flavonoids, are only soluble in water at extreme alkaline pH values. At acid pH, these compounds are not soluble (if in water), but they are stable and do not aggregate. The pH of the skin is 5.5. The skin is a perfect milieu for introducing ethanol soluble, acid pH stable, compounds into the body. Once the epidermis is crossed, the compounds can enter both the blood and the lymphatic system that bathes all the cells in the body with nutrients, oxygen, etc. The topical introduction of natural and synthetic medicinal compounds into the body allows high concentrations of medicinal compounds to target specific areas of the body, such as fat deposits (for weight control) or the joints (for arthritis). Since many triglycerides directly enter the lymphatic system after absorption from the intestines, complexing ethanol soluble compounds with specific fats allows both to cross the epidermis and eventually enter the lymph nodes throughout the body, the hiding place of the HIV virus and the organs where all immune responses are initiated. If lipid-complexed natural compounds can readily penetrate the lymph nodes, they could neutralize the HIV virus at its source.

The implications of this technology for public health are enormous. Third world countries with little or no public health budgets can use ethanol to extract medicinal compounds from plants. These extracts can be mixed with the appropriate lipids and topically applied to treat, prevent or ameliorate the symptoms of disease. It is difficult to imagine a more powerful, inexpensive therapeutic or preventative treatment protocol. Properly formulated, the ethanol extract/lipid mixture does not induce contact hypersensitivity. We have topically applied many different ethanol extracts to the bodies of test subjects without inducing a trace of inflammation. There are two basic reasons for the lack of inflammation. First, the extract/lipid mixture does not disrupt the stratum corneum, or cornified layer of the skin. It penetrates it by mixing with the natural lipids in the skin. Second, a specific plant extract is included in each formulation that inhibits a topical allergic response to the ethanol soluble plant compounds.

This technology has implications that transcend the treatment of disease. Important medicinal foods, such as soy, broccoli, and other vegetables and fruits can be ethanol extracted and mixed into a topical cream. This cream can be used as a method of introducing these preventative compounds into the body in concentrations high enough to prevent disease, such as breast cancer. In fact, a cream consisting of known anti-cancer flavones (genistein) could be rubbed directly onto the breasts. The flavones, complexed to the lipid carrier, would be expected to remain in the fat deposits of the breast for prolonged periods of time (the breast consists primarily of fat cells). The smell of the extract/lipid mixture can be varied by essential oils, such as lavender, peppermint, orange, etc. This technology can be used to introduce important medicinal compounds into the bodies of children and animals, or anyone who is a “picky eater”. Taste is taken out of the equation. These creams can be either nutritional supplements or drugs if they are used to treat disease. One thing they are not is food. The effective introduction of medicinal compounds across the epidermal barrier has been one of the major goals of the pharmaceutical and biotech industries for years. This carrier system was designed to introduce natural medicinal compounds into the body, but it could be used to introduce virtually anything water insoluble into the body, including synthetic compounds such as aspirin derivatives or vaccine components.