(Journal of Complementary and Integrative Medicine) Phytonutrients As Therapeutic Agents

J Complement Integr Med.
2014; 11(3): 151–169
Review
Charu Gupta* and Dhan Prakash
Phytonutrients as therapeutic agents

Abstract: Nutrients present in various foods plays an impor- Introduction
tant role in maintaining the normal functions of the human
body. The major nutrients present in foods include carbohy- Food plays a vital role in maintaining normal function of
drates, proteins, lipids, vitamins, and minerals. Besides the human body. With recent advances in medical and
these, there are some bioactive food components known as nutritional sciences, natural products have received
“phytonutrients” that play an important role in human extensive attention as health-promoting foods from both
health. They have tremendous impact on the health care health professionals and the consumers. Bioactive foods
system and may provide medical health benefits including and nutraceuticals have emerged as potential supple-
the prevention and/or treatment of disease and various phy- ments in various diseases and preventive natural sources
siological disorders. Phytonutrients play a positive role by from food [1]. Consumers can use nutraceuticals as sup-
maintaining and modulating immune function to prevent plementation to a poor diet, to improve overall health, to
specific diseases. Being natural products, they hold a great delay the onset of age-related diseases, after illness, for
promise in clinical therapy as they possess no side effects that stress, in pregnancy and slimming, to improve sports
are usually associated with chemotherapy or radiotherapy. performance, and to treat symptoms (cold, cough, arthri-
They are also comparatively cheap and thus significantly tis, etc.). These functional also called as medicinal foods
reduce health care cost. Phytonutrients are the plant nutrients contain phytonutrients or phytomedicines that play ben-
with specific biological activities that support human health. eficial roles in maintaining well-being, enhancing health,
Some of the important bioactive phytonutrients include poly- and modulating immune function to prevent specific dis-
phenols, terpenoids, resveratrol, flavonoids, isoflavonoids, eases. “Phytonutrients” and “Phytotherapy” is a more
carotenoids, limonoids, glucosinolates, phytoestrogens, phy- recent term that refers to a science of treatment using a
tosterols, anthocyanins, ω-3 fatty acids, and probiotics. They group of natural substances that include certain herbs
play specific pharmacological effects in human health such and their derivatives for use as dietary supplements and
as anti-microbial, anti-oxidants, anti-inflammatory, anti- regulated as foods [2, 3].
allergic, anti-spasmodic, anti-cancer, anti-aging, hepatopro- As phytonutrients are of natural origin, they are use-
tective, hypolipidemic, neuroprotective, hypotensive, dia- ful in clinical therapy due to their lower side effects as
betes, osteoporosis, CNS stimulant, analgesic, protection compared to chemotherapy or radiotherapy and are
from UVB-induced carcinogenesis, immuno-modulator, and advantageous in reducing the health care cost [4].
carminative. This mini-review attempts to summarize the There are scientific evidences of their chemical and
major important types of phytonutrients and their role in biological properties, clinical information, mode of action,
promoting human health and as therapeutic agents along quality control, and effectiveness of phytonutrients in
with the current market trend and commercialization. nutritional therapy [5]. Phytonutrients play an important
Keywords: anthocyanins, carotenoids, flavonoids, gluco- role in human health as anti-oxidants, anti-bacterial, anti-
sinolates, nutraceuticals, phytoestrogens, phytonutrients, fungal, anti-inflammatory, anti-allergic, anti-spasmodic,
polyphenols, terpenoids chemo-preventive, hepatoprotective, hypolipidemic, neu-
roprotective, and hypotensive agents and help in prevent-
DOI 10.1515/jcim-2013-0021 ing aging, diabetes, osteoporosis, cancer and heart
Received June 14, 2013; accepted May 20, 2014; previously diseases, induced apoptosis, diuretic, CNS stimulant,
published online July 22, 2014 analgesic, protection from UVB-induced carcinogenesis,
immuno-modulator, and carminative [6, 7].
*Corresponding author: Charu Gupta, Amity Institute for Herbal Dietary intake of phytochemicals promotes health ben-
Research and Studies, Amity University, Noida, Uttar Pradesh, India,
efits and protects against chronic degenerative disorders,
E-mail: charumicro@gmail.com
Dhan Prakash, Amity Institute for Herbal Research and Studies, such as cancer, cardiovascular and neurodegenerative
Amity University, Noida, Uttar Pradesh, India diseases, diabetes, high blood pressure, inflammation,
Brought to you by | La Trobe University

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152 Gupta and Prakash: Bioactive compounds in health
microbial, viral and parasitic infections, psychotic diseases, property and major food sources of some of the important
spasmodic conditions, and ulcers. These phytochemicals, phytonutrients or bioactive food components like antho-
either alone and/or in combination, have tremendous ther- cyanidins, carotenoids, lycopenes, flavonoids, GLSs, iso-
apeutic potential in curing various ailments. flavonoids, limonoids, polyphenols, ω-3 fatty acids,
The important phytonutrients include carotenoids, phytoestrogens, resveratrol, phytosterols, probiotics,
tocopherols, ascorbates, lipoic acids, and polyphenols. and terpenoids. All these phytonutrients play specific
They are strong natural anti-oxidants with free radical pharmacological effects on human health as anti-inflam-
scavenging activity and are associated with a lower inci- matory, anti-allergic, anti-oxidants, anti-microbial, anti-
dence of degenerative diseases. Phytoestrogens are non- spasmodic, chemopreventive, hepatoprotective, hypolipi-
steroidal phytochemicals quite similar in structure and demic, neuroprotective, hypotensive, anti-aging, dia-
function to gonadal estrogen hormone. They offer an betes, osteoporosis, protection of DNA damage, cancer
alternative therapy for hormone replacement therapy and heart diseases, induced apoptosis, diuretic, CNS sti-
(HRT) with beneficial effects on cardiovascular system mulant, analgesic, protection from UVB-induced carcino-
and may even alleviate menopausal symptoms. genesis, immuno-modulator, and carminative [6].
Terpenoids are the largest class of phytonutrients present Phytonutrients or bioactive food components can be
in green foods and grains, and they provide a measure of added or increased to traditional foods through genetic
protection from certain diseases, especially those related engineering techniques. An example would be the high
to chronic damage and growth deregulation. Carotenoids lycopene tomato, a genetically modified tomato with
lower risk of chronic diseases like cardiovascular, certain delayed ripening characteristics that is high in lycopene
cancers, and eye. Limonoids provide substantial anti- and has potent anti-oxidant capabilities.
cancer actions; phytosterols compete with cholesterol in The present chapter would discuss about these
the intestine for uptake and aid in the elimination of potential bioactive food components that could provide
cholesterol from the body; glucosinolates (GLSs) that benefits in terms of health and well-being and the poten-
are activators of liver detoxification enzymes, provide tial role of these functional ingredients (Table 1) along
protection against carcinogenesis, mutagenesis, and with their current market trends and scenario.
other forms of toxicity. An unconventional category of
nutraceuticals of microbial origin known as probiotics
also exists. The majority of probiotic microorganisms
belong to the genera Lactobacillus and Bifidobacterium. Phytonutrients and their health
The probiotic bacteria are used for the manufacture of a benefits
natural remedy, for controlling weight gain, preventing
obesity, increasing satiety, prolonging satiation, reducing
food intake, reducing fat deposition, improving energy Polyphenols
metabolism, treating and enhancing insulin sensitivity,
and treating obesity. Major source
Although most phytonutrients currently used are
known as vital nutrients for the human body, many Polyphenols are naturally occurring compounds found
details such as dose, drug–drug interaction, nutraceuti- largely in fruits, vegetables, cereals, and beverages.
cal–drug interaction, and their effects on individuals Legumes and chocolate also contribute to the polyphe-
under certain health conditions remain elusive [8]. It is nolic intake. The major sources of dietary polyphenols
normally assumed that proper nutrient balance is are cereals, legumes (barley, corn, nuts, oats, rice, sor-
required to maintain a healthy status of the human ghum, wheat, beans, and pulses), oilseeds (rapeseed,
body, and excess intake of any nutrient may not benefit canola, flaxseed, and olive seeds), fruits, vegetables,
or even can be harmful to health. and beverages (fruit juices, tea, coffee, cocoa, beer, and
Knowledge from food chemistry, nutrition, and clin- wine) [11–13].
ical studies provides more insight into our understanding
of biological functions, usage, and potential adverse
effects of nutraceuticals [8, 9]. This advanced knowledge Amounts
helps to standardize manufacturing processes and clin-
ical practices and add more value to nutraceutical mar- Fruits such as apple, grape, pear, cherry, and various
kets [10]. The present review would focus on therapeutic berries contain up to 200–300 mg polyphenols per 100 g

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Gupta and Prakash: Bioactive compounds in health 153
Table 1 Major phytonutrients of nutraceutical importance, their sources, and health benefits [109, 110].
Phytonutrient Source plant Health benefits
Anthocyanins Blackberry, cherry, orange, purple corn, raspberry, and Anti-allergic, anti-inflammatory, anti-oxidants, and
red grapes pigments
Carotene Carrots, leafy greens and red, orange and yellow Anti-carcinogenic, enhances release of immunogenic
vegetables, and pumpkin cytokines IL-1 and TNF-α, provides cornea protection
against UV light, and stimulates DNA repair enzymes
Lycopene Apricots, papaya, pink guava, tomato, and watermelon Lowers risk of atherosclerosis and prostate cancer
Resveratrol Blueberry, peanuts, red grapes, and red wine Anti-oxidant, anti-cancer, prevents aging, diabetes, and
heart diseases
Stigmasterol Soybean Anti-cancer, hypolipidemic, and prevention of
(phytosterol) osteoporosis
GLSs Broccoli sprouts, cabbage, cauliflower, collards, Anti-oxidant, prevent DNA damage, and reduce risk of
cruciferous vegetables, kale, radish, and turnip breast and prostate cancers
Flavonoids Berries, legumes, tea, grapes, olive oil, cocoa, walnuts, Anti-bacterial, anti-oxidant, anti-viral, analgesic
peanuts, spices, fruits, and vegetables. Especially activities, inhibition of hydrolytic and oxidative
green vegetables, onion, apple, berries, and tea enzymes, anti-inflammatory, anti-viral, and anti-
proliferative
Quercetin Red onions, buckwheat, red grapes, green tea, and Strong anti-oxidant, reduces low-density lipoprotein
apple skin (LDL) oxidation, vasodilator, and blood thinner
Isoflavonoids Members of the Fabaceae (Leguminosae) family, soy Anti-oxidant, anti-proliferative, anti-cancer, and
cheese, soy flour, soy bean, and tofu prevention of osteoporosis
Limonoids Citrus juice and citrus tissues Anti-cancer, insecticidal, insect anti-feedant, and
growth regulating activity on insects, as well as anti-
bacterial, anti-fungal, anti-malarial, and anti-viral.
Polyphenols Cereals, legumes (barley, corn, nuts, oats, rice, Anti-oxidant, anti-carcinogenic, anti-inflammatory, anti-
sorghum, wheat, beans, and pulses), oilseeds neurodegenerative, anti-diabetic, anti-viral, skin photo-
(rapeseed, canola, flaxseed, and olive seeds), fruits, protective, anti-allergic, anti-platelet, anti-aging,
vegetables, and beverages (fruit juices, tea, coffee, cytoprotective, and DNA-protective properties.
cocoa, beer, and wine)
ω-3-fatty acids Fish such as salmon, rainbow trout, mackerel, herring, Osteoarthritis, lowers cholesterol, reduces high blood
and sardines. Plants – canola, soybean, and flax oils pressure, protects from heart attacks, eases joint
pains, fights wrinkles and skin ailments, and improves
memory
Phytoestrogens Soybeans, wheat, barley, corn, alfalfa, and oats Anti-cancer, heart diseases, menopausal symptoms,
and osteoporosis
Terpenoids Green foods, fruits, vegetables, and grains Anti-microbial, anti-fungal, anti-parasitic, anti-viral,
anti-allergenic, anti-spasmodic, anti-hyperglycemic,
anti-inflammatory, chemotherapeutic, and immuno-
modulatory properties
Probiotics Fermented foods – milk, curd, and cheese, fermented Anti-microbial, prevention of traveler’s diarrhea and
vegetables antibiotic-associated diarrhea, inflammatory bowel
disease, lactose intolerance, protection against
intestinal infections, irritable bowel syndrome, vaginal
infections, and immune enhancement, inactivation of
pathogens in the gut, rheumatoid arthritis, improving
the immune response, and liver cirrhosis

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fresh weights. Similarly, a glass of red wine or a cup of believed to suppress the inflammatory processes, moder-
coffee or tea contains about 100 mg polyphenols. Their ate cell signaling pathways, proliferation, apoptosis,
total dietary intake may be about 1 g per day, which is redox balance and most often appear to be protective
about 10 times higher than that of vitamin C and 100 times against cancer, neurodegenerative disorders and cardio-
higher than those of vitamin E and carotenoids [14, 15]. vascular diseases among others [17, 18]. Polyphenols are
known for their unique property of activation at multiple
levels, through the modulation of MAPK, Akt, and NF-κB
Mode of action signaling pathways, inhibiting the production of inflam-
matory cytokines and chemokines, suppressing the activ-
These molecules are secondary metabolites of plants and ity of COX and iNOS and decreasing the production of
are generally involved in defense against ultraviolet (UV) free radicals [19]. Several phytochemicals including gen-
radiation or aggression by pathogens. Basic researches istein [20], curcuminoids [17], and catechins [21] are
and epidemiological studies have shown the inverse known to suppress the activation of Akt, thus, inhibiting
association between risk of degenerative diseases and cancer cell growth. Some phenols like resveratrol, curcu-
intake of diet rich in polyphenols. The epidemiological min, and green tea catechins have been shown to sup-
studies provide convincing evidences that diet rich in press COX-2 giving the benefit of decreasing the
anti-oxidants is associated with a lower incidence of production of reactive oxygen species (ROS) [22, 23].
degenerative diseases. Polyphenols, with ~8,000 struc- Furthermore, several polyphenols suppress lipid per-
tural variants, are characterized by the presence of aro- oxidation to maintain the cellular status of anti-oxidant
matic rings bearing one or more hydroxyl moieties, which enzymes like superoxide dismutase, catalase, and glu-
have proven pivotal roles in mediating their properties tathione peroxidase [24]. Due to the NF-κB suppressing
(Figure 1) [16]. Although the knowledge of absorption, effect of polyphenols, some of them (e.g. curcumin, resver-
bioavailability, and metabolism of polyphenols is not atrol, quercetin, and green tea polyphenols) have been
entirely known, it appears that some polyphenols are shown to decrease the expression of chemokines and cyto-
bioactive and are absorbed in their native or modified kines [25]. Polyphenols present in healthy foods or drinks
form by the microflora of the intestine. The active com- are readily metabolized to phenolic acids and aldehydes
ponents of dietary phytochemicals (e.g. curcumin, resver- by the microflora of the intestine, raising the possibility
atrol, capsaicin, catechins, vitamins, and β-carotene) are that these metabolites are responsible for their anti-inflam-
matory properties [26]. A wide variety of polyphenols, most
of which are dietary supplements, have been reported to
R possess substantial skin photo-protective effects [27].
Therapeutic property
R1 R2
OH
In the recent years, there has been much awareness about
functional foods and nutraceuticals fortified with natural
R R1 R2
polyphenols and their health benefits like their potent
Protocatechuic acid COOH OH H anti-oxidant activity, anti-carcinogenic, anti-inflammatory,
anti-neurodegenerative, anti-diabetic, anti-viral, skin
Gallic acid COOH OH OH
photo-protective, anti-allergic, anti-platelet, anti-aging,
Syringic acid COOH OCH3 OCH3 cytoprotective, and DNA-protective properties [23].
Vanillic acid COOH OCH3 H
p-Coumaric acid CH = CH.COOH H H

Terpenoids
Caffeic acid CH = CH.COOH OH H
Ferulic acid CH = CH.COOH OCH3 H Major source
Chlorogenic acid CH = CH.COO-quinic acid OH H

The terpenes, also known as isoprenoids, are the largest
Figure 1 Phenolic acids: hydroxycinnamic acids. class of phytonutrients in green foods and grains. These
compounds are found in higher plants, mosses,

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liverworts, algae, and lichens, as well as in insects, Resveratrol

microbes, or marine organisms. Terpenoids are derived
from a common biosynthetic pathway based on mevalo- Resveratrol is a natural compound made by type of
nate as parent and are named terpenoids, terpenes, or plants. It is a phyto-alixin, made by plants in stress
isoprenoids with the subgroup of steroids among them as conditions and pathogen attack.
a class [28, 29]. Their importance to plants relates to their
necessity to fix carbon through photosynthetic reactions
using photosensitizing pigments. Animals have evolved Major source
to utilize these compounds for hormonal and growth
regulatory functions (vitamin A), and the presence of It is found in considerable concentrations in grapes, pea-
these molecules in animal tissues also provides a mea- nuts, and so forth. In the diet, the major source is found
sure of protection from certain diseases, especially those in red wine (Figure 2). Resveratrol is made in grape skins,
related to chronic damage and growth deregulation. but not in the flesh, thus it is found very little in white
The diverse functional roles of some of the terpenoids wine, and proportionally in rose wines with the highest
are characterized as hormones (gibberellins), photosyn- concentration in red wines. The richest natural sources of
thetic pigments (phytol and carotenoids), electron car- resveratrol are dark grape extracts (Vitis vinifera) and
riers (ubiquinone and plastoquinone), and mediators of giant knotweed (Polygonnum cuspidatum, a perennial
polysaccharide assembly, as well as communication and shrub). It is also found in abundance in labrusca and
defense mechanisms [30]. muscadine grapes. It is also present in other plants such
as Eucalyptus, spruce, and lily and in foods such as
mulberries, peanuts, blueberries, strawberries, hops,
Mode of action and their products [35, 36].
Terpenes have a unique anti-oxidant activity in their

OH
interaction with free radicals. They react with free radi-
cals by partitioning themselves into fatty membranes by
HO
virtue of their long carbon side chain. The most studied
terpene anti-oxidants are the tocotrienols and tocopher-
ols. They are found naturally in whole grains and have
effects on cancer cells. The tocotrienols are effective OH
apoptotic inducers for human breast cancer cells. The
Figure 2 Resveratrol.
impact of a diet of fruits, vegetables, and grains on
reduction of cancer risk may be explained by the actions
of terpenes in vivo [6, 13]. Amount
It also occurs in the vines, roots, seeds, and stalks, but

Therapeutic property its highest concentration is in the skin, which contains
50–100 µg/g [37].
Several biological actions have been reported for diter-
penes including anti-bacterial, anti-fungal, anti-inflamma-
tory, anti-leishmanial, cytotoxic, and anti-tumor activities Mode of action
[31]. Currently, a broad range of biological responses can
be elicited in humans through various terpenoids that are Resveratrol produces various physiological effects. At low
applicable to human health care [32]. Different terpenoid concentrations that normally occur in food, resveratrol
molecules have anti-microbial, anti-fungal, anti-parasitic, has been shown to exert neuroprotective effects [38], as
anti-viral, anti-allergenic, anti-spasmodic, anti-hyperglyce- well as beneficial effects on the cardiovascular system
mic, anti-inflammatory, chemotherapeutic, and immuno- [39]. These effects are mostly attributed to its anti-oxidant
modulatory properties [32, 33]. Terpenes are also used as properties. Resveratrol inhibits the proliferation and
skin penetration enhancers, as well as natural insecticides, induces apoptotic cell death in multiple cancers cell
and can be of use as protective substances in storing types in vitro [40, 41]; moreover, in animal models of
agriculture products [34]. cancer, resveratrol has been shown to inhibit

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angiogenesis and delay tumor growth [42], impede carci- R5

nogenesis [43], and reduce experimental metastasis [44]. R4
R6
Resveratrol acts on the process of carcinogenesis by
R O
affecting the three phases: tumor initiation, promotion, R3
and progression phases, and suppresses the final steps of

R1 R7
carcinogenesis, i.e. angiogenesis and metastasis. It is also
R2 O
able to activate apoptosis, arrest the cell cycle, or inhibit
kinase pathways.
R R1 R2 R3 R4 R5 R6 R7
Therapeutic property Kaempferol OH H OH H OH H H OH

Quercetin OH H OH H OH OH H OH
Resveratrol is trans-stilbene that undergoes isomerization Figure 3 Flavonoids.

under UV radiation. It is the “trans” form of resveratrol
that has been shown to display a much broader spectrum
are naringenin in grapefruit, hesperetin in oranges, and
of pharmacological activity than its “cis” isomer.
eriodictyol in lemons. The major sources of flavonoids
Stilbenes, in particular trans-resveratrol and its gluco-
intake are tea (61%), onions (13%), and apples (10%); the
side, are widely reported to be beneficial to health and
other sources include cherry, tomato, broccoli, black
possess anti-oxidative, anti-carcinogenic, and anti-tumor
grapes, and blueberries [45].
properties [37]. Trans-resveratrol is synthesized naturally
by several plants in response to pathogen infection, trau-
matic damage, UV irradiation, and other stresses.
Most noticeable biological activities are anti-throm-
bogenic, anti-inflammatory, cardio-protective, neuropro-
Flavonoids have been studied extensively since they have
tective, anti-aging, and cancer preventive and therapeutic
many curative effects such as anti-bacterial, anti-oxidant,
activities.
anti-viral, and analgesic activities [46]. Flavonoids form a
group of many different compounds of which more than
5,000 have been currently characterized. Flavonoids can
Flavonoids
be classified into several distinct subclasses based on
their chemical structures and exert various health-
Major source
promoting effects in human body for disease prevention.
Among the biological activities, flavonoids are active
Flavonoids are polyphenolic compounds present in ber-
against free radicals; free radical mediated cellular sig-
ries, legumes, tea, grapes, olive oil, cocoa, walnuts, pea-
naling, inflammation, allergies, platelet aggregation,
nuts, spices, fruits, and vegetables. Green vegetables,
microbes, ulcers, viruses, tumors, and hepatotoxins.
onion, apple, berries, and tea are the rich sources of
Anti-proliferative effects such as cancers, cardio vascular,
flavonoids. Flavonoids are present in most plant tissues
and inflammatory diseases of dietary flavonoids are also
and often in vacuoles [45].
well recognized. Scavenging activity of hydroxyl radicals,
superoxide anion radicals, and lipid peroxy radicals sig-
nifies the health-promoting functions of flavonoids [47].
Amount
Flavonols are the most ubiquitous flavonoids in the

foods. Quercetin and kaempfreol are the main represen- Mode of action
tatives of this group (Figure 3). They are generally present
at relatively low concentrations of about 15–30 mg/kg Flavonoids are a subclass of plant phenols which include
fresh weight. Onions, curly kale, leeks, broccoli, and the minor flavonoids (flavanones and dihydroflavonols),
blueberries are the rich sources of flavonols. Flavanones flavones, and flavonols (Table 2). Proposed mechanisms
are found in tomatoes and certain aromatic plants such by which they provide health benefits, in addition to being
as mint (Mentha piperita), but they are present in high direct chemical protectants involve modulatory effects on
concentrations only in citrus fruits. The main flavanones a variety of metabolic and signaling enzymes. Flavonoids

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Table 2 Dietary sources of polyphenols [109, 110].
Classes/subclasses Polyphenols Sources
Anthocyanidins Cyanidin 3-glycosides Black berries, black currant, black grape, blue berries,
Flavonoids Delphinidin cherries, cranberry, plums, pomegranate, raspberry, red
Malvidin wine, strawberries
Pelargonidin
Anthoxanthins Fisetin Apples, apricots, beans, berries, black currant, broccoli,
Flavonols Isorhamnetin buckwheat, celery
Kaempferol Cherries, cherry tomatoes, chives, cocoa, grapes, kale,
Myricetin lettuce, onions
Quercetin Peppers, plums, red wine, spinach
Sweet potato, tea
Flavanones Hesperetin Citrus fruits and their juices
Naringenin Grapes, tangerine juice
Eriodictyol
Flavones Apigenin Celery, fresh parsley, olives, oregano
Luteolin Peppers, rosemary
Flavanols Epicatechin and their gallates, Morin Apples, apricots, berries, cherries
(Flavan-3-ols) Procyanidins Chocolate, grapes, peaches, pears, plums, raisins, red
Prodelphinidins, Catechin wine, tea
Isoflavones Daidzein Grape seeds/skin, soy cheese and sauces, soy products,
(Flavans) Equol, Genistein soybean
Flavonoid glycoside Hesperidin Grape fruit, lemon, orange juice
Naringin, Rutin Orange, tangerine juice
Phenolic acids Caffeic acid Apple, apple juice, blueberry, cider, cranberry, grape fruit,
Chlorogenic acid lemon, lettuce, coffee beans, orange, peach, pear, cherry,
Ferulic acid potato, spinach, tea
p-Coumaric acid
Hydroxy-benzoic acids Ellagic and Gallic acids Grape juice, pomegranate juice
Raspberry grape juice, longan seed, strawberry
Trihydroxy-stilbenes Resveratrol Grapes, peanuts, red wine
Tannins Catechin Apple juice, blackberry, chick pea
Epicatechin polymers, Ellagitannins Cocoa, coffee, grape seeds and skin
Proanthocyanidins Lentils, olive, peach, peas, plum
Tannic acids Pomegranate, raspberries, red wine
Strawberries, tea, walnuts
Diferuloylmethane Curcumin Turmeric
have been shown to block the angiotensin converting Flavonoids in regularly consumed foods appeared to
enzyme that raises blood pressure; inhibit cyclooxygenase reduce the risk of death from coronary heart disease; but
which forms prostaglandins; and block enzymes that pro- some flavonoids have been reported to be mutagenic as
duce estrogen. The implications of these in vitro inhibitory well [49]. The capacity of flavonoids to act as anti-oxidants
actions are that certain flavonoids prevent platelet aggre- depends upon their molecular structure. The position of
gation, reduce heart disease and thrombosis, and inhibit hydroxyl groups and other features in the chemical struc-
estrogen synthase which binds estrogen to receptors in ture of flavonoids are important for their anti-oxidant and
several tissues, thus decreasing the risk of estrogen-related free radical scavenging activities. Quercetin, the most
cancers. Bioactive properties such as free radical scaven- abundant dietary flavonol, is a potent anti-oxidant
ging, inhibition of hydrolytic and oxidative enzymes, anti- because it has all the right structural features for free
inflammatory and anti-viral [48] action of flavonoids are radical scavenging activity [47]. Luteolin has anti-inflam-
well known. There is inverse association between flavo- matory, anti-mutagenic, and anti-bacterial activities.
noids intake and coronary heart disease mortality. Research has proved that apigenin suppressed

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12-O-tetradecanoylphorbol-3-acetate (TPA)-mediated R2
tumor promotion of mouse skin, similar to curcumin, a R1 O
dietary pigmented polyphenol, possibly through suppres-
sion of protein kinase C activity and nuclear oncogene
expression. Apigenin is anti-bacterial, anti-inflammatory,
diuretic, and hypotensive and also promotes smooth mus- HO
O
cle relaxation. Myricetin, a hexahydroxyflavone, exhibits
anti-bacterial activity and has anti-gonadotropic activity,
but apparently is not a mutagen. The flavonol kaempferol,
which is widely found in the diet, has anti-inflammatory R1 = OH, R2 = OH (Genistein)
R1 = H, R2 = OH (Daidzein)
and anti-bacterial activities and is directly mutagenic.
R1 = OH, R2 = OMe (Biochanin A)
Quercetin, the most common flavonoid in higher plants,
R1 = H, R2 = OMe (Formononetin)
seems to contribute to the mutagenicity of kaempferol in
the presence of microsomal metabolizing systems.
Figure 4 Isoflavones (phytoestrogen).
Quercetin inhibits a number of enzymes, smooth muscle
contraction, and proliferation of rat lymphocytes.
Although it is anti-inflammatory, anti-bacterial, anti-viral, an activity of a number of phytochemicals termed phy-
and anti-hepatotoxic, it exhibits mutagenic activity and toestrogens. Genistein inhibits the growth of most hor-
allergenic properties [50]. Catechins and gallic acids, mone-dependent and -independent cancer cells in vitro,
major sources of catechins are grapes, berries, cocoa, including colonic cancer cells. Isoflavones have received
and green tea. Tea contains considerable amounts of gallic considerable attention as potentially preventing and
acid esters, such as epicatechin, epicatechingallate and treating cancer and osteoporosis [52]. Research in mice
epigallocatechingallate. Numerous studies have suggested has shown that dietary soybean components inhibited
that these components provide protective benefits by their the growth of experimental prostate cancer and altered
free radical scavenging ability and their inhibition of eico- tumor biomarkers associated with angiogenesis.
sanoid synthesis and platelet aggregation. The green tea Although the epidemiological data suggest that soy
provides protection against prostate cancer [51]. Wines potentially decreases the risk of breast and prostate can-
contain catechins and procyanidins that are responsible cer but the evidence that soy exerts a protective effect
for its astringency sensation. Catechin is one of the major against colonic cancer is limited.
phenolics in grapes and red wines and is considered to be
partly responsible for the protective effect against athero-
sclerotic cardiovascular disease. Mode of action
Anti-oxidant and anti-proliferative properties of isoflavones

Isoflavonoids offer important mechanisms for their protection against
many prevalent chronic diseases [53, 54]. Cellular damage
Major sources resulting from oxidative stress is believed to be a major
contributor to the etiology of cardiovascular disease
They are another subclass of the phenolic phytonutrients. through the oxidation of LDL and cancer by causing DNA
Isoflavonoids are produced almost exclusively by the strand breaks which may lead to mutations [55, 56]. Recent
members of the Fabaceae (Leguminosae) family. Their research has shown that the isoflavone genistein from soy,
main food sources are soy cheese, soy flour, soy bean, selectively bound to the β-estrogen receptor and reduced
and tofu. Soybeans are an unusually concentrated source binding to the α-receptor 20-fold.
of isoflavones, including genistein and daidzein (Figure 4),
and soy is the major source of dietary isoflavones.
Carotenoids
Therapeutic property Major sources
The isoflavones of soy have a property of binding to the The group of carotenoids consists of more than 700 phy-
estrogen receptor class of compounds, thus representing tochemicals, which constitute photosynthetic membranes

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H3C
CH3 CH3
H3C CH3
H3C CH3
CH3 CH3 CH3
Figure 5 β-Carotene.
and produce colors in plants and animals. Out of 700 Therapeutic property
pigments, only about 24 commonly occur in human food-
stuffs [57]. The most studied carotenoids are α-carotene, The β-carotene and lycopene have been shown to be
β-carotene, lycopene, lutein, and zeaxanthin (Figure 5). inversely related to the risk of cardiovascular diseases
The principal carotenoids of foods are β-carotene, β-cryp- and certain cancers, whereas lutein and zeaxanthin are
toxanthin, lycopene, and lutein. Carotenoid pigments are related with the prevention of eye disorders [60, 62].
abundant in many fruits and vegetables and have been Lutein protects against uterine, prostate, breast, color-
studied for their diverse roles in phytochemistry and ectal, and lung cancers. They also protect against risk
phytomedicine [57]. of digestive tract cancer. Xanthophyll, a type of carote-
Carotenoids are mainly C40 isoprenoids, consisting noids, offers protection to other anti-oxidants and exhibit
of eight isoprene units. There are two main groups of tissue specific protection. Zeaxanthin, cryptoxanthin, and
carotenoids (i) carotenes (β-carotene, lycopene) contain astaxanthin are all the members of xanthophyll group
only hydrogen and carbon and may be cyclic or linear; [63, 64].
(ii) oxycarotenoids (xanthophylls, lutein) contain hydro-
gen, carbon, and oxygen in the form of hydroxy, epoxy,
and oxy groups, respectively. The polyene chain in car- Mode of action
otenoids contains upto 15 conjugated double bonds,
which are responsible for their characteristic absorption The anti-oxidant properties of carotenoids have been sug-
spectra and specific photochemical properties [58]. They gested to be the main mechanism by which they afford their
are responsible for quenching singlet oxygen and for beneficial effects. Research has shown that carotenoids med-
intercepting deleterious free radicals and ROS. These iate their effects through other mechanisms such as gap
properties make them a part in diverse anti-oxidant junction communication, cell growth regulation, modulat-
defense system. Most carotenoids are found in linear or ing gene expression, immune response, and modulators of
all trans-configuration. However on exposure to light or Phase I and II drug metabolizing enzymes [65, 66].
heat facilitates their inter-conversion from “trans” to “cis”
isomerization of one or more double bonds [59].
The physico-chemical properties and the biological activ- Lycopene
ities of carotenoids are intimately related to their chemi-
cal structures. Epidemiological studies have shown a Major source
positive link between higher dietary intake and tissue
concentrations of carotenoids with lower risk of chronic Lycopene, a carotenoid without provitamin-A activity, is
diseases [60, 61]. present in many fruits and vegetables (Figure 6);
H3C OH
CH3 CH3
H3C CH3
H3C CH3
HO CH3 CH3 CH3
Figure 6 Lycopene.

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however, tomatoes and processed tomato products con- Limonoids

stitute the major source of lycopene in diet. Among the
carotenoids, lycopene is a major component found in the Major sources
serum and other tissues.
These are terpenes present in citrus fruit. Citrus limo-
noids are present in large amounts in citrus juice and
Therapeutic property citrus tissues as water-soluble limonoid glucosides or in
seeds as water-insoluble limonoid aglycones [72].
Dietary intakes of tomatoes and tomato products contain-
ing lycopene have been shown to be associated with
decreased risk of chronic diseases such as cancer and Therapeutic property
cardiovascular diseases. Serum and tissue lycopene
levels have also been inversely related with the chronic Limonoids are highly oxygenated triterpenoid com-
disease risk. Although the anti-oxidant properties of lyco- pounds with significant biological activity.
pene are primarily responsible for its beneficial proper-
ties, other mechanisms such as modulation of
intercellular gap junction communication, hormonal Mode of action
and immune system, and metabolic pathways are also
involved [67]. Several citrus limonoids are studied for their role as anti-
cancer utilizing laboratory animals and human breast
cancer cell cultures. In mice, it was found that five limo-
Mode of action noid aglycones (limonin, nomilin, obacunone, iso-obacu-
noic acid, and ichangin) induced significant amounts of
Lycopene also has the ability to destroy free radicals that glutathione-S-transferase (GST) in the liver and intestinal
are produced as a result of metabolic reactions in the mucosa [73]. GST is a major detoxifying enzyme system
body. It suppresses the attack of cellular oxygen and that catalyzes the conjugation of glutathione with many
ROS thereby slowing down the formation of free radicals potentially carcinogenic compounds which are highly
and therefore prevents destruction of the lipophilic parts electrophilic in nature. A study of the inhibitory effects
of the cell [68]. of two limonoid aglycones (limonin and nomilin) on the
A study assessing the acute effects of lycopene on formation of benzo[a]pyrene induced neoplasia in the
airway hyper-responsiveness was carried out in patients fore stomach of ICR/Ha mice showed that incidence of
with exercise-induced asthma (EIA). The results showed tumors could be reduced by more than 50% at 10 mg/
that 55% of those taking lycopene were significantly dose [74]. The experimental results described above indi-
protected against EIA and did not experience this inhaled cate that citrus limonoids may provide substantial anti-
steroid dose FEV1 reduction [69]. The anti-oxidant capa- cancer actions. The compounds have been shown to be
city of lycopene offers protection against γ-radiation free of toxic effects in animal models so limonoids has a
induced damage to cells [70]. potential against human cancer in either the natural
A study by Gitenay et al. [71] showed that even yellow fruit or in citrus fruits fortified with limonoids, or in
varieties of tomatoes that are without lycopene showed a purified forms of specific limonoids. They provide che-
stronger anti-oxidant effect in rats. Rats with mild oxida- motherapeutic activity by inhibiting Phase I enzymes and
tive stress, caused by low vitamin E level, were fed with inducing Phase II detoxification enzymes in the liver.
placebo, yellow tomato extract, red tomato extract, and D-Limonene, a common monocyclic monoterpene,
lycopene. All diets had no effect on plasma cholesterol found within orange peel oil, inhibits pancreatic carcino-
but only the red tomato diet reduced triglycerides. Rats genesis induced in experimental models and also pro-
fed with yellow or red tomato extract showed lower levels vides protection to lung tissue [63, 64]. Although the
of thiobarbituric reactive species in the heart than those initial studies are very promising, they have been con-
fed with placebo or lycopene. This led the researchers to ducted primarily with in vitro cell culture and animal
conclude that tomatoes, containing lycopene or not, have models. Thus, more research is needed to determine
a higher potential than lycopene alone to attenuate whether limonoids may be useful in preventing or treat-
oxidative stress parameters in a mild oxidative stress ing cancer in humans. The first step is to assess the
context [71]. bioavailability of the compounds for humans, their

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absorption after ingestion, and appearance in the blood Phytosterols compete with cholesterol in the intestine for
and tissues. If limonoid compounds are found to be uptake and aid in the elimination of cholesterol from the
bioavailable, then more human studies are needed to body. Plant sterols are initially solubilized into a micelle
assess the effects of limonoid ingestion on biomarkers form in the intestine. These micelles interact with brush
related to cancer [64]. border cells and are transferred into enterocytes. Plant ster-
ols are esterified within the enterocyte, assembled into
chylomicrons, and secreted into the lymphatics. They are
Phytosterols
excreted through the biliary system. The non-esterified phy-
tosterols are transported back into the intestinal lumen by
Major source
sterolin (1 and 2) pumps containing the ATP binding cas-
sette (ABC) proteins encoded by the genes ABCG5 and
These are another important terpene subclass. The primary
ABCG8. These are expressed in the mucosal cells and the
sources of phytosterols are vegetables, nuts, fruits, and seeds.
canalicular membrane, and they re-secrete sterols, espe-
cially absorbed plant sterols, back into the intestinal
Amount lumen and from the liver into bile [76]. Saturated phytoster-
ols appear to be more effective than unsaturated com-
Seeds contain an average of 120 mg of plant sterols/100 g pounds in decreasing cholesterol concentrations in the
wet weight; vegetables contain 20 mg/100 g of wet body. Their actions reduce serum or plasma total choles-
weight and fruit about 15 mg/100 g wet weight. terol and LDL cholesterol. There is a competition between
Sitosterol, campesterol, and stigmasterol are most abun- phytosterol and cholesterol for absorption from the intes-
dant in nature comprising 65%, 30%, and 3% of dietary tine due to their structural similarity. In mammals, concen-
phytosterol intake (Figure 7) [75]. trations of plasma phytosterol are low because of their poor
absorption from the intestine, their faster excretion from
liver and metabolism to bile acids, compared with choles-
terol [77]. Animal studies have shown that phytosterols
reduce atherosclerosis in the Apo-E deficient mouse
model. Mixed results were obtained from the human studies
HO and these studies do not prove or disprove an increase in
HO atherosclerotic risk that can be clearly related to serum
Brassicasterol Campesterol
phytosterol levels. Studies have proved that vegetarians
who consume considerable plant sterols are at decreased
risk of arteriosclerosis cardiovascular disease [75].
HO HO
Phytoestrogens
Sitosterol Stigmasterol
Major source
Figure 7 Phytosterols.
Phytoestrogens are non-steroidal compounds produced

by plants and present in many natural dietary products,
such as soybeans, wheat, barley, corn, alfalfa, and oats.
They occur in either plants or their seeds. There are
The two sterol molecules synthesized by plants are
several classes of phytoestrogens: steroidal estrogens,
β-sitosterol and its glycoside. In animals, these two mole-
found in few plants and the more ubiquitous are phenolic
cules exhibit anti-inflammatory, anti-neoplastic, anti-
estrogens, isoﬂavones, stilbenes, coumestans, and lig-
pyretic, and immuno-modulating activity.
nans. Soybean is rich in isoflavones, whereas the soy
sprout is a potent source of coumestrol, the major coume-
Mode of action stan. The precursors of these substances are widespread
in the plant kingdom, but mainly found in Leguminosae
Phytosterols block inflammatory enzymes by modifying the and are especially abundant in soybean and its products,
prostaglandin pathways in a way that protect platelets. legumes, berries, whole grains, and cereals [7].

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The main dietary sources of coumestans are sprouted Secoisolariciresinol and matairesinol are two lignan
legumes such as soy and alfalfa; however, low levels dimers which are not estrogenic by themselves, but read-
have been reported in brussel sprouts and spinach. ily convert to the mammalian lignans, enterodiol and
Clover and soybean sprouts are reported to have its high- enterolactone, respectively, which are estrogenic. These
est concentrations. The phytolignans are found in high are of great interest because of their estrogenic, anti-
amounts in flaxseed, asparagus, whole grains, vegeta- carcinogenic, anti-viral, anti-fungal, and anti-oxidant
bles, and tea. Fruits also have their low levels with the activities [83].
exception of strawberries and cranberries [7]. In humans, gut microflora enzymatically metabolizes
the isoflavones and lignans, and the mammalian lignans
are readily absorbed [84]. The different activities and the
Mode of action bioavailability of phytoestrogens vary depending on fac-
tors such as the form of administration, dosage, individual
These are non-steroidal phytochemicals quite similar in metabolism, and the ingestion of other pharmacological
structure and function to gonadal estrogen hormone. substances [85].
They offer an attractive alternate for HRT with beneficial
effects on cardiovascular system and may even alleviate
menopausal symptoms. They are potential alternatives to Glucosinolates
the synthetic selective estrogen receptor modulators,
which are currently applied in HRT. They have anti-oxi- Major sources
dant effects due to their polyphenolic nature, anti-carcino-
genic, modulation of steroid metabolism or of GLSs are exclusively found in dicotyledonous plants,
detoxification enzymes, interference with calcium-trans- genus Brassica alone contains more than 350 genera
port, and favorable effects on lipid and lipoprotein profiles and 3,000 species [86]. Crucifers contain very high con-
[7, 78]. On the basis of chemical structure phytoestrogens centration of GLSs. Many commonly consumed vegeta-
can be classified as isoflavones, flavones, coumestans, bles, condiments, forages and oil containing plants, such
stilbenes lignans, and coumestans (Figure 4). as cabbage, broccoli, cauliflower, collards, kale, mustard,
brussels sprouts, and rapeseeds are good sources of GLSs
[87]. These vegetables are an excellent dietary source of
Therapeutic property phytochemicals including GLSs and its breakdown pro-
ducts, phenolics and other anti-oxidants like vitamins C
Flavonoids have similar structure to estrogen, have the and K, as well as dietary essential minerals [88].
capacity to exert both estrogenic and anti-estrogenic
effects, and provide possible protection against bone
loss and heart diseases. They share structural features Therapeutic property
with estrogen, in the sense that the presence of particular
hydroxyl groups can be positioned in a stereo chemical They are present in cruciferous vegetables and are activa-
alignment virtually identical to one of the estrogens. tors of liver detoxification enzymes. These chemicals are
Populations in China, Japan, Taiwan, and Korea are esti- responsible for the pungent aroma and bitter flavor of
mated to consume high quantities of isoflavones, and cruciferous vegetables. Consumption of cruciferous vege-
women of these countries complain fewer incidences of tables provides protection against carcinogenesis, muta-
osteoporosis and related health problems, especially hot genesis, and other forms of toxicity of electrophiles and
flushes and cardiovascular diseases and lower incidence reactive forms of oxygen. The sprouts of certain crucifers,
of hormone-dependent breast and uterine cancers including broccoli and cauliflower, contain higher
[79–81]. The main dietary source of phytoestrogenic stil- amounts of glucoraphanin (the GLS of sulforaphane)
benes is resveratrol from red wine and peanuts. Although than do the corresponding mature plants. Crucifer sprouts
there are two isomers of resveratrol, “cis” and “trans”, may protect against the risk of cancer more effectively than
but only the “trans” form has been reported to be estro- the same quantity of mature vegetables of the same variety
genic. It is found only in the skin of red grapes and green [89, 90]. During food preparation, chewing, and digestion,
grapes whereas white wine contains very low levels of GLSs in cruciferous vegetables are broken down to form
trans-resveratrol [82]. The term lignan is used for a biologically active compounds such as indoles, nitriles,
diverse class of phenylpropanoid dimers and oligomers. thiocyanates, and isothiocyanates [91]. Indole-3-carbinol

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(an indole) and sulforaphane (an isothiocyanate) have recognized that ω-3 fatty acids are essential in the diet and
been scientifically proved for their anti-cancer effects. established an estimated adequate intake for them [94].
Epidemiological studies indicate that consumption of bras-
sica vegetables is associated with a reduced incidence of
cancers at a number of sites including the lung, stomach, Major source
colon, and rectum due to the presence of a predominating
thioglucosides GLSs, [92] (Figure 8). The main food sources of the long-chain ω-3 fatty acids
are fish, especially fatty species such as salmon, rainbow
trout, mackerel, herring, and sardines. Plants like canola,
S b-D-glucose
soybean, and flax oils provide the 18-carbon ω-3 fatty
R C
acid, α-linolenic acid (Figure 9). However, higher plants
N OSO3-
lack the enzymes to make 20- and 22-carbon polyunsatu-
Figure 8 General structure of GLS.
rated fatty acids (PUFAs) needed by mammals. Humans
can convert α-linolenic acid to the more biologically
active long-chain form but not so efficiently. Thus, plant
Mode of action foods with α-linolenic acid may be insufficient to supply
the need for long-chain ω-3 fatty acids, especially during
Dietary GLSs block the formation of endogenous or exo- pregnancy and lactation [95].
genous carcinogens that prevent the initiation of carcino-
genesis [93]. The mechanism of protective effect is due to
the modulation of carcinogen metabolism by the induc- Therapeutic property
tion of Phase II detoxification enzymes and inhibition of
Phase I carcinogen-activating enzymes, thereby influen- The benefit of ω-3 fatty acids is well known in the treat-
cing several processes related to chemical carcinogenesis, ment of people suffering from osteoarthritis. Clinical stu-
e.g. the metabolism, DNA binding, and mutagenic activ- dies have proved the value of ω-3 fatty acids in treating
ity of promutagens. Studies in experimental animals inflammatory conditions ranging from atherosclerosis to
including humans have proved a reducing effect on osteoarthritis. People suffering from osteoarthritis can
tumor formation and positive effect on health on con- improve symptoms and even allow a reduction in the
sumption of adequate amounts of indoles in brassica use of NSAIDs on increasing their dietary intake of ω-3
vegetables. Indole-3-carbinol is a GLS metabolite that fatty acids and monounsaturated fatty acids as found in
inhibits organ-site carcinogenesis in rodent models. Its olive oil [96]. These fatty acids have other positive effects
preventive effect on human mammary carcinogenesis is like influencing cellular metabolic functions, supporting
due to its ability to regulate cell cycle progression, cell membrane structure, and reducing the expression of
increase the formation of anti-proliferative estradiol pro-inflammatory cytokines [97]. The most potent of the
metabolite, and induce cellular apoptosis [89, 90]. ω-3 fatty acids containing oils are eicosapentaenoic acid
(EPA) and docosahexaenoic acid, which are found in
abundance in cold-water fish [98].
ω-3 fatty acids Western diets contain predominately ω-6 PUFAs
found in soybean, corn, sunflower, canola, and cotton-
There is an extensive interest in increasing consumption of ω- seed oils. It is now recognized that diets high in ω-6 fatty
3 fatty acids, because they are associated with many health acids and low in ω-3 fatty acids may exacerbate several
benefits, but are consumed only in small amounts. In 2002, chronic diseases [99]. One strategy to increase the avail-
the National Academy of Sciences Institute of Medicine ability of long-chain ω-3 fatty acids is to develop oilseed
a 15 12 9 1 O
C
OH
1 O
12 9 C
b OH
Figure 9 (a) α-Linolenic acid and (b) structure linoleic acid.

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crops such as canola and soybean that contain stearido- Anthocyanins are secondary metabolites and are also
nic acid (18:4n-3). This ω-3 fatty acid occurs naturally in approved for use as a food additive in the European
only a few plants such as black currant seed oil and Union, Australia, and New Zealand. The main anthocya-
echium. Stearidonic acid is the first product formed nin compounds are pelargonidin, cyaniding, and delphi-
when α-linolenic acid is converted to EPA, a desirable nidin. Cyanidin and its glycosides are naturally dietary
long-chain ω-3 fatty acid. pigments which have been found with promising poten-
tial benefits to humans, especially in the prevention and
treatment of diabetes mellitus [104, 105].
Anthocyanins
Major source Probiotics – the unconventional source of

bioactive food components
Anthocyanins occur in all tissues of higher plants, includ-
ing leaves, stems, roots, flowers, and fruits. The probiotics are the unconventional source of bioactive
Anthocyanins are derivatives of anthocyanidins, which food components. The combination of probiotics and
include pendant sugars (Figure 10). Plants rich in antho- prebiotics commonly known as synbiotics modifies the
cyanins are Vaccinium species, such as blueberry, cran- composition of the GI microbiota, restores the microbial
berry, blackberry, cherry, and red cabbage. The highest balance, and therefore has the potential to provide health
recorded amount appears to be especially in the seed benefits [106, 107].
coat of black soybean [100].
R5 Major source
R6 R4
The majority of probiotic microorganisms belonging to the
+
R O genera Lactobacillus and Bifidobacterium are present in
R3
abundance in fermented dairy products like yoghurt, fer-
R1 R7 mented milk, and butter-milk. Both Lactobacillus and
R2 Bifidobacterium are Gram-positive lactic acid-producing
bacteria that constitute a major part of the normal intest-
inal microflora in animals and humans [108]. The number
R R1 R2 R3 R4 R5 R6 R7 of Bifidobacteria in the colon of adults is 1010–1011 CFU/g,
Pelargonidin OH H OH H OH H H OH but this number decreases with age. Bifidobacteria are non-
Cyanidin OH H OH OH OH H H OH motile, non-spore forming, Gram-positive rods with varying
Delphinidin OH H OH OH OH OH H OH cell morphology. Most strains are strictly anaerobic.
Prebiotics and lactic acid bacteria (LAB) (probiotics)
Figure 10 Anthocyanins.
have demonstrated beneficial effects with respect to the
function of innate immunity, intestinal barrier function,
and increased resistance to disease. The gut mucosa and
Therapeutic property microbiota are intimately linked in the maintenance of a
functional interface between the host and the external
Anthocyanins are the largest group of water-soluble pig- environment [109, 110]. A combined supply of prebiotics
ments in the plant kingdom. They have potential health and probiotics (synbiotics) has synergistic effects in enhan-
benefits and disease prevention properties and are cing immunity and facilitating intestinal barrier function.
known as potential anti-oxidants [101]. Consumption of
anthocyanin-enriched foods is associated with a reduced
risk of several diseases such as atherosclerosis [102], Therapeutic property
dyslipidemia [103], and diabetes [104]. Anthocyanins
may appear red, purple, or blue depending on the pH. The probiotic bacteria are used for the manufacture of a
They are synthesized through the phenylpropanoid path- natural remedy, for controlling weight gain, preventing
way; they are odorless and nearly flavorless, contributing obesity, increasing satiety, prolonging satiation, reducing
to taste as a moderately astringent sensation. food intake, reducing fat deposition, improving energy

Authenticated
metabolism, treating and enhancing insulin sensitivity, represent annual global sales of US$75 billion in 2007. It
and treating obesity. Animal studies have demonstrated is reported that the Global Nutraceutical market would
the efficacy of some strains of LAB to lower serum cho- grow at a CAGR of 6.30% over the period of 2013–2018.
lesterol levels, presumably by breaking down bile in the One of the key factors contributing to this market growth
gut, thus inhibiting its re-absorption [111]. is the increasing global aging population. The Global
Lactobacillus (Lb. sporogenes and Lb. acidophilus Nutraceutical market has also been witnessing the
NCFB 1748) and Bifidobacterium genus representatives increase in the nutraceutical product development.
have been reported to play a critical role in weight reg- However, the threats of ingredients and raw material
ulation as an anti-obesity effect in experimental models contamination could pose a challenge to the growth of
and humans [112]. Lactobacillus sporogenes has the abil- this market [117].
ity to lower cholesterol levels. It produces a significant The predicted annual growth rates of various nutra-
reduction in LDL levels and a small but significant ceutical categories have been estimated to range from 6%
increase in high-density lipoprotein cholesterol. for products treating digestive ailments up to 25% for eye
Lactobacillus acidophilus ferments lactose into lactic health products.
acid, like many LAB. During digestion, L. acidophilus Current and predicted sales claim that the joint
assists in the production of niacin, folic acid, and pyri- health supplements like glucosamine, chondroitin, and
doxine. It also helps in bile de-conjugation, separating MSM appear to be the major product group, followed by
amino acids from bile acids, which can then be recycled the PUFAs. However, fish oils and MSM have been pre-
by the body [113]. L. acidophilus may provide additional dicted to show the greatest increase in sales [118]. The
health benefits, including improved gastrointestinal func- contemporary use of soy, for example, is not simply a
tion, a boosted immune system, and a decrease in the matter of geographical habitat or cultural lifestyle. The
frequency of vaginal yeast infections and relief from indi- availability of specific foods and nutraceuticals refined
gestion and diarrhea [114]. In addition, probiotics, pre- from soy allows all consumers to derive the proposed
biotics, and synbiotics are frequently recommended after benefits. This also applies to green tea, fish oils, flaxseed,
a course of antibiotics as a means of restoring the micro- and others. However, a more active approach has to be
biota within the intestinal tract to its normal, healthy taken with those only normally available in formulated
state, as well as an aid in resolving uncomplicated dosages such as glucosamine, chondroitin, and MSM, for
cases of diarrhea. Synbiotics are also being investigated example.
as aids in treating some non-gastrointestinal diseases. Nutraceutical manufacturers are extolling the virtues
There is some evidence that synbiotics may be useful in of controlled release formulations for release of precise
treating some skin ailments, such as atopy. levels of active entities over a particular time period, in
order to achieve maximum therapeutic effects. An exam-
ple of the use of this technology is the Novasoy soya
Mode of action isoflavone range [119].
Intake of probiotics, prebiotics, and synbiotics has been

demonstrated to modify the composition of the GI micro-
biota, restore the microbial balance, and therefore, have the
Conclusions
potential to provide health benefits. However, only recently,
The present paper thus provides a comprehensive insight
well-designed clinical studies have provided clear evidence
into some of the major phytonutrients of therapeutic
of health-promoting effects, such as prevention of antibiotic-
importance, their human health benefits, and their pos-
associated diarrhea, treatment of acute diarrhea, inflamma-
sible use as health supplements and nutraceuticals.
tory bowel disease, eradication of Clostridium difficile infec-
Dietary intake of phytochemicals promotes health bene-
tion, and enhancement of intestinal immunity [115, 116].
fits by protecting against chronic degenerative disorders,
such as cancer, cardiovascular, and neurodegenerative
diseases. These phytochemicals, either alone and/or in
Market trend of phytonutrients combination, have tremendous therapeutic potential in
curing various ailments. Phytochemicals with nutraceuti-
The markets for phytonutrients in the form of nutraceu- cal properties present in food are of enormous signifi-
ticals and functional foods are rapidly expanding. They cance due to their beneficial effects on human health

Authenticated
since they offer protection against numerous diseases or 6. Prakash D, Gupta KR. The antioxidant phytochemicals of
disorders such as cancers, coronary heart disease, dia- nutraceutical importance. The Open Nutraceuticals J
2009;2:20–35.
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conditions, and ulcers. Thus phytonutrients can be reg- 8. Whitman M. Understanding the perceived need for
ularly taken without any side effects. The future of nutra- complementary and alternative nutraceuticals: lifestyle
ceuticals from both plant (phytonutrients) and animal issues. Clin J Oncol Nurs 2001;5:190–4.
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origin holds exciting opportunities for the food industry
10. Gidley MJ. Naturally functional foods-challenges and
to create novel food products containing bioactive food
opportunities. Asia Pac J Clin Nutr 2004;13:31.
components. The government should persuade the food 11. Cieslik E, Greda A, Adamus W. Contents of polyphenols in
industry by investing more in the nutraceuticals and fruits and vegetables. Food Chem 2006;94:135–42.
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However, the products should be designed and formu- 70 medicinal plant extracts for antioxidant capacity and total
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Acknowledgments: Authors are grateful to Dr Ashok K. supplements and nutraceuticals. USA: Humana Press,
Chauhan, Chairman and Founder President and Mr Atul Springer, 2011:163–88.
Chauhan, Chancellor, Amity University-UP, Noida- 14. Packer L, Weber SU. The role of vitamin E in the
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16. Leiro J, Alvarez E, Arranz JA, Laguna R, Uriarte E, Orallo F.
Conflict of interest statement
Effects of cis-resveratrol on inflammatory murine macro-
phages: antioxidant activity and down regulation of
Authors’ conflict of interest disclosure: The authors sta-
inflammatory genes. J Leukoc Biol 2004;75:1156–65.
ted that there are no conflicts of interest regarding the
17. Aggarwal BB, Shishodia S. Molecular targets of dietary agents
publication of this article. Research support played no for prevention and therapy of cancer. Biochem Pharmacol
role in the study design; in the collection, analysis, and 2006;71:1397–421.
interpretation of data; in the writing of the report; or in 18. Rahman I, Biswas SK, Kirkham PA. Regulation of
the decision to submit the report for publication. inflammation and redox signaling by dietary polyphenols.
Biochem Pharmacol 2006;72:1439–52.
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J Complement Integr Med.

2014; 11(3): 151–169

Charu Gupta* and Dhan Prakash

Phytonutrients as therapeutic agents

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Phytonutrient Source plant Health benefits

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p-Coumaric acid CH = CH.COOH H H

Ferulic acid CH = CH.COOH OCH3 H Major source

Chlorogenic acid CH = CH.COO-quinic acid OH H

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liverworts, algae, and lichens, as well as in insects, Resveratrol

Terpenes have a unique anti-oxidant activity in their

It also occurs in the vines, roots, seeds, and stalks, but

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angiogenesis and delay tumor growth [42], impede carci- R5

and progression phases, and suppresses the final steps of

Therapeutic property Kaempferol OH H OH H OH H H OH

Resveratrol is trans-stilbene that undergoes isomerization Figure 3 Flavonoids.

Flavonols are the most ubiquitous flavonoids in the

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Table 2 Dietary sources of polyphenols [109, 110].

Classes/subclasses Polyphenols Sources

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Anti-oxidant and anti-proliferative properties of isoflavones

Therapeutic property Major sources

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however, tomatoes and processed tomato products con- Limonoids

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Phytoestrogens are non-steroidal compounds produced

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Figure 9 (a) α-Linolenic acid and (b) structure linoleic acid.

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Major source Probiotics – the unconventional source of

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Intake of probiotics, prebiotics, and synbiotics has been

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