Phytochemicals: Guardians of Our Health

A Continuing Education Article

by Winston J Craig, PhD, RD
Professor of Nutrition at Andrews University, Berrien Springs, MI

Increasingly, Americans are being told to eat more plant foods (1). The optimal diet that is recommended by most
professional health organizations is a low-fat, low-saturated fat, high-complex carbohydrate diet characterized by a
frequent consumption of vegetables, fruit, whole-grain bread, rice and pasta. The WHO study group on diet,
nutrition and prevention of communicable diseases recommended that we daily consume at least 400 grams (14 ozs)
of fruits and vegetables, including at least 30 gm (1 oz) of pulses, nuts and seeds (2).
Consuming a diet rich in such plant foods will provide a milieu of phytochemicals, non-nutritive substances in
plants that possess health-protective effects. Nuts, whole grains, fruits and vegetables contain an abundance of
phenolic compounds, terpenoids, pigments and other natural antioxidants (including vitamins A, C and E) that have
been associated with protection from and/or treatment of chronic diseases such as heart disease, cancer, diabetes,
and hypertension as well as other medical conditions (3). In addition to the phytochemicals, fruits and vegetables are
naturally low in fat, saturated fat, cholesterol, calories and sodium, and are rich in potassium, fiber, folic acid and
vitamin C.
Eat more fruits and vegetables
In eighty-two percent of 156 dietary studies reviewed recently, it was found that fruit and vegetable consumption
provided significant protection against many cancers (4). People who eat higher amounts of fruits and vegetables
have about one-half the risk of cancer and less mortality from cancer (5,6). Fruits and vegetables are most effective
against those cancers that involve epithelial cells such as cancer of the lung, cervix, esophagus, stomach, colon and
pancreas. Results from a large-scale Italian study revealed that relative risk of common epithelial cancers ranged
from 0.2 to 0.5 for the highest tertile compared with the lowest tertile of vegetable intake (7). The protective effect
of vegetables was also observed for hormone-related cancers. Higher intakes of fruit provided reduced risk of many
epithelial cancers although the protection was generally of a lesser magnitude.
At present there is a nationwide campaign to promote an increased use of fruits and vegetables. The "5-a-Day for
Better Health" program was designed to encourage the consumption of at least five servings a day of fruit and
vegetables. The average American eats only about one and one-half servings of vegetables per day and less than one
serving of fruit per day. A recent survey of American eating habits showed that only 1 in 11 Americans met the
guidelines for eating at least 3 servings a day of vegetables and at least 2 servings a day of fruit (8). In fact, one in
every nine Americans surveyed ate no fruit and no vegetable on the day of the survey, and 45% reported eating no
fruit that day. When asked how many servings of fruits and vegetables someone should eat every day for good
health, people gave amazing answers. Two out of every three Americans surveyed said they thought that only 2 or
fewer servings were sufficient for good health (9).
A recently published study of 2400 Greek women noted that vegetable and fruit consumption were independently
associated with significant reductions in the incidence of breast cancer (10). Women with the highest intake of
vegetables (4-5 servings/day) had a 46 percent lower risk of breast cancer compared with women that had the lowest
vegetable intake (less than 2 servings/day). Women with the highest intake of fruit (6 servings/day) had a 35 percent
lower risk of breast cancer compared with women that had the lowest fruit intake (less than 2 servings/day).
Plant protection
The National Cancer Institute has spent in excess of $20 million over the past 5 years researching the anticancer
potential of plant foods (11). The foods and herbs with the highest anticancer activity include garlic, soybeans,
cabbage, ginger, licorice, and the umbelliferous vegetables (including carrots, celery, cilantro, parsley, and parsnips).
Foods with a modest level of cancer-protective activity include onions, flax, citrus, turmeric, cruciferous vegetables
(broccoli, Brussels sprouts, cabbage and cauliflower), solanaceous vegetables (tomatoes and peppers), brown rice
and whole wheat. Other foods and herbs that were found to contain a measure of anti-cancer activity included oats
and barley, mints, rosemary, thyme, oregano, sage, basil, cucumber, cantaloupe and berries (11).
Research has identified a host of active substances in these foods that provide the protection against cancer. These
phytochemicals include allyl sulfides in garlic and onions; phytates in grains and legumes; glucarates in citrus,
grains and solanaceous vegetables; lignans in flax and soy beans; isoflavones in soy beans; saponins in legumes;
indoles, isothiocyanates and dithiolthione in cruciferous vegetables; ellagic acid in grapes, strawberries, raspberries
and nuts; phthalides and polyacetylenes in the umbelliferous vegetables; and a whole range of flavonoids,
carotenoids and terpenoids in various plant foods. These beneficial chemicals block various hormone actions and
metabolic pathways that are associated with the development of cancer (11,12).
Estrogens can be metabolized by cytochrome P-450 enzymes to produce 2-hydroxyestrogens or 16 alpha-
hydroxyestrogens. The relative activity of these two pathways in an individual determines risk for hormone-
dependant cancers. Hydroxylation at C-16 leads to metabolites that promotes estrogen action and increases risk of
breast and uterine cancer while C-2 hydroxylation produces metabolites that oppose estrogen action and decreases
cancer risk (13). Lifestyle factors influence the activity of these two pathways. For example, obesity suppresses C-2
hydroxylation while aerobic exercise elevates it. The C- 16 pathway is elevated by high-fat diets. Phytochemicals in
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our food can alter the relative activities of these pathways. Indole-3-carbinol in cruciferous vegetables is a powerful
inducer of the enzyme estrogen 2-hydroxylase (13).
Are the phytochemicals destroyed by cooking? Most of the compounds are heat stable and are not significantly lost
in the cooking water. While vitamin C is partially lost by cooking, the availability of carotenoids and the level of
indoles in broccoli may actually be increased during cooking(14).
Less cancer with soy
Soybeans contain fairly high levels of several compounds with demonstrated anti-cancer activity, including phytates,
protease inhibitors, phytosterols, saponins and isoflavonoids (15). Consumption of soybeans is suggested as a
contributing factor in the low incidence of breast and prostate cancer in Japanese women and men, respectively.
Chinese having a regular consumption of soybeans and/or tofu have only one-half as much cancer of the stomach,
colon, rectum, breast, and lung compared with those Chinese who rarely consume soy or soy products (16)
Soybeans, and non-fermented soy products such as tofu, are a very rich and unique source of the isoflavones,
genistein and diadzein. These isoflavonoids inhibit the growth of hormone-dependant and hormone-independent
cancer cells in culture (17). The isoflavones in soy have been shown to inhibit the growth of both human breast
cancer and prostate cancer (16). A low mortality from prostatic cancer is seen in Japanese men who consume a low-
fat diet high in soy products. Decreased prostatic cancer is also seen in Hawaiian men of Japanese descent who
regularly eat rice and tofu.
Estrogens can stimulate the growth of mammary tumors in experimental animals. Genistein in soy acts as a weak
antiestrogen, competitively binding to the estrogen receptors and reducing the synthesis and activity of endogenous
estrogen (18). Hence, genestein can function as an estrogen antagonist and reduce the risk of promoting the growth
of estrogen-sensitive tumors. One can obtain substantial levels of dietary isoflavones by a daily consumption of an
ounce or two of soy protein. One- half cup of soybeans, one cup of soy beverage, or 4 ounces of tofu can provide
about 30-40 mg of genestein (19).
Soy also lowers cholesterol
A number of human studies over the past 20 years have shown that persons who daily consume about 1 to 2 ozs of
soy protein for about 4 weeks can experience a decrease in their total and LDL cholesterol levels of as much as 10 to
20 percent when initial blood cholesterol levels are elevated (20). In some instances, persons with normal blood
cholesterol levels may also enjoy the benefit of lowered blood lipid levels by consuming soy. While LDL levels are
decreased, HDL cholesterol levels normally remain unchanged.
The use of soy also lowers triglyceride levels, especially in subjects with elevated blood triglyceride levels. The
blood lipid responses tend to be more pronounced in younger adults than in older adults. The reductions are
normally greater in subjects with high initial cholesterol levels. A recent meta-analysis of 38 controlled, clinical
trials found that an average intake of 47 gms of soy protein per day produced on average a 13 percent decrease in
LDL cholesterol levels and a 10 percent decrease in triglyceride levels (21).
As little as 1 to 2 ozs of isolated soy protein incorporated into muffins, breads, cookies, and other commonly eaten
bakery items can effectively lower the cholesterol levels of men who initially had cholesterol levels above 220 mg/dl
(22). Simply replacing milk with a soy beverage has been shown to cause blood cholesterol levels to decrease about
5 to 10% and LDL cholesterol levels to drop 10 to 20 percent within 4 weeks (23). It is obvious that very modest
changes in our diet appear to have a measurable effect on blood lipid levels.
The mechanism for the action of soy is not known with certainty at this time. The soy isoflavones are potent
inhibitors of cholesterol synthesis, and the plant sterols (for example, beta-sitosterol) and saponins in soy can block
cholesterol absorption from the diet or increase cholesterol excretion from the body (24).
Phytochemicals in citrus
Citrus, in addition to its ample supply of vitamin C, folic acid, potassium and pectin, contains a host of active
phytochemicals that also protect our health. In fact, there are over 170 phytochemicals in an orange (25). The more
than 60 flavonoids in citrus possess a wide range of properties including anti- inflammatory and antitumor activity,
inhibition of blood clots and strong antioxidant activity (26). The flavonoids, tangeretin and nobiletin, are known to
be potent inhibitors of tumor cell growth and can activate the detoxifying P-450 enzyme system (27).
There are about 40 limonoids in citrus, with limonin and nomilin being the principal ones. These compounds, which
occur in high concentrations in grapefruit and orange juice, partly provide the bitter taste in citrus. Limonoids
possess the ability to inhibit tumor formation by stimulating the enzyme glutathione S-transferase (GST) (28). GST
is a detoxifying enzyme that catalyzes the reaction of glutathione with dangerous electrophiles to form less toxic and
more water-soluble compounds that can be easily excreted from the body.
Orange and lemon oil contain substantial amounts of limonene, a terpenoid that also possesses anti-cancer activity
(29). Citrus pulp and the albedo (the white of the orange) is rich in glucarates. These substances are being studied
for their potential to prevent breast cancer and to lower the risk of symptoms of premenstrual syndrome (25).
There are about 20 carotenoids in an orange. Pink grapefruit have a high content of beta- carotene, while other citrus
(such as tangerines, oranges) contain high levels of other carotenoids (lutein, zeaxanthin, beta-cryptoxanthin) (30)
that have significant antioxidant activity. These carotenoids are associated with a lower incidence of age-related
macular degeneration, the leading cause of blindness in the US after age 65 (31). Pink grapefruit also contains a high
level of 1ycopene, the red pigment in tomatoes and guava that has a significant anti-tumor activity.
Protection from whole grains

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The phytochemicals found in fruit and vegetables are very similar to those located in whole grains. The
phytochemicals that are found in grains include plant sterols, phytases, phytoestrogens, tocotrienols, lignans, ellagic
acid, and saponins (32). These substances reduce the risk of cardiovascular disease and cancer. The active
phytochemicals are concentrated in the bran and the germ, so that the health benefits of grains are maximized when
the whole grain product is consumed. Refining wheat, for example, causes about a 200 to 300-fold loss in the
phytochemical content (33).
Fruits, vegetables and cereal grains contain a variety of isoprenoid compounds that exhibit anticancer activities.
These compounds, which derive from mevalonate metabolism, include the tocotrienols (related to the tocopherols),
and monoterpenes such as limonene, geraniol, menthol, carvone, beta-ionone, perillyl alcohol (34). Since tumor
cells synthesize and accumulate cholesterol faster than normal cells, the isoprenoids can suppress tumor growth by
inhibiting HMG-CoA reductase (the rate limiting step in cholesterol synthesis).
In addition, terpenoids such as limonene, geraniol, menthol and carvone act as anticarcinogens by inducing the
detoxifying enzyme GST (34). Overall, the terpenoids and tocotrienols increase tumor latency and decrease tumor
multiplicity. In addition, these same compounds elicit a significant reduction in total and LDL cholesterol levels (34-
36), thereby reducing the risk of heart disease.
Benefits of flax
Flour derived from flax seed is increasingly being used in bread and bakery products to provide not only a nutty
flavor but also to increase the nutritional and health benefits of the final product. The use of flax seed can lower both
blood cholesterol and LDL cholesterol levels due to its very low saturated fat content (37). Flax seed oil is one of the
richest known sources of omega-3 fat, since linolenic acid comprises 55 percent of the oil. This provides flax with
its anti-inflammatory effect (and hence the possible usefulness for the treatment of lupus, arthritis, and different
allergies) and the ability to boost the immune system (38).
Flax seed is also an extremely rich source of lignans. Plant lignans are converted to mammalian lignans
(enterolactone and enterodiol) by bacterial fermentation in the colon (39). These mammalian lignans appear to be
anticarcinogenic. The lignan metabolites bear a structural similarity to estrogens and can bind to estrogen receptors
and inhibit the growth of estrogen-stimulated breast cancer (40-42). Urinary excretion of lignans is reduced in
women with breast cancer, while the consumption of flaxseed powder increases the urinary level of lignans by 8 to
18-fold (43).
Flavonoids
The many flavonoids in plants (fruit, vegetables, nuts and grains) have extensive biological properties that promote
human health and help reduce the risk of disease. Flavonoids extend the activity of vitamin C; act as antioxidants;
protect LDL cholesterol from oxidation to the unsafe cholesterol oxides; inhibit platelet aggregation; and have anti-
inflammatory and anti-tumor action (44,45).
Quercetin is the major flavonol in the Western diet. Rich sources of quercetin are red and yellow onions, kale,
broccoli, red grapes, cherries, French beans, apples and cereals. Quercetin possesses both anticarcinogenic activity
and the ability to inhibit LDL oxidation (46). The Zutphen study of elderly men in the Netherlands found that the
flavonoid intake was inversely associated with heart disease mortality and incidence of heart attack over a five-year
period. Those who had the highest consumption of flavonoids had 60% less mortality from heart disease than the
low flavonoid consumers (47).
Red wine and grape juice (but not white wine) contain a significant level of phenolic flavonoids and red anthocyanin
pigments. These compounds can act as antioxidants, protect against LDL oxidation and inhibit platelet aggregation,
thereby providing protection against heart disease (48-50). The phenolic components of red wine, rather than the
alcohol content, have been shown to reduce the levels of LDL cholesterol and lipoprotein (a) (51). Substantial levels
of the phenolic antioxidant compounds are found in grapes and unfermented grape juice (44).
A whole variety of phenolic compounds, in addition to the flavonoids, are widely distributed in grains, fruits,
vegetables and herbs so that it is not uncommon for one to consume up to 1 g of phenolic compounds per day. These
phenolics influence the quality, acceptability and stability of foods by acting as flavorants, colorants and
antioxidants (52). The phenolic compounds (such as caffeic, ellagic and ferulic acids, sesamol and vanillin) also
exhibit anticarcinogenic activity and inhibit atherosclerosis (52).
Color your life
Pigments provide a lot of color to our food and enhance the enjoyment of the eating experience. Presently, there are
almost 2000 known plant pigments in our food, including over 800 flavonoids, 450 carotenoids and 150
anthocyanins (53). These pigments do more than just appeal to our senses; they also protect us from disease.
Anthocyanins are the water soluble, reddish pigments found in many fruits, such as strawberries, cherries,
cranberries, raspberries, blueberries, grapes and black currants. Since anthocyanins inhibit HMG-CoA reductase and
thereby inhibit cholesterol synthesis these fruits provide protection against heart disease. The carotenoids are
powerful antioxidants that act to quench free radicals and provide protection against oxidative damage, and
stimulate immune function. Persons with high levels of serum carotenoids have a reduced risk of heart disease and
cancer (54-56). Carotenoids are the pigments found in yellow-orange, red and green vegetables and the yellow-
orange fruits.
Several large-scale, randomized trials (such as the Physicians' Health Study and the Women's Health Study) are in
progress to determine the health benefits and safety of well-nourished populations taking beta-carotene and other
antioxidant supplements. Results from some of the clinical trials have been disappointing to some in that the
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supplements were unable to provide any substantial protective effect against heart disease or cancer (57). On the
other hand, the consumption of foods naturally rich in beta- carotene, lycopene, lutein or other carotenoids is
consistently associated with a lower risk of cancer or heart disease (54,55).
The pigments isolated from the bean seed coat of Phaseolus vulgarus, the common bean, exhibit strong
antioxidative activity. These anthocyanin pigments play an important role in chemically protecting the bean from
oxidative damage (58). When the beans are ingested the pigments may also provide protection to the consumer
against oxidative damage of cell membrane lipids, and supplement the work of vitamins C and E.
Additional protection from herbs
Compounds that stimulate the activity of glutathione S-transferase (GST) are considered as inhibitors of cancer.
Substances that stimulate GST activity include the phthalides in celery seed, the sulfides in garlic and onions, the
dithiolthiones and isothiocyanates in broccoli and other cruciferous vegetables, the bitter liminoids in citrus and the
curcumins in ginger and turmeric (12,28,59).
Rosemary, sage, oregano, thyme and other flavoring herbs that belong to the Labiatae family are known to possess
strong antioxidative activity (60). For example, rosemary and sage contain substantial levels of carnosol and ursolic
acid, potent antioxidants that possess anti-tumor activity (61). Ginger contains a dozen phenolic compounds, known
as gingerols and diarylhaptanoids, that have an antioxidant activity that is even greater than alpha-tocopherol
(vitamin E) (62). The compounds responsible for the flavors of many common herbs and seasonings are terpenoids,
similar to those mentioned earlier in fruits, vegetables and cereal grains. The terpenoids in herbs are reported to be
useful cancer chemopreventive agents (63-67).
Garlic, onions and other members of the Allium family are rich in sulfides and other protective substances. Garlic
contains a number of allyl sulfides that are known to decrease the tendency of blood clots to form, significantly
lower total and LDL cholesterol levels and decrease the risk of cancer at many sites (68,69). Clearly, a diet in which
herbs are generously used to flavor the food will provide a variety of active phytochemicals that promote health and
protect against chronic diseases. A number of other frequently used herbal products are reported to provide
protection or relief from a variety of common ailments (70).
Conclusion
Clearly, with such a wide variety of protective phytochemicals in fruits, vegetables, whole grains, nuts, legumes and
herbal seasonings the regular consumption of these foods is essential to ensuring a healthier population that has
lower rates of heart disease and cancer (3). According to the USDA Food Guide Pyramid it is recommended that
adults consume between 5 and 9 servings a day of fruits and vegetables. Since very few Americans achieve that
level of consumption many could surely benefit from a substantial increase in their use of fruits and vegetables.
While the antioxidant vitamins C and E and beta-carotene apparently have a low toxicity (71), the benefits of a
regular and long-term intake of antioxidant supplements are far from conclusive and await further verification from
the large-scale intervention trials (57,72). On the other hand, the regular consumption of foods that are naturally
high in antioxidants (fruits, vegetables and whole grains) is positively associated with substantial health benefits.
These foods contain hundreds of antioxidants, and at least some of them act synergistically (73). Furthermore, the
safety of consuming concentrated extracts of fruits and vegetables that contain very high levels of phytochemicals is
unknown and unwarranted at this time. The protective benefits of a phytochemical-rich diet is best obtained from a
frequent consumption of fruits, vegetables and whole grain products.
References (sunt vreo 2 pagini - ti le pot trimite daca doresti)

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 FUNCTIONAL FOODS

What are Functional Foods?

"Functional foods" is a broad term that has attracted significant attention from scientific researchers, health
professionals and journalists. Although there is no consensus on an exact definition, "functional foods" usually refers
to foods containing significant levels of biologically active components that impart health benefits beyond basic
nutrition. These components are often referred to as phytochemicals-meaning plant chemicals.
For example, we know that soy is a good source of protein and other nutrients. However, some scientific research
indicates that certain components in soy, called isoflavones, may provide long-term benefits such as reducing the
risk of certain diseases.
Some people have used the term "nutraceuticals" in place of functional foods, however, this term may be more
appropriate to describe medical foods-that is, foods designed for specific medical purposes, normally taken under
direction of a doctor.

Are Functional Foods New?

Functional components have always been present in foods. What is new is that researchers are beginning to identify
these components and they are now trying to determine exactly what benefits they may offer. Functional attributes
of many traditional foods are being discovered, while new food products are also being developed to enhance or
incorporate beneficial components.
Growing consumer interest in the relationship between diet and health has produced an insatiable demand for
information. Among the factors fueling U.S. interest in functional foods are rapid advances in science and
technology, rising healthcare costs, an aging population, changes in food laws allowing expanded label claims, and a
focus on attaining wellness through diet.
Credible scientific research already indicates potential health benefits from food components that would expand the
benefits now permitted to be identified by the Food and Drug Administra-tion's approved health claims. This has
prompted consumer and food industry interest in functional foods internationally.

Implications of Current Scientific Knowledge

While no formal criteria have been established to classify functional foods or components, a number of academic,
scientific and regulatory organizations are considering various approaches to further define and establish the science
basis to designate functional foods or components. Food products are now regulated by FDA depending on their
intended use and the nature of claims made on the package. Of course, a large body of credible scientific research is
needed to confirm the benefits of any particular food or component.
For functional foods to realize potential public health benefits, consumers must have a clear understanding of and
strong confidence level in the scientific criteria that are likely to be established. The scientific community is in the
early stages of understanding the potential for functional foods. Until this knowledge is more complete, to gain
maximum health benefits, consumers should strive to consume a wide variety of foods.
Many existing foods and food components fit the general definition of functional foods, including the examples
below in which preliminary research suggests potential health benefits. However, these examples are not "magic
bullets" and the best advice is to eat a wide variety of foods which would incorporate many potentially beneficial
components.

Component Where It's Found Potential Benefit

Bifidobacteria yogurt, other dairy -may enhance gastrointestinal system function
-regular intake may reduce risk of cancer and lower blood
Allyl garlic
pressure and cholesterol levels
Catechin tea -may reduce risk of cancer
tomatoes, tomato sauce, red
Lycopene -high intake may reduce risk of prostate and cervical cancers
grapefruit, red peppers
Beta glucan oats -may help reduce risk of cardiovascular disease
used as bulk sugar substitutes in -may improve quality of intestinal microflora and decrease
Oligosaccharides
confections risk of tooth decay
-regular consumption may lower cholesterol in individuals
Isoflavones soy
with high cholesterol levels
wheat bran, brown rice, bananas,
Insoluble fiber -may help reduce risk of breast and colon cancers
lentils, nuts