ArticlePDF AvailableLiterature Review

Abstract and Figures

Abstract Nutrients present in various foods plays an important role in maintaining the normal functions of the human body. The major nutrients present in foods include carbohydrates, proteins, lipids, vitamins, and minerals. Besides these, there are some bioactive food components known as "phytonutrients" that play an important role in human health. They have tremendous impact on the health care system and may provide medical health benefits including the prevention and/or treatment of disease and various physiological disorders. Phytonutrients play a positive role by maintaining and modulating immune function to prevent specific diseases. Being natural products, they hold a great promise in clinical therapy as they possess no side effects that are usually associated with chemotherapy or radiotherapy. They are also comparatively cheap and thus significantly reduce health care cost. Phytonutrients are the plant nutrients with specific biological activities that support human health. Some of the important bioactive phytonutrients include polyphenols, terpenoids, resveratrol, flavonoids, isoflavonoids, carotenoids, limonoids, glucosinolates, phytoestrogens, phytosterols, anthocyanins, ω-3 fatty acids, and probiotics. They play specific pharmacological effects in human health such as anti-microbial, anti-oxidants, anti-inflammatory, anti-allergic, anti-spasmodic, anti-cancer, anti-aging, hepatoprotective, hypolipidemic, neuroprotective, hypotensive, diabetes, osteoporosis, CNS stimulant, analgesic, protection from UVB-induced carcinogenesis, immuno-modulator, and carminative. This mini-review attempts to summarize the major important types of phytonutrients and their role in promoting human health and as therapeutic agents along with the current market trend and commercialization.
Content may be subject to copyright.
Charu Gupta* and Dhan Prakash
Phytonutrients as therapeutic agents
Abstract: Nutrientspresentinvariousfoodsplaysanimpor-
tant role in maintaining the normal functions of the human
body. The major nutrients present in foods include carbohy-
drates, proteins, lipids, vitamins, and minerals. Besides
these, there are some bioactive food components known as
phytonutrients that play an important role in human
health. They have tremendous impact on the health care
system and may provide medical health benefits including
the prevention and/or treatment of disease and various phy-
siological disorders. Phytonu trients play a positive role by
maintaining and modulating immune function to prevent
specific diseases. Being natural products, they hold a great
promise in clinical therapy as they possess no side effects that
are usually associated with chemotherapy or radiotherapy.
They are also comparatively cheap and thus significantly
reduce health care cost. Phytonutrients are the plant nutrients
with specific biological activities that support human health.
Some of the important bioactive phytonutrients include poly-
phenols, terpenoids, resveratrol, flavonoids, isoflavonoids,
carotenoids, limonoids, glucosinolates, phytoestrogens, phy-
tosterols, anthocyanins, ω-3 fatty acids, and probiotics. They
play specific pharmacological effects in human health such
as anti-microbial, anti-oxidants, anti-inflammatory, anti-
allergic, anti-spasmodic, anti-cancer, anti-aging, hepatopro-
tective, hypolipidemic, neurop rotective, hypotensive, dia-
betes, osteoporosis, CNS stimulant, analgesic, protection
from UVB-induced carcinogenesis, immuno-modulator, and
carminative. This mini-review attempts to summarize the
major important types of phytonutrients and their role in
promoting human health and as therapeutic agents along
with the current market trend and commercialization.
Keywords: anthocyanins, carotenoids, flavonoids, gluco-
sinolates, nutraceuticals, phytoestrogens, phytonutrients,
polyphenols, terpenoids
DOI 10.1515/jcim-2013-0021
Received June 14, 2013; accepted May 20, 2014; previously
published online July 22, 2014
Food plays a vital role in maintaining normal function of
the human body. With recent advances in medical and
nutritional sciences, natural products have received
extensive attention as health-promoting foods from both
health professionals and the consumers. Bioactive foods
and nutraceuticals have emerged as potential supple-
ments in various diseases and preventive natural sources
from food [1]. Consumers can use nutraceuticals as sup-
plementation to a poor diet, to improve overall health, to
delay the onset of age-related diseases, after illness, for
stress, in pregnancy and slimming, to improve sports
performance, and to treat symptoms (cold, cough, arthri-
tis, etc.). These functional also called as medicinal foods
contain phytonutrients or phytomedicines that play ben-
eficial roles in maintaining well-being, enhancing health,
and modulating immune function to prevent specific dis-
eases. Phytonutrients and Phytotherapy is a more
recent term that refers to a science of treatment using a
group of natural substances that include certain herbs
and their derivatives for use as dietary supplements and
regulated as foods [2, 3].
As phytonutrients are of natural origin, they are use-
ful in clinical therapy due to their lower side effects as
compared to chemotherapy or radiotherapy and are
advantageous in reducing the health care cost [4].
There are scientific evidences of their chemical and
biological properties, clinical information, mode of action,
quality control, and effectiveness of phytonutrients in
nutritional therapy [5]. Phytonutrients play an important
role in human health as anti-oxidants, anti-bacterial, anti-
fungal, anti-inflammatory, anti-allergic, anti-spasmodic,
chemo-preventive, hepatoprotective, hypolipidemic, neu-
roprotective, and hypotensive agents and help in prevent-
ing aging, diabetes, osteoporosis, cancer and heart
diseases, induced apoptosis, diuretic, CNS stimulant,
analgesic, protection from UVB-induced carcinogenesis,
immuno-modulator, and carminative [6, 7].
Dietary intake of phytochemicals promotes health ben-
efits and protects against chronic degenerative disorders,
such as cancer, cardiovascular and neurodegenerative
diseases, diabetes, high blood pressure, inflammation,
*Corresponding author: Charu Gupta, Amity Institute for Herbal
Research and Studies, Amity University, Noida, Uttar Pradesh, India,
Dhan Prakash, Amity Institute for Herbal Research and Studies,
Amity University, Noida, Uttar Pradesh, India
J Complement Integr Med. 2014; 11(3): 151169
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
microbial, viral and parasitic infections, psychotic diseases,
spasmodic conditions, and ulcers. These phytochemicals,
either alone and/or in combination, have tremendous ther-
apeutic potential in curing various ailments.
The important phytonutrients include carotenoids,
tocopherols, ascorbates, lipoic acids, and polyphenols.
They are strong natural anti-oxidants with free radical
scavenging activity and are associated with a lower inci-
dence of degenerative diseases. Phytoestrogens are non-
steroidal phytochemicals quite similar in structure and
function to gonadal estrogen hormone. They offer an
alternative therapy for hormone replacement therapy
(HRT) with beneficial effects on cardiovascular system
and may even alleviate menopausal symptoms.
Terpenoids are the largest class of phytonutrients present
in green foods and grains, and they provide a measure of
protection from certain diseases, especially those related
to chronic damage and growth deregulation. Carotenoids
lower risk of chronic diseases like cardiovascular, certain
cancers, and eye. Limonoids provide substantial anti-
cancer actions; phytosterols compete with cholesterol in
the intestine for uptake and aid in the elimination of
cholesterol from the body; glucosinolates (GLSs) that
are activators of liver detoxification enzymes, provide
protection against carcinogenesis, mutagenesis, and
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.
The probiotic bacteria are used for the manufacture of a
natural remedy, for controlling weight gain, preventing
obesity, increasing satiety, prolonging satiation, reducing
food intake, reducing fat deposition, improving energy
metabolism, treating and enhancing insulin sensitivity,
and treating obesity.
Although most phytonutrients currently used are
known as vital nutrients for the human body, many
details such as dose, drugdrug interaction, nutraceuti-
caldrug interaction, and their effects on individuals
under certain health conditions remain elusive [8]. It is
normally assumed that proper nutrient balance is
required to maintain a healthy status of the human
body, and excess intake of any nutrient may not benefit
or even can be harmful to health.
Knowledge from food chemistry, nutrition, and clin-
ical studies provides more insight into our understanding
of biological functions, usage, and potential adverse
effects of nutraceuticals [8, 9]. This advanced knowledge
helps to standardize manufacturing processes and clin-
ical practices and add more value to nutraceutical mar-
kets [10]. The present review would focus on therapeutic
property and major food sources of some of the important
phytonutrients or bioactive food components like antho-
cyanidins, carotenoids, lycopenes, flavonoids, GLSs, iso-
flavonoids, limonoids, polyphenols, ω-3 fatty acids,
phytoestrogens, resveratrol, phytosterols, probiotics,
and terpenoids. All these phytonutrients play specific
pharmacological effects on human health as anti-inflam-
matory, anti-allergic, anti-oxidants, anti-microbial, anti-
spasmodic, chemopreventive, hepatoprotective, hypolipi-
demic, neuroprotective, hypotensive, anti-aging, dia-
betes, osteoporosis, protection of DNA damage, cancer
and heart diseases, induced apoptosis, diuretic, CNS sti-
mulant, analgesic, protection from UVB-induced carcino-
genesis, immuno-modulator, and carminative [6].
Phytonutrients or bioactive food components can be
added or increased to traditional foods through genetic
engineering techniques. An example would be the high
lycopene tomato, a genetically modified tomato with
delayed ripening characteristics that is high in lycopene
and has potent anti-oxidant capabilities.
The present chapter would discuss about these
potential bioactive food components that could provide
benefits in terms of health and well-being and the poten-
tial role of these functional ingredients (Table 1) along
with their current market trends and scenario.
Phytonutrients and their health
Major source
Polyphenols are naturally occurring compounds found
largely in fruits, vegetables, cereals, and beverages.
Legumes and chocolate also contribute to the polyphe-
nolic intake. The major sources of dietary polyphenols
are cereals, legumes (barley, corn, nuts, oats, rice, sor-
ghum, wheat, beans, and pulses), oilseeds (rapeseed,
canola, flaxseed, and olive seeds), fruits, vegetables,
and beverages (fruit juices, tea, coffee, cocoa, beer, and
wine) [1113].
Fruits such as apple, grape, pear, cherry, and various
berries contain up to 200300 mg polyphenols per 100 g
152 Gupta and Prakash: Bioactive compounds in health
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
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
red grapes
Anti-allergic, anti-inflammatory, anti-oxidants, and
Carotene Carrots, leafy greens and red, orange and yellow
vegetables, and pumpkin
Anti-carcinogenic, enhances release of immunogenic
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
Soybean Anti-cancer, hypolipidemic, and prevention of
GLSs Broccoli sprouts, cabbage, cauliflower, collards,
cruciferous vegetables, kale, radish, and turnip
Anti-oxidant, prevent DNA damage, and reduce risk of
breast and prostate cancers
Flavonoids Berries, legumes, tea, grapes, olive oil, cocoa, walnuts,
peanuts, spices, fruits, and vegetables. Especially
green vegetables, onion, apple, berries, and tea
Anti-bacterial, anti-oxidant, anti-viral, analgesic
activities, inhibition of hydrolytic and oxidative
enzymes, anti-inflammatory, anti-viral, and anti-
Quercetin Red onions, buckwheat, red grapes, green tea, and
apple skin
Strong anti-oxidant, reduces low-density lipoprotein
(LDL) oxidation, vasodilator, and blood thinner
Isoflavonoids Members of the Fabaceae (Leguminosae) family, soy
cheese, soy flour, soy bean, and tofu
Anti-oxidant, anti-proliferative, anti-cancer, and
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,
sorghum, wheat, beans, and pulses), oilseeds
(rapeseed, canola, flaxseed, and olive seeds), fruits,
vegetables, and beverages (fruit juices, tea, coffee,
cocoa, beer, and wine)
Anti-oxidant, anti-carcinogenic, anti-inflammatory, anti-
neurodegenerative, anti-diabetic, anti-viral, skin photo-
protective, anti-allergic, anti-platelet, anti-aging,
cytoprotective, and DNA-protective properties.
ω-3-fatty acids Fish such as salmon, rainbow trout, mackerel, herring,
and sardines. Plants canola, soybean, and flax oils
Osteoarthritis, lowers cholesterol, reduces high blood
pressure, protects from heart attacks, eases joint
pains, fights wrinkles and skin ailments, and improves
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 travelers diarrhea and
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
Gupta and Prakash: Bioactive compounds in health 153
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
fresh weights. Similarly, a glass of red wine or a cup of
coffee or tea contains about 100 mg polyphenols. Their
total dietary intake may be about 1 g per day, which is
about 10 times higher than that of vitamin C and 100 times
higher than those of vitamin E and carotenoids [14, 15].
Mode of action
These molecules are secondary metabolites of plants and
are generally involved in defense against ultraviolet (UV)
radiation or aggression by pathogens. Basic researches
and epidemiological studies have shown the inverse
association between risk of degenerative diseases and
intake of diet rich in polyphenols. The epidemiological
studies provide convincing evidences that diet rich in
anti-oxidants is associated with a lower incidence of
degenerative diseases. Polyphenols, with ~8,000 struc-
tural variants, are characterized by the presence of aro-
matic rings bearing one or more hydroxyl moieties, which
have proven pivotal roles in mediating their properties
(Figure 1) [16]. Although the knowledge of absorption,
bioavailability, and metabolism of polyphenols is not
entirely known, it appears that some polyphenols are
bioactive and are absorbed in their native or modified
form by the microflora of the intestine. The active com-
ponents of dietary phytochemicals (e.g. curcumin, resver-
atrol, capsaicin, catechins, vitamins, and β-carotene) are
believed to suppress the inflammatory processes, moder-
ate cell signaling pathways, proliferation, apoptosis,
redox balance and most often appear to be protective
against cancer, neurodegenerative disorders and cardio-
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
signaling pathways, inhibiting the production of inflam-
matory cytokines and chemokines, suppressing the activ-
ity of COX and iNOS and decreasing the production of
free radicals [19]. Several phytochemicals including gen-
istein [20], curcuminoids [17], and catechins [21] are
known to suppress the activation of Akt, thus, inhibiting
cancer cell growth. Some phenols like resveratrol, curcu-
min, and green tea catechins have been shown to sup-
press COX-2 giving the benefit of decreasing the
production of reactive oxygen species (ROS) [22, 23].
Furthermore, several polyphenols suppress lipid per-
oxidation to maintain the cellular status of anti-oxidant
enzymes like superoxide dismutase, catalase, and glu-
tathione peroxidase [24]. Due to the NF-κB suppressing
effect of polyphenols, some of them (e.g. curcumin, resver-
atrol, quercetin, and green tea polyphenols) have been
shown to decrease the expression of chemokines and cyto-
kines [25]. Polyphenols present in healthy foods or drinks
are readily metabolized to phenolic acids and aldehydes
by the microflora of the intestine, raising the possibility
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
possess substantial skin photo-protective effects [27].
Therapeutic property
In the recent years, there has been much awareness about
functional foods and nutraceuticals fortified with natural
polyphenols and their health benefits like their potent
anti-oxidant activity, anti-carcinogenic, anti-inflammatory,
anti-neurodegenerative, anti-diabetic, anti-viral, skin
photo-protective, anti-allergic, anti-platelet, anti-aging,
cytoprotective, and DNA-protective properties [23].
Major source
The terpenes, also known as isoprenoids, are the largest
class of phytonutrients in green foods and grains. These
compounds are found in higher plants, mosses,
-Coumaric acid CH=CH.COOH H H
Ferulic acid CH=CH.COOH
Chlorogenic acid CH=CH.COO-quinic acid OH H
Vanillic acid
Syringic acid
Gallic acid
Protocatechuic acid COOH
Caffeic acid
Figure 1 Phenolic acids: hydroxycinnamic acids.
154 Gupta and Prakash: Bioactive compounds in health
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
liverworts, algae, and lichens, as well as in insects,
microbes, or marine organisms. Terpenoids are derived
from a common biosynthetic pathway based on mevalo-
nate as parent and are named terpenoids, terpenes, or
isoprenoids with the subgroup of steroids among them as
a class [28, 29]. Their importance to plants relates to their
necessity to fix carbon through photosynthetic reactions
using photosensitizing pigments. Animals have evolved
to utilize these compounds for hormonal and growth
regulatory functions (vitamin A), and the presence of
these molecules in animal tissues also provides a mea-
sure of protection from certain diseases, especially those
related to chronic damage and growth deregulation.
The diverse functional roles of some of the terpenoids
are characterized as hormones (gibberellins), photosyn-
thetic pigments (phytol and carotenoids), electron car-
riers (ubiquinone and plastoquinone), and mediators of
polysaccharide assembly, as well as communication and
defense mechanisms [30].
Mode of action
Terpenes have a unique anti-oxidant activity in their
interaction with free radicals. They react with free radi-
cals by partitioning themselves into fatty membranes by
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
apoptotic inducers for human breast cancer cells. The
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].
Therapeutic property
Several biological actions have been reported for diter-
penes including anti-bacterial, anti-fungal, anti-inflamma-
tory, anti-leishmanial, cytotoxic, and anti-tumor activities
[31]. Currently, a broad range of biological responses can
be elicited in humans through various terpenoids that are
applicable to human health care [32]. Different terpenoid
molecules have anti-microbial, anti-fungal, anti-parasitic,
anti-viral, anti-allergenic, anti-spasmodic, anti-hyperglyce-
mic, anti-inflammatory, chemotherapeutic, and immuno-
modulatory properties [32, 33]. Terpenes are also used as
skin penetration enhancers, as well as natural insecticides,
and can be of use as protective substances in storing
agriculture products [34].
Resveratrol is a natural compound made by type of
plants. It is a phyto-alixin, made by plants in stress
conditions and pathogen attack.
Major source
It is found in considerable concentrations in grapes, pea-
nuts, and so forth. In the diet, the major source is found
in red wine (Figure 2). Resveratrol is made in grape skins,
but not in the flesh, thus it is found very little in white
wine, and proportionally in rose wines with the highest
concentration in red wines. The richest natural sources of
resveratrol are dark grape extracts (Vitis vinifera) and
giant knotweed (Polygonnum cuspidatum, a perennial
shrub). It is also found in abundance in labrusca and
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,
and their products [35, 36].
It also occurs in the vines, roots, seeds, and stalks, but
its highest concentration is in the skin, which contains
50100 µg/g [37].
Mode of action
Resveratrol produces various physiological effects. At low
concentrations that normally occur in food, resveratrol
has been shown to exert neuroprotective effects [38], as
well as beneficial effects on the cardiovascular system
[39]. These effects are mostly attributed to its anti-oxidant
properties. Resveratrol inhibits the proliferation and
induces apoptotic cell death in multiple cancers cell
types in vitro [40, 41]; moreover, in animal models of
cancer, resveratrol has been shown to inhibit
Figure 2 Resveratrol.
Gupta and Prakash: Bioactive compounds in health 155
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
angiogenesis and delay tumor growth [42], impede carci-
nogenesis [43], and reduce experimental metastasis [44].
Resveratrol acts on the process of carcinogenesis by
affecting the three phases: tumor initiation, promotion,
and progression phases, and suppresses the final steps of
carcinogenesis, i.e. angiogenesis and metastasis. It is also
able to activate apoptosis, arrest the cell cycle, or inhibit
kinase pathways.
Therapeutic property
Resveratrol is trans-stilbene that undergoes isomerization
under UV radiation. It is the trans form of resveratrol
that has been shown to display a much broader spectrum
of pharmacological activity than its cis isomer.
Stilbenes, in particular trans-resveratrol and its gluco-
side, are widely reported to be beneficial to health and
possess anti-oxidative, anti-carcinogenic, and anti-tumor
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-
tective, anti-aging, and cancer preventive and therapeutic
Major source
Flavonoids are polyphenolic compounds present in ber-
ries, legumes, tea, grapes, olive oil, cocoa, walnuts, pea-
nuts, spices, fruits, and vegetables. Green vegetables,
onion, apple, berries, and tea are the rich sources of
flavonoids. Flavonoids are present in most plant tissues
and often in vacuoles [45].
Flavonols are the most ubiquitous flavonoids in the
foods. Quercetin and kaempfreol are the main represen-
tatives of this group (Figure 3). They are generally present
at relatively low concentrations of about 1530 mg/kg
fresh weight. Onions, curly kale, leeks, broccoli, and
blueberries are the rich sources of flavonols. Flavanones
are found in tomatoes and certain aromatic plants such
as mint (Mentha piperita), but they are present in high
concentrations only in citrus fruits. The main flavanones
are naringenin in grapefruit, hesperetin in oranges, and
eriodictyol in lemons. The major sources of flavonoids
intake are tea (61%), onions (13%), and apples (10%); the
other sources include cherry, tomato, broccoli, black
grapes, and blueberries [45].
Therapeutic property
Flavonoids have been studied extensively since they have
many curative effects such as anti-bacterial, anti-oxidant,
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
be classified into several distinct subclasses based on
their chemical structures and exert various health-
promoting effects in human body for disease prevention.
Among the biological activities, flavonoids are active
against free radicals; free radical mediated cellular sig-
naling, inflammation, allergies, platelet aggregation,
microbes, ulcers, viruses, tumors, and hepatotoxins.
Anti-proliferative effects such as cancers, cardio vascular,
and inflammatory diseases of dietary flavonoids are also
well recognized. Scavenging activity of hydroxyl radicals,
superoxide anion radicals, and lipid peroxy radicals sig-
nifies the health-promoting functions of flavonoids [47].
Mode of action
Flavonoids are a subclass of plant phenols which include
the minor flavonoids (flavanones and dihydroflavonols),
flavones, and flavonols (Table 2). Proposed mechanisms
by which they provide health benefits, in addition to being
direct chemical protectants involve modulatory effects on
a variety of metabolic and signaling enzymes. Flavonoids
Figure 3 Flavonoids.
156 Gupta and Prakash: Bioactive compounds in health
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
have been shown to block the angiotensin converting
enzyme that raises blood pressure; inhibit cyclooxygenase
which forms prostaglandins; and block enzymes that pro-
duce estrogen. The implications of these in vitro inhibitory
actions are that certain flavonoids prevent platelet aggre-
gation, reduce heart disease and thrombosis, and inhibit
estrogen synthase which binds estrogen to receptors in
several tissues, thus decreasing the risk of estrogen-related
cancers. Bioactive properties such as free radical scaven-
ging, inhibition of hydrolytic and oxidative enzymes, anti-
inflammatory and anti-viral [48] action of flavonoids are
well known. There is inverse association between flavo-
noids intake and coronary heart disease mortality.
Flavonoids in regularly consumed foods appeared to
reduce the risk of death from coronary heart disease; but
some flavonoids have been reported to be mutagenic as
well [49]. The capacity of flavonoids to act as anti-oxidants
depends upon their molecular structure. The position of
hydroxyl groups and other features in the chemical struc-
ture of flavonoids are important for their anti-oxidant and
free radical scavenging activities. Quercetin, the most
abundant dietary flavonol, is a potent anti-oxidant
because it has all the right structural features for free
radical scavenging activity [47]. Luteolin has anti-inflam-
matory, anti-mutagenic, and anti-bacterial activities.
Research has proved that apigenin suppressed
Table 2 Dietary sources of polyphenols [109, 110].
Classes/subclasses Polyphenols Sources
Cyanidin 3-glycosides
Black berries, black currant, black grape, blue berries,
cherries, cranberry, plums, pomegranate, raspberry, red
wine, strawberries
Apples, apricots, beans, berries, black currant, broccoli,
buckwheat, celery
Cherries, cherry tomatoes, chives, cocoa, grapes, kale,
lettuce, onions
Peppers, plums, red wine, spinach
Sweet potato, tea
Flavanones Hesperetin
Citrus fruits and their juices
Grapes, tangerine juice
Flavones Apigenin
Celery, fresh parsley, olives, oregano
Peppers, rosemary
Epicatechin and their gallates, Morin
Prodelphinidins, Catechin
Apples, apricots, berries, cherries
Chocolate, grapes, peaches, pears, plums, raisins, red
wine, tea
Equol, Genistein
Grape seeds/skin, soy cheese and sauces, soy products,
Flavonoid glycoside Hesperidin
Naringin, Rutin
Grape fruit, lemon, orange juice
Orange, tangerine juice
Phenolic acids Caffeic acid
Chlorogenic acid
Ferulic acid
p-Coumaric acid
Apple, apple juice, blueberry, cider, cranberry, grape fruit,
lemon, lettuce, coffee beans, orange, peach, pear, cherry,
potato, spinach, tea
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
Epicatechin polymers, Ellagitannins
Tannic acids
Apple juice, blackberry, chick pea
Cocoa, coffee, grape seeds and skin
Lentils, olive, peach, peas, plum
Pomegranate, raspberries, red wine
Strawberries, tea, walnuts
Diferuloylmethane Curcumin Turmeric
Gupta and Prakash: Bioactive compounds in health 157
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
12-O-tetradecanoylphorbol-3-acetate (TPA)-mediated
tumor promotion of mouse skin, similar to curcumin, a
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-
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
and anti-bacterial activities and is directly mutagenic.
Quercetin, the most common flavonoid in higher plants,
seems to contribute to the mutagenicity of kaempferol in
the presence of microsomal metabolizing systems.
Quercetin inhibits a number of enzymes, smooth muscle
contraction, and proliferation of rat lymphocytes.
Although it is anti-inflammatory, anti-bacterial, anti-viral,
and anti-hepatotoxic, it exhibits mutagenic activity and
allergenic properties [50]. Catechins and gallic acids,
major sources of catechins are grapes, berries, cocoa,
and green tea. Tea contains considerable amounts of gallic
acid esters, such as epicatechin, epicatechingallate and
epigallocatechingallate. Numerous studies have suggested
that these components provide protective benefits by their
free radical scavenging ability and their inhibition of eico-
sanoid synthesis and platelet aggregation. The green tea
provides protection against prostate cancer [51]. Wines
contain catechins and procyanidins that are responsible
for its astringency sensation. Catechin is one of the major
phenolics in grapes and red wines and is considered to be
partly responsible for the protective effect against athero-
sclerotic cardiovascular disease.
Major sources
They are another subclass of the phenolic phytonutrients.
Isoflavonoids are produced almost exclusively by the
members of the Fabaceae (Leguminosae) family. Their
main food sources are soy cheese, soy flour, soy bean,
and tofu. Soybeans are an unusually concentrated source
of isoflavones, including genistein and daidzein (Figure 4),
and soy is the major source of dietary isoflavones.
Therapeutic property
The isoflavones of soy have a property of binding to the
estrogen receptor class of compounds, thus representing
an activity of a number of phytochemicals termed phy-
toestrogens. Genistein inhibits the growth of most hor-
mone-dependent and -independent cancer cells in vitro,
including colonic cancer cells. Isoflavones have received
considerable attention as potentially preventing and
treating cancer and osteoporosis [52]. Research in mice
has shown that dietary soybean components inhibited
the growth of experimental prostate cancer and altered
tumor biomarkers associated with angiogenesis.
Although the epidemiological data suggest that soy
potentially decreases the risk of breast and prostate can-
cer but the evidence that soy exerts a protective effect
against colonic cancer is limited.
Mode of action
Anti-oxidant and anti-proliferative properties of isoflavones
offer important mechanisms for their protection against
many prevalent chronic diseases [53, 54]. Cellular damage
resulting from oxidative stress is believed to be a major
contributor to the etiology of cardiovascular disease
through the oxidation of LDL and cancer by causing DNA
strand breaks which may lead to mutations [55, 56]. Recent
research has shown that the isoflavone genistein from soy,
selectively bound to the β-estrogen receptor and reduced
binding to the α-receptor 20-fold.
Major sources
The group of carotenoids consists of more than 700 phy-
tochemicals, which constitute photosynthetic membranes
= H, R
= OMe (Formononetin)
= OH, R
= OMe (Biochanin A)
= H, R
= OH (Daidzein)
= OH, R
= OH (Genistein)
Figure 4 Isoflavones (phytoestrogen).
158 Gupta and Prakash: Bioactive compounds in health
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
and produce colors in plants and animals. Out of 700
pigments, only about 24 commonly occur in human food-
stuffs [57]. The most studied carotenoids are α-carotene,
β-carotene, lycopene, lutein, and zeaxanthin (Figure 5).
The principal carotenoids of foods are β-carotene, β-cryp-
toxanthin, lycopene, and lutein. Carotenoid pigments are
abundant in many fruits and vegetables and have been
studied for their diverse roles in phytochemistry and
phytomedicine [57].
Carotenoids are mainly C
isoprenoids, consisting
of eight isoprene units. There are two main groups of
carotenoids (i) carotenes (β-carotene, lycopene) contain
only hydrogen and carbon and may be cyclic or linear;
(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-
otenoids contains upto 15 conjugated double bonds,
which are responsible for their characteristic absorption
spectra and specific photochemical properties [58]. They
are responsible for quenching singlet oxygen and for
intercepting deleterious free radicals and ROS. These
properties make them a part in diverse anti-oxidant
defense system. Most carotenoids are found in linear or
all trans-configuration. However on exposure to light or
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-
ities of carotenoids are intimately related to their chemi-
cal structures. Epidemiological studies have shown a
positive link between higher dietary intake and tissue
concentrations of carotenoids with lower risk of chronic
diseases [60, 61].
Therapeutic property
The β-carotene and lycopene have been shown to be
inversely related to the risk of cardiovascular diseases
and certain cancers, whereas lutein and zeaxanthin are
related with the prevention of eye disorders [60, 62].
Lutein protects against uterine, prostate, breast, color-
ectal, and lung cancers. They also protect against risk
of digestive tract cancer. Xanthophyll, a type of carote-
noids, offers protection to other anti-oxidants and exhibit
tissue specific protection. Zeaxanthin, cryptoxanthin, and
astaxanthin are all the members of xanthophyll group
[63, 64].
Mode of action
The anti-oxidant properties of carotenoids have been sug-
gested to be the main mechanism by which they afford their
beneficial effects. Research has shown that carotenoids med-
iate their effects through other mechanisms such as gap
junction communication, cell growth regulation, modulat-
ing gene expression, immune response, and modulators of
Phase I and II drug metabolizing enzymes [65, 66].
Major source
Lycopene, a carotenoid without provitamin-A activity, is
present in many fruits and vegetables (Figure 6);
Figure 5 β-Carotene.
Figure 6 Lycopene.
Gupta and Prakash: Bioactive compounds in health 159
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
however, tomatoes and processed tomato products con-
stitute the major source of lycopene in diet. Among the
carotenoids, lycopene is a major component found in the
serum and other tissues.
Therapeutic property
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
cardiovascular diseases. Serum and tissue lycopene
levels have also been inversely related with the chronic
disease risk. Although the anti-oxidant properties of lyco-
pene are primarily responsible for its beneficial proper-
ties, other mechanisms such as modulation of
intercellular gap junction communication, hormonal
and immune system, and metabolic pathways are also
involved [67].
Mode of action
Lycopene also has the ability to destroy free radicals that
are produced as a result of metabolic reactions in the
body. It suppresses the attack of cellular oxygen and
ROS thereby slowing down the formation of free radicals
and therefore prevents destruction of the lipophilic parts
of the cell [68].
A study assessing the acute effects of lycopene on
airway hyper-responsiveness was carried out in patients
with exercise-induced asthma (EIA). The results showed
that 55% of those taking lycopene were significantly
protected against EIA and did not experience this inhaled
steroid dose FEV1 reduction [69]. The anti-oxidant capa-
city of lycopene offers protection against γ-radiation
induced damage to cells [70].
A study by Gitenay et al. [71] showed that even yellow
varieties of tomatoes that are without lycopene showed a
stronger anti-oxidant effect in rats. Rats with mild oxida-
tive stress, caused by low vitamin E level, were fed with
placebo, yellow tomato extract, red tomato extract, and
lycopene. All diets had no effect on plasma cholesterol
but only the red tomato diet reduced triglycerides. Rats
fed with yellow or red tomato extract showed lower levels
of thiobarbituric reactive species in the heart than those
fed with placebo or lycopene. This led the researchers to
conclude that tomatoes, containing lycopene or not, have
a higher potential than lycopene alone to attenuate
oxidative stress parameters in a mild oxidative stress
context [71].
Major sources
These are terpenes present in citrus fruit. Citrus limo-
noids are present in large amounts in citrus juice and
citrus tissues as water-soluble limonoid glucosides or in
seeds as water-insoluble limonoid aglycones [72].
Therapeutic property
Limonoids are highly oxygenated triterpenoid com-
pounds with significant biological activity.
Mode of action
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-
noid aglycones (limonin, nomilin, obacunone, iso-obacu-
noic acid, and ichangin) induced significant amounts of
glutathione-S-transferase (GST) in the liver and intestinal
mucosa [73]. GST is a major detoxifying enzyme system
that catalyzes the conjugation of glutathione with many
potentially carcinogenic compounds which are highly
electrophilic in nature. A study of the inhibitory effects
of two limonoid aglycones (limonin and nomilin) on the
formation of benzo[a]pyrene induced neoplasia in the
fore stomach of ICR/Ha mice showed that incidence of
tumors could be reduced by more than 50% at 10 mg/
dose [74]. The experimental results described above indi-
cate that citrus limonoids may provide substantial anti-
cancer actions. The compounds have been shown to be
free of toxic effects in animal models so limonoids has a
potential against human cancer in either the natural
fruit or in citrus fruits fortified with limonoids, or in
purified forms of specific limonoids. They provide che-
motherapeutic activity by inhibiting Phase I enzymes and
inducing Phase II detoxification enzymes in the liver.
D-Limonene, a common monocyclic monoterpene,
found within orange peel oil, inhibits pancreatic carcino-
genesis induced in experimental models and also pro-
vides protection to lung tissue [63, 64]. Although the
initial studies are very promising, they have been con-
ducted primarily with in vitro cell culture and animal
models. Thus, more research is needed to determine
whether limonoids may be useful in preventing or treat-
ing cancer in humans. The first step is to assess the
bioavailability of the compounds for humans, their
160 Gupta and Prakash: Bioactive compounds in health
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
absorption after ingestion, and appearance in the blood
and tissues. If limonoid compounds are found to be
bioavailable, then more human studies are needed to
assess the effects of limonoid ingestion on biomarkers
related to cancer [64].
Major source
These are another important terpene subclass. The primary
sources of phytosterols are vegetables, nuts, fruits, and seeds.
Seeds contain an average of 120 mg of plant sterols/100 g
wet weight; vegetables contain 20 mg/100 g of wet
weight and fruit about 15 mg/100 g wet weight.
Sitosterol, campesterol, and stigmasterol are most abun-
dant in nature comprising 65%, 30%, and 3% of dietary
phytosterol intake (Figure 7) [75].
Therapeutic property
The two sterol molecules synthesized by plants are
β-sitosterol and its glycoside. In animals, these two mole-
cules exhibit anti-inflammatory, anti-neoplastic, anti-
pyretic, and immuno-modulating activity.
Mode of action
Phytosterols block inflammatory enzymes by modifying the
prostaglandin pathways in a way that protect platelets.
Phytosterols compete with cholesterol in the intestine for
uptake and aid in the elimination of cholesterol from the
body. Plant sterols are initially solubilized into a micelle
form in the intestine. These micelles interact with brush
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
excreted through the biliary system. The non-esterified phy-
tosterols are transported back into the intestinal lumen by
sterolin (1 and 2) pumps containing the ATP binding cas-
sette (ABC) proteins encoded by the genes ABCG5 and
ABCG8. These are expressed in the mucosal cells and the
canalicular membrane, and they re-secrete sterols, espe-
cially absorbed plant sterols, back into the intestinal
lumen and from the liver into bile [76]. Saturated phytoster-
ols appear to be more effective than unsaturated com-
pounds in decreasing cholesterol concentrations in the
body. Their actions reduce serum or plasma total choles-
terol and LDL cholesterol. There is a competition between
phytosterol and cholesterol for absorption from the intes-
tine due to their structural similarity. In mammals, concen-
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
and these studies do not prove or disprove an increase in
atherosclerotic risk that can be clearly related to serum
phytosterol levels. Studies have proved that vegetarians
who consume considerable plant sterols are at decreased
risk of arteriosclerosis cardiovascular disease [75].
Major source
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
several classes of phytoestrogens: steroidal estrogens,
found in few plants and the more ubiquitous are phenolic
estrogens, isoavones, stilbenes, coumestans, and lig-
nans. Soybean is rich in isoflavones, whereas the soy
sprout is a potent source of coumestrol, the major coume-
stan. The precursors of these substances are widespread
in the plant kingdom, but mainly found in Leguminosae
and are especially abundant in soybean and its products,
legumes, berries, whole grains, and cereals [7].
Sitosterol Sti
Figure 7 Phytosterols.
Gupta and Prakash: Bioactive compounds in health 161
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
The main dietary sources of coumestans are sprouted
legumes such as soy and alfalfa; however, low levels
have been reported in brussel sprouts and spinach.
Clover and soybean sprouts are reported to have its high-
est concentrations. The phytolignans are found in high
amounts in flaxseed, asparagus, whole grains, vegeta-
bles, and tea. Fruits also have their low levels with the
exception of strawberries and cranberries [7].
Mode of action
These are non-steroidal phytochemicals quite similar in
structure and function to gonadal estrogen hormone.
They offer an attractive alternate for HRT with beneficial
effects on cardiovascular system and may even alleviate
menopausal symptoms. They are potential alternatives to
the synthetic selective estrogen receptor modulators,
which are currently applied in HRT. They have anti-oxi-
dant effects due to their polyphenolic nature, anti-carcino-
genic, modulation of steroid metabolism or of
detoxification enzymes, interference with calcium-trans-
port, and favorable effects on lipid and lipoprotein profiles
[7, 78]. On the basis of chemical structure phytoestrogens
can be classified as isoflavones, flavones, coumestans,
stilbenes lignans, and coumestans (Figure 4).
Therapeutic property
Flavonoids have similar structure to estrogen, have the
capacity to exert both estrogenic and anti-estrogenic
effects, and provide possible protection against bone
loss and heart diseases. They share structural features
with estrogen, in the sense that the presence of particular
hydroxyl groups can be positioned in a stereo chemical
alignment virtually identical to one of the estrogens.
Populations in China, Japan, Taiwan, and Korea are esti-
mated to consume high quantities of isoflavones, and
women of these countries complain fewer incidences of
osteoporosis and related health problems, especially hot
flushes and cardiovascular diseases and lower incidence
of hormone-dependent breast and uterine cancers
[7981]. The main dietary source of phytoestrogenic stil-
benes is resveratrol from red wine and peanuts. Although
there are two isomers of resveratrol, cis and trans,
but only the trans form has been reported to be estro-
genic. It is found only in the skin of red grapes and green
grapes whereas white wine contains very low levels of
trans-resveratrol [82]. The term lignan is used for a
diverse class of phenylpropanoid dimers and oligomers.
Secoisolariciresinol and matairesinol are two lignan
dimers which are not estrogenic by themselves, but read-
ily convert to the mammalian lignans, enterodiol and
enterolactone, respectively, which are estrogenic. These
are of great interest because of their estrogenic, anti-
carcinogenic, anti-viral, anti-fungal, and anti-oxidant
activities [83].
In humans, gut microflora enzymatically metabolizes
the isoflavones and lignans, and the mammalian lignans
are readily absorbed [84]. The different activities and the
bioavailability of phytoestrogens vary depending on fac-
tors such as the form of administration, dosage, individual
metabolism, and the ingestion of other pharmacological
substances [85].
Major sources
GLSs are exclusively found in dicotyledonous plants,
genus Brassica alone contains more than 350 genera
and 3,000 species [86]. Crucifers contain very high con-
centration of GLSs. Many commonly consumed vegeta-
bles, condiments, forages and oil containing plants, such
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
phytochemicals including GLSs and its breakdown pro-
ducts, phenolics and other anti-oxidants like vitamins C
and K, as well as dietary essential minerals [88].
Therapeutic property
They are present in cruciferous vegetables and are activa-
tors of liver detoxification enzymes. These chemicals are
responsible for the pungent aroma and bitter flavor of
cruciferous vegetables. Consumption of cruciferous vege-
tables provides protection against carcinogenesis, muta-
genesis, and other forms of toxicity of electrophiles and
reactive forms of oxygen. The sprouts of certain crucifers,
including broccoli and cauliflower, contain higher
amounts of glucoraphanin (the GLS of sulforaphane)
than do the corresponding mature plants. Crucifer sprouts
may protect against the risk of cancer more effectively than
the same quantity of mature vegetables of the same variety
[89, 90]. During food preparation, chewing, and digestion,
GLSs in cruciferous vegetables are broken down to form
biologically active compounds such as indoles, nitriles,
thiocyanates, and isothiocyanates [91]. Indole-3-carbinol
162 Gupta and Prakash: Bioactive compounds in health
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
(an indole) and sulforaphane (an isothiocyanate) have
been scientifically proved for their anti-cancer effects.
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,
colon, and rectum due to the presence of a predominating
thioglucosides GLSs, [92] (Figure 8).
Mode of action
Dietary GLSs block the formation of endogenous or exo-
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-
tion of Phase II detoxification enzymes and inhibition of
Phase I carcinogen-activating enzymes, thereby influen-
cing several processes related to chemical carcinogenesis,
e.g. the metabolism, DNA binding, and mutagenic activ-
ity of promutagens. Studies in experimental animals
including humans have proved a reducing effect on
tumor formation and positive effect on health on con-
sumption of adequate amounts of indoles in brassica
vegetables. Indole-3-carbinol is a GLS metabolite that
inhibits organ-site carcinogenesis in rodent models. Its
preventive effect on human mammary carcinogenesis is
due to its ability to regulate cell cycle progression,
increase the formation of anti-proliferative estradiol
metabolite, and induce cellular apoptosis [89, 90].
ω-3 fatty acids
There is an extensive interest in increasing consumption of ω-
3 fatty acids, because they are associated with many health
benefits, but are consumed only in small amounts. In 2002,
the National Academy of Sciences Institute of Medicine
recognized that ω-3 fatty acids are essential in the diet and
established an estimated adequate intake for them [94].
Major source
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,
soybean, and flax oils provide the 18-carbon ω-3 fatty
acid, α-linolenic acid (Figure 9). However, higher plants
lack the enzymes to make 20- and 22-carbon polyunsatu-
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
foods with α-linolenic acid may be insufficient to supply
the need for long-chain ω-3 fatty acids, especially during
pregnancy and lactation [95].
Therapeutic property
The benefit of ω-3 fatty acids is well known in the treat-
ment of people suffering from osteoarthritis. Clinical stu-
dies have proved the value of ω-3 fatty acids in treating
inflammatory conditions ranging from atherosclerosis to
osteoarthritis. People suffering from osteoarthritis can
improve symptoms and even allow a reduction in the
use of NSAIDs on increasing their dietary intake of ω-3
fatty acids and monounsaturated fatty acids as found in
olive oil [96]. These fatty acids have other positive effects
like influencing cellular metabolic functions, supporting
cell membrane structure, and reducing the expression of
pro-inflammatory cytokines [97]. The most potent of the
ω-3 fatty acids containing oils are eicosapentaenoic acid
(EPA) and docosahexaenoic acid, which are found in
abundance in cold-water fish [98].
Western diets contain predominately ω-6 PUFAs
found in soybean, corn, sunflower, canola, and cotton-
seed oils. It is now recognized that diets high in ω-6 fatty
acids and low in ω-3 fatty acids may exacerbate several
chronic diseases [99]. One strategy to increase the avail-
ability of long-chain ω-3 fatty acids is to develop oilseed
S b-D-glucose
Figure 8 General structure of GLS.
Figure 9 (a) α-Linolenic acid and (b) structure linoleic acid.
Gupta and Prakash: Bioactive compounds in health 163
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
crops such as canola and soybean that contain stearido-
nic acid (18:4n-3). This ω-3 fatty acid occurs naturally in
only a few plants such as black currant seed oil and
echium. Stearidonic acid is the first product formed
when α-linolenic acid is converted to EPA, a desirable
long-chain ω-3 fatty acid.
Major source
Anthocyanins occur in all tissues of higher plants, includ-
ing leaves, stems, roots, flowers, and fruits.
Anthocyanins are derivatives of anthocyanidins, which
include pendant sugars (Figure 10). Plants rich in antho-
cyanins are Vaccinium species, such as blueberry, cran-
berry, blackberry, cherry, and red cabbage. The highest
recorded amount appears to be especially in the seed
coat of black soybean [100].
Therapeutic property
Anthocyanins are the largest group of water-soluble pig-
ments in the plant kingdom. They have potential health
benefits and disease prevention properties and are
known as potential anti-oxidants [101]. Consumption of
anthocyanin-enriched foods is associated with a reduced
risk of several diseases such as atherosclerosis [102],
dyslipidemia [103], and diabetes [104]. Anthocyanins
may appear red, purple, or blue depending on the pH.
They are synthesized through the phenylpropanoid path-
way; they are odorless and nearly flavorless, contributing
to taste as a moderately astringent sensation.
Anthocyanins are secondary metabolites and are also
approved for use as a food additive in the European
Union, Australia, and New Zealand. The main anthocya-
nin compounds are pelargonidin, cyaniding, and delphi-
nidin. Cyanidin and its glycosides are naturally dietary
pigments which have been found with promising poten-
tial benefits to humans, especially in the prevention and
treatment of diabetes mellitus [104, 105].
Probiotics the unconventional source of
bioactive food components
The probiotics are the unconventional source of bioactive
food components. The combination of probiotics and
prebiotics commonly known as synbiotics modifies the
composition of the GI microbiota, restores the microbial
balance, and therefore has the potential to provide health
benefits [106, 107].
Major source
The majority of probiotic microorganisms belonging to the
genera Lactobacillus and Bifidobacterium are present in
abundance in fermented dairy products like yoghurt, fer-
mented milk, and butter-milk. Both Lactobacillus and
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
of Bifidobacteria in the colon of adults is 10
but this number decreases with age. Bifidobacteria are non-
motile, non-spore forming, Gram-positive rods with varying
cell morphology. Most strains are strictly anaerobic.
Prebiotics and lactic acid bacteria (LAB) (probiotics)
have demonstrated beneficial effects with respect to the
function of innate immunity, intestinal barrier function,
and increased resistance to disease. The gut mucosa and
microbiota are intimately linked in the maintenance of a
functional interface between the host and the external
environment [109, 110]. A combined supply of prebiotics
and probiotics (synbiotics) has synergistic effects in enhan-
cing immunity and facilitating intestinal barrier function.
Therapeutic property
The probiotic bacteria are used for the manufacture of a
natural remedy, for controlling weight gain, preventing
obesity, increasing satiety, prolonging satiation, reducing
food intake, reducing fat deposition, improving energy
Figure 10 Anthocyanins.
164 Gupta and Prakash: Bioactive compounds in health
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
metabolism, treating and enhancing insulin sensitivity,
and treating obesity. Animal studies have demonstrated
the efficacy of some strains of LAB to lower serum cho-
lesterol levels, presumably by breaking down bile in the
gut, thus inhibiting its re-absorption [111].
Lactobacillus (Lb. sporogenes and Lb. acidophilus
NCFB 1748) and Bifidobacterium genus representatives
have been reported to play a critical role in weight reg-
ulation as an anti-obesity effect in experimental models
and humans [112]. Lactobacillus sporogenes has the abil-
ity to lower cholesterol levels. It produces a significant
reduction in LDL levels and a small but significant
increase in high-density lipoprotein cholesterol.
Lactobacillus acidophilus ferments lactose into lactic
acid, like many LAB. During digestion, L. acidophilus
assists in the production of niacin, folic acid, and pyri-
doxine. It also helps in bile de-conjugation, separating
amino acids from bile acids, which can then be recycled
by the body [113]. L. acidophilus may provide additional
health benefits, including improved gastrointestinal func-
tion, a boosted immune system, and a decrease in the
frequency of vaginal yeast infections and relief from indi-
gestion and diarrhea [114]. In addition, probiotics, pre-
biotics, and synbiotics are frequently recommended after
a course of antibiotics as a means of restoring the micro-
biota within the intestinal tract to its normal, healthy
state, as well as an aid in resolving uncomplicated
cases of diarrhea. Synbiotics are also being investigated
as aids in treating some non-gastrointestinal diseases.
There is some evidence that synbiotics may be useful in
treating some skin ailments, such as atopy.
Mode of action
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
potential to provide health benefits. However, only recently,
well-designed clinical studies have provided clear evidence
of health-promoting effects, such as prevention of antibiotic-
associated diarrhea, treatment of acute diarrhea, inflamma-
toryboweldisease,eradicationofClostridium difficile infec-
tion, and enhancement of intestinal immunity [115, 116].
Market trend of phytonutrients
The markets for phytonutrients in the form of nutraceu-
ticals and functional foods are rapidly expanding. They
represent annual global sales of US$75 billion in 2007. It
is reported that the Global Nutraceutical market would
grow at a CAGR of 6.30% over the period of 20132018.
One of the key factors contributing to this market growth
is the increasing global aging population. The Global
Nutraceutical market has also been witnessing the
increase in the nutraceutical product development.
However, the threats of ingredients and raw material
contamination could pose a challenge to the growth of
this market [117].
The predicted annual growth rates of various nutra-
ceutical categories have been estimated to range from 6%
for products treating digestive ailments up to 25% for eye
health products.
Current and predicted sales claim that the joint
health supplements like glucosamine, chondroitin, and
MSM appear to be the major product group, followed by
the PUFAs. However, fish oils and MSM have been pre-
dicted to show the greatest increase in sales [118]. The
contemporary use of soy, for example, is not simply a
matter of geographical habitat or cultural lifestyle. The
availability of specific foods and nutraceuticals refined
from soy allows all consumers to derive the proposed
benefits. This also applies to green tea, fish oils, flaxseed,
and others. However, a more active approach has to be
taken with those only normally available in formulated
dosages such as glucosamine, chondroitin, and MSM, for
Nutraceutical manufacturers are extolling the virtues
of controlled release formulations for release of precise
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
isoflavone range [119].
The present paper thus provides a comprehensive insight
into some of the major phytonutrients of therapeutic
importance, their human health benefits, and their pos-
sible use as health supplements and nutraceuticals.
Dietary intake of phytochemicals promotes health bene-
fits by protecting against chronic degenerative disorders,
such as cancer, cardiovascular, and neurodegenerative
diseases. These phytochemicals, either alone and/or in
combination, have tremendous therapeutic potential in
curing various ailments. Phytochemicals with nutraceuti-
cal properties present in food are of enormous signifi-
cance due to their beneficial effects on human health
Gupta and Prakash: Bioactive compounds in health 165
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
since they offer protection against numerous diseases or
disorders such as cancers, coronary heart disease, dia-
betes, high blood pressure, inflammation, microbial, viral
and parasitic infections, psychotic diseases, spasmodic
conditions, and ulcers. Thus phytonutrients can be reg-
ularly taken without any side effects. The future of nutra-
ceuticals from both plant (phytonutrients) and animal
origin holds exciting opportunities for the food industry
to create novel food products containing bioactive food
components. The government should persuade the food
industry by investing more in the nutraceuticals and
functional foods and gaining monetary rewards.
However, the products should be designed and formu-
lated as per the interest and tastes of the consumers.
Acknowledgments: Authors are grateful to Dr Ashok K.
Chauhan, Chairman and Founder President and Mr Atul
Chauhan, Chancellor, Amity University-UP, Noida-
201303, (India) for the encouragement, research facilities,
and financial support.
Conflict of interest statement
Authors conflict of interest disclosure: The authors sta-
ted that there are no conflicts of interest regarding the
publication of this article. Research support played no
role in the study design; in the collection, analysis, and
interpretation of data; in the writing of the report; or in
the decision to submit the report for publication.
Research funding: None declared.
Employment or leadership: None declared.
Honorarium: None declared.
1. Gupta C, Prakash D, Gupta S. Relationships between bioactive
food components and their health benefits. In: Martirosyan
DM, editor. Introduction to functional food science textbook,
1st ed. USA: Create Space Independent Publishing Platform,
2. Bagchi D. Nutraceuticals and functional foods regulations
in the United States and around the world. Toxicol
3. Berger MM, Shenkin A. Vitamins and trace elements: practical
aspects of supplementation. Nutrition 2006;22:9525.
4. Ramaa CS, Shirode AR, Mundada AS, Kadam VJ.
Nutraceuticals- an emerging era in the treatment and
prevention of cardiovascular diseases. Curr Pharm Biotechnol
5. Brower V. Nutraceuticals: poised for a healthy slice of the
healthcare market? Nat Biotechnol 1998;16:72831.
6. Prakash D, Gupta KR. The antioxidant phytochemicals of
nutraceutical importance. The Open Nutraceuticals J
7. Prakash D, Gupta C. Role of phytoestrogens as nutraceuticals
in human health. Pharmacol online 2011;1:51023.
8. Whitman M. Understanding the perceived need for
complementary and alternative nutraceuticals: lifestyle
issues. Clin J Oncol Nurs 2001;5:1904.
9. Zeisel SH. Regulation of nutraceuticals. Sci 1999;285:1856.
10. Gidley MJ. Naturally functional foods-challenges and
opportunities. Asia Pac J Clin Nutr 2004;13:31.
11. Cieslik E, Greda A, Adamus W. Contents of polyphenols in
fruits and vegetables. Food Chem 2006;94:13542.
12. Katalinic V, Milos M, Kulisic T, Jukic M. Screening of
70 medicinal plant extracts for antioxidant capacity and total
phenols. Food Chem 2006;94:5507.
13. Prakash D, Kumar N. Cost effective natural antioxidants. In:
Watson RR, Gerald JK, Preedy VR, editors. Nutrients, dietary
supplements and nutraceuticals. USA: Humana Press,
Springer, 2011:16388.
14. Packer L, Weber SU. The role of vitamin E in the
emerging field of nutraceuticals. New York: Marcel Dekker,
15. Scalbert A, Manach C, Morand C, Remesy C. Dietary
polyphenols and the prevention of diseases. Crit Rev Food Sci
Nutr 2005;45:287306.
16. Leiro J, Alvarez E, Arranz JA, Laguna R, Uriarte E, Orallo F.
Effects of cis-resveratrol on inflammatory murine macro-
phages: antioxidant activity and down regulation of
inflammatory genes. J Leukoc Biol 2004;75:115665.
17. Aggarwal BB, Shishodia S. Molecular targets of dietary agents
for prevention and therapy of cancer. Biochem Pharmacol
18. Rahman I, Biswas SK, Kirkham PA. Regulation of
inflammation and redox signaling by dietary polyphenols.
Biochem Pharmacol 2006;72:143952.
19. Chang F, Lee JT, Navolanic PM, Steelman LS, Shelton JG,
Blalock WL, et al. Involvement of PI3K/Akt pathway in cell
cycle progression, apoptosis, and neoplastic
transformation: a target for cancer chemotherapy. Leukemia
20. Li Y, Sarkar FH. Inhibition of nuclear factor kappa-B activation
in PC3 cells by genistein is mediated via akt signaling path-
way. Clin Cancer Res 2002;7:236977.
21. Tang FY, Nguyen N, Meydani M. Green tea catechins inhibit
VEGF-induced angiogenesis in vitro through suppression of
VE-cadherin phosphorylation and inactivation of akt molecule.
Int J Cancer 2003;106:8718.
22. Gerhauser C, Klimo K, Heiss E, Neumann I, Gamal-Eldeen A,
Knauft J, et al. Mechanism-based in vitro screening of
potential cancer chemopreventive agents. Mutat Res
23. Babu PV, Liu D. Green tea catechins and cardiovascular
health: an update. Curr Med Chem 2008;15:184050.
24. Labinskyy N, Csiszar A, Veress G, Stef G, Pacher P, Oroszi G,
et al. Vascular dysfunction in aging: potential effects of
resveratrol, an anti-inflammatory phytoestrogen. Curr Med
Chem 2006;13:98996.
25. Kowalski J, Samojedny A, Paul M, Pietsz G, Wilczok T. Effect of
apigenin, kaempferol and resveratrol on the expression of
166 Gupta and Prakash: Bioactive compounds in health
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
interleukin-1 beta and tumor necrosis factor-alpha genes in
J774. 2 macrophages. Pharmacol Rep 2005;57:3904.
26. Rios LY, Gonthier MP, Remesy C, Mila I, Lapierre C, Lazarus
SA, et al. Chocolate intake increases urinary excretion of
polyphenol derived phenolic acids in healthy human subjects.
Am J Clin Nutr 2003;77:91218.
27. Nichols JA, Katiyar SK. Skin photoprotection by natural poly-
phenols: anti-inflammatory, anti-oxidant and DNA repair
mechanisms. Arch Dermatol Res 2010;302:7183.
28. Tholl D. Terpene synthases and the regulation, diversity and
biological roles of terpene metabolism. Curr Opin Plant Biol
29. Bohlmann J, Keeling CI. Terpenoid biomaterials. Plant J
30. Langenheim JH. Higher plant terpenoids: a phytocentric
overview of their ecological roles. J Chem Ecol 1994;20:
31. Singh M, Pal M, Sharma RP. Biological activity of the labdane
diterpenes. Planta Med 1999;65:28.
32. Paduch R, Kandefer-Szerszen M, Trytek M, Terpenes FJ.
Substances useful in human healthcare. Arch Immunol Ther
Exp 2007;55:31527.
33. Wagner KH, Elmadfa I. Biological relevance of terpenoids.
Overview focusing on mono, di-, and tetraterpenes. Ann Nutr
Metabol 2003;47:95106.
34. Lee S, Peterson CJ, Coats JR. Fumigation toxicity of mono-
terpenoids to several stored product insects. J Stored Prod
Res 2003;39:7785.
35. Valenzano DR, Terzibasi E, Genade T, Cattaneo A, Domenici L,
Cellerino A. Resveratrol prolongs lifespan and retards the
onset of age-related markers in a short-lived vertebrate. Curr
Biol 2006;16:296300.
36. Wang SY, Chen C, Wang CY, Chen P. Resveratrol content in
strawberry fruit is affected by pre-harvest conditions. J Agric
Food Chem 2007;55:826974.
37. Burns J, Yokota T, Ashihara H, Lean ME, Crozier A. Plant foods
and herbal sources of resveratrol. J Agri Food Chem
38. De Ruvo C, Amodio R, Algeri S, Martelli N, Intilangelo A,
DAncona GM, et al. Nutritional antioxidants as
anti-degenerative agents. Int J Dev Neurosci 2000;18:
39. Pendurthi UR, Williams JT, Rao LV. Resveratrol, a polyphenolic
compound found in wine, inhibits tissue factor expression in
vascular cells: a possible mechanism for the cardiovascular
benefits associated with moderate consumption of wine.
Arterioscler Thromb Vasc Biol 1999;19:41926.
40. Pozo-Guisado E, Alvarez-Barrientos A, Mulero-Navarro S,
Santiago-Josefat B, Fernandez-Salguero PM. The
anti-proliferative activity of resveratrol results in apoptosis
in MCF-7 but not in MDAMB-231 human breast cancer cells:
cell-specific alteration of the cell cycle. Biochem Pharmacol
41. Kim YA, Choi BT, Lee YT, Park DI, Rhee SH, Park KY, et al.
Resveratrol inhibits cell proliferation and induces apoptosis
of human breast carcinoma MCF-7 cells. Oncol Rep
42. Tseng SH, Lin SM, Chen JC, Su YH, Huang HY, Chen CK, et al.
Resveratrol suppresses the angiogenesis and tumor growth of
gliomas in rats. Clin Cancer Res 2004;10:2190202.
43. Gusman J, Malonne H, Atassi G. A reappraisal of the potential
chemopreventive and chemotherapeutic properties of resver-
atrol. Carcinogenesis 2001;22:111117.
44. Busquets S, Ametller E, Fuster G, Olivan M, Raab V, Argiles JM,
et al. Resveratrol, a natural diphenol, reduces metastatic
growth in an experimental cancer model. Cancer Lett
45. Croteau R, Kutchan TM, Lewis NG. Natural products (second-
ary metabolites). In: Buchanan B, Gruissem W, Joneas R,
editors. Biochemistry and molecular biology of plants.
Rockville, MD: American Society of Plant Biologists,
46. Burda S, Oleszek W. Antioxidant and antiradical activities of
flavonoids. J Agric Food Chem 2001;49:27749.
47. Kumar S, Andy A. Health promoting bioactive chemicals from
brassica. Int Food Res J 2012;19:14152.
48. Hodek P, Trebil P, Stiborova M. Flavonoids- potent and
versatile biologically active compounds interacting with
cytochromes. Chem Biol Interact 2002;139:121.
49. Miller NJ, Larrea MB. Flavonoids and other plant phenols in
the diet: their significance as antioxidants. J Nutr Environ Med
50. Sharma G, Prakash D, Gupta C. Phytochemicals of
nutraceutical importance: do they defend against diseases?
In: Prakash D, Sharma G, editors. Phytochemicals of
nutraceutical importance. UK: CABI International Publishers,
51. Nichenametla SN, Taruscio TG, Barney DL, Exon JH. A review of
the effects and mechanism of polyphenolics in cancer. Crit
Rev Food Sci Nutr 2006;46:16183.
52. Ko KP, Park SK, Park B. Isoflavones from phytoestrogens and
gastric cancer risk: a nested case-control study within the
Korean multicenter cancer cohort. Cancer Epidemiol
Biomarkers Prev 2010;19:1292300.
53. Messina M, Erdman Jr J, Setchell KD. Introduction to and
perspectives from the fifth international symposium on the
role of soy in preventing and treating chronic disease. J Nutr
54. Zeng H, Chen Q, Zhao B. Genistein ameliorates β-amyloid
peptide (2535)- induced hippocampal neuronal apoptosis.
Free Rad Biol Med 2004;36:1808.
55. Giles D, Wei H. Effect of structurally related flavones/
isoflavones on hydrogen peroxide production and oxidative
DNA damage in phorbol ester-stimulated HL-60 cells. Nutr
Cancer 1997;29:7782.
56. Patel RP, Boersma BJ, Crawford JH, Hogg N, Kirk M,
Kalyanaraman B, et al. Antioxidant mechanisms of isoflavones
in lipid systems: paradoxical effects of peroxyl radical
scavenging. Free Rad Biol Med 2001;31:157081.
57. Dutta D, Chaudhuri UR, Chakraborty R. Structure, health
benefits, antioxidant property and processing and storage of
carotenoids. Afr J Biotechnol 2005;4:151020.
58. Britton G, Liaaen-Jemsen S, Carotenoids PH. Biosynthesis and
metabolism. Basel, Switzerland: Birkauser Verlag, 1998.
59. Krinsky NI. Antioxidant functions of carotenoids. Free Rad Biol
Med 1989;7:61735.
60. Johnson EJ. The role of carotenoids in human health. Nutr Clin
Care 2002;5:479.
61. Elliott R. Mechanisms of genomic and non-genomic actions of
carotenoids. Biochim Biophys Acta 2005;1740:14754.
Gupta and Prakash: Bioactive compounds in health 167
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
62. Ribaya-Mercado JD, Blumberg JB. Lutein and zeaxanthin and
their potential roles in disease prevention. J Am Coll Nutr
63. Prakash D, Dhakarey R, Mishra A. Carotenoids: the
phytochemicals of nutraceutical importance. Indian J Agric
Biochem 2004;17:18.
64. Stahl W. Bioactivity and protective effects of natural
carotenoids. Biochim Biophys Acta 2005;1740:1017.
65. Jewell C, OBrien NM. Effect of dietary supplementation with
carotenoids on xenobiotic metabolizing enzymes in the liver,
lung, kidney and small intestine of the rat. Br J Nutr
66. Paiva S, Russell R. Beta carotene and other carotenoids as
antioxidants. J Am Coll Nutr 1999;18:42633.
67. Klebanov GI, Kapitanov AB, Teselkin YO, Babenkova IV,
Zhambalova BA, Lyubitsky OB, et al. The antioxidant
properties of lycopene. Membr Cell Biol 1998;12:287300.
68. Rao AV, Shen H. Effect of low dose lycopene intake on
lycopene bioavailability and oxidative stress. Nutr Res
69. Neuman I, Nahum H, Ben-Amotz A. Reduction of
exercise-induced asthma oxidative stress by lycopene, a
natural antioxidant. Allergy 2000;55:11849.
70. Srinivasan M, Sudhear AR, Pillai KR, Kumar PR, Sudhakaran R,
Menon VP. Lycopene as a natural protector against gamma
radiation induced DNA damage, lipid peroxidation and anti-
oxidant status in primary culture of isolated rats hepatocytes
in vitro. Biochim Biophys Acta 2007;177:65965.
71. Gitenay D, Lyan B, Rambeau M, Mazur A, Rock E.
Comparison of lycopene and tomato effects on biomarkers of
oxidative stress in vitamin E deficient rats. Eur J Nutr
72. Ozaki Y, Ayano S, Inaba N, Miyake M, Berhow MA,
Hasegawa S. Limonoid glucosides in fruit, juice and
processing by-products of satsuma mandarin (Citrus unshiu
Marcov.). J Food Sci 1995;60:1869.
73. Lam LK, Zhang J, Hasegawa S. Citrus limonoid reduction of
chemically induced tumorigenesis. Food Technol
74. Lam LK, Hasegawa S. Inhibition of benzo[a]pyrene-induced
forestomach neoplasia in mice by citrus limonoids. Nutr
Cancer 1989;12:437.
75. John S, Sorokin AV, Thompson PD. Phytosterols and vascular
disease. Curr Opin Lipidol 2007;18:3540.
76. Von Bergmann K, Sudhop T, Lutjohann D. Cholesterol and
plant sterol absorption: recent insights. Am J Cardiol
77. Dillard CJ, German JB. Review phytochemicals:
nutraceuticals and human health. J Sci Food Agric
78. Morabito N, Crisafulli A, Vergara C, Gaudio A, Lasco A, Frisina
N, et al. Effects of genistein and hormone-replacement therapy on
bone loss in early postmenopausal women: a
randomized double-blind placebo-controlled study. J Bone
Mineral Res 2002;17:190412.
79. Mense SM, Hei TK, Ganju RK. Phytoestrogens and breast
cancer prevention: possible mechanisms of action. Environ
Health Perspect 2008;116:42633.
80. Dip R, Lenz S, Gmuender H. Pleiotropic combinatorial
transcriptomes of human breast cancer cells exposed to
mixtures of dietary phytoestrogens. Food Chem Toxicol
81. Sakamoto T, Horiguchi H, Oguma E. Effects of diverse dietary
phytoestrogens on cell growth, cell cycle and apoptosis in
estrogen-receptor-positive breast cancer cells. J Nutr Biochem
82. Fremont L. Biological effects of resveratrol. Life Sci
83. Cornwell T, Cohick W, Raskin I. Dietary phytoestrogens and
health. Phytochemistry 2004;65:9951016.
84. Cos P, De Bruyne T, Apers S, Vanden Berghe D, Pieters L,
Vlietinck AJ. Phytoestrogens: recent developments. Planta
Med 2003;69:58999.
85. Wiseman H. The bioavailability of non-nutrient plant factors:
dietary flavonoids and phyto-oestrogens. Proc Nutr Soc
86. Fahey JW, Wehage SL, Holtzclaw WD, Kensler TW, Egner PA,
Shapiro TA, et al. Protection of humans by plant glucosino-
lates: efficiency of conversion of glucosinolates to isothio-
cyanates by the gastrointestinal microflora. Cancer Prev Res
87. Oerlemans K, Barrett DM, Bosch Suades C, Verkerk R, Dekker
M. Thermal degradation of glucosinolates in red cabbage.
Food Chem 2006;95:1929.
88. Jeffery EH, Araya M. Physiological effects of broccoli
consumption. Phytochem Rev 2009;8:28398.
89. Cartea ME, Velasco P. Glucosinolates in brassica foods:
bioavailability in food and significance for human health.
Phytochem Rev 2008;7:21329.
90. Traka M, Mithen R. Glucosinolates, isothiocyanates and
human health. Phytochem Rev 2009;8:26982.
91. Hayes JD, Kelleher MO, Eggleston IM. The cancer
chemopreventive actions of phytochemicals derived from
glucosinolates. Eur J Nutr 2008;47:7388.
92. Conaway CC, Getachun SM, Liebes LL, Pusateri DJ, Tophan DK,
Botero-Omary M, et al. Disposition of glucosinolates and
sulphoraphanes in human after ingestion of steam and fresh
broccoli. Nutr Cancer 2001;38:16878.
93. Vig AP, Rampal G, Singh TS, Arora S. Bioprotective effects of
glucosinolates A review. LWT Food Sci Technol
94. Institute of Medicine. Dietary reference intakes for energy,
carbohydrate, fiber, fat, fatty acids, cholesterol, protein, and
amino acids. National Academy Press, 2002.
95. Pawlosky RJ, Hibbeln JR, Novotny JA, Salem Jr N. Physiological
compartmental analysis of alpha-linolenic acid metabolism in
adult humans. J Lipid Res 2001;42:125765.
96. Miggiano GA, Gagliardi L. Diet, nutrition and rheumatoid
arthritis. Clin Ter 2005;156:11523.
97. Zak A, Tyrzicka E. Pathophysiology and clinical significance of
polyunsaturated fatty acids n-3 family [in Czech]. Cas Lék
Cesk 2005;144:618.
98. Mori TA, Beilin LJ. Omega-3 fatty acids and inflammation. Curr
Atheroscler Rep 2004;6:4617.
99. Simopoulos AP, Leaf A, Salem Hr N. Workshop statement on
the essentiality of and recommended dietary intakes for
omega-6 and omega-3 fatty acids. Prostaglandins Leukot
Essent Fatty Acids 2000;63:11921.
100. Choung MG, Baek IY, Kang ST, Baek IY, Kang ST, Han WY,
et al. Isolation and determination of anthocyanins in seed
168 Gupta and Prakash: Bioactive compounds in health
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
coats of black soybean (Glycine max (L.) Merr.). J Agric Food
Chem 2001;49:584851.
101. Zafra-Stone S, Yasmin T, Bagchi M, Chatterjee A, Vinson JA,
Bagchi D. Berry anthocyanins as novel antioxidants in human
health and disease prevention. Mol Nutr Food Res
102. Xia X, Ling W, Ma J, Xia M, Hou M, Wang Q, et al. An
anthocyanin-rich extract from black rice enhances
atherosclerotic plaque stabilization in apolipoprotein
E-deficient mice. J Nutr 2006;136:22205.
103. Qin Y, Xia M, Ma J, Hao Y, Liu J, Mou H, et al. Anthocyanin
supplementation improves serum LDL- and HDL-cholesterol
concentrations associated with the inhibition of cholesteryl
ester transfer protein in dyslipidemic subjects. Am J Clin Nutr
104. Ghosh D, Konishi T. Anthocyanins and anthocyanin-rich
extracts: role in diabetes and eye function. Asia Pac J Clin Nutr
105. Akkarachiyasit S, Charoenlertkul P, Yibchok-Anun S,
Adisakwattana S. Inhibitory activities of cyanidin and its
glycosides and synergistic effect with acarbose against
intestinal α-Glucosidase and pancreatic α-Amylase. Int J Mol
Sci 2010;11:338796.
106. Gibson GR, Roberfroid MB. Dietary modulation of the human
colonic microbiota: introducing the concept of prebiotics. J
Nutr 1995;125:140112.
107. MacFarlane GT, Cummings JH. Probiotics and prebiotics: can
regulating the activities of intestinal bacteria benefit health?
Br Med J 1999;318:9991003.
108. Baffoni L, Biavati B. Ecologia microbica dellapparato
digerente. In: Biavati B, Sorlini C, editors. Microbiologia
agroambientale. Milan: Casa Editrice Ambrosiana,
109. Henke JM, Bassler BL. Bacterial social engagements. Trends
Cell Biol 2004;14:64856.
110. Sansonetti PJ. War and peace at mucosal surfaces. Nat Rev
Immunol 2004;4:95364.
111. Sanders ME. Considerations for use of probiotic bacteria to
modulate human health. J Nutr 2000;130:384S90S.
112. Mercenier A, Pavan S, Pot B. Probiotics as biotherapeutic
agents: present knowledge and future prospects. Curr Pharm
Des 2002;8:99110.
113. Gilliland SE, Speck ML. Antagonistic action of Lactobacillus
acidophilus toward intestinal and food-borne pathogens in
associative cultures. J Food Prot 1977;40:8203.
114. De Roos NM, Katan MB. Effects of probiotic bacteria on
diarrhea, lipid metabolism, and carcinogenesis: a review of
papers published between 1988 and 1998. Am J Clin Nutr
115. Gupta C, Prakash D, Rostagno MH, Callaway TR. Synbiotics:
promoting gastrointestinal health. In: Prakash D, Sharma G,
editors. Phytochemicals of nutraceutical importance. UK: CABI
International Publishers, 2014:6178.
116. Prakash D, Sharma G. Phytochemicals of nutraceutical
importance. In: Prakash D, Sharma G, editors. UK: CABI
International Publishers, 2014:1364.
117. Global Nutraceuticals market. Infiniti research
limited November 2013. Report Code: Infiniti Research Limited
3112, 20142018.
118. Challener C. Speciality supplements are the bright spot
in US dietary supplement market. Chem Market Rep
119. Jones M. Controlled delivery technology in nutraceutical
applications: a users perspective. Nutra Cos 2003.
Useful links and database
Gupta and Prakash: Bioactive compounds in health 169
Brought to you by | De Gruyter / TCS
Authenticated |
Download Date | 8/19/14 7:54 AM
... These pathways deal with energy metabolism, cellular regeneration and repair, modulation of the immune response, elimination of unwanted metabolites or cancer prevention (Linnewiel-Hermoni et al., 2015). Some of these vital plant compounds (e.g., flavonoids, anthocyanins, carotenoids) contain aromatic moieties, conjugated systems or both in their chemical structure (Shimizu et al., 2010;Gupta and Prakash, 2014). Such structures are of great significance to effectively participate in electron transferring or redox mediating processes in biotic and abiotic reactions. ...
Due to the pandemics of COVID-19, herbal medicine has recently been explored for possible antiviral treatment and prevention via novel platform of microbial fuel cells. It was revealed that Coffea arabica leaves was very appropriate for anti-COVID-19 drug development. Antioxidant and anti-inflammatory tests exhibited the most promising activities for C. arabica ethanol extracts and drying approaches were implemented on the leaf samples prior to ethanol extraction. Ethanol extracts of C. arabica leaves were applied to bioenergy evaluation via DC-MFCs, clearly revealing that air-dried leaves (CA-A-EtOH) exhibited the highest bioenergy-stimulating capabilities (ca. 2.72 fold of power amplification to the blank). Furthermore, molecular docking analysis was implemented to decipher the potential of C. arabica leaves metabolites. Chlorogenic acid (-6.5 kcal/mol) owned the highest binding affinity with RdRp of SARS-CoV-2, showing a much lower average RMSF value than an apoprotein. This study suggested C. arabica leaves as an encouraging medicinal herb against SARS-CoV-2.
... They have a great impact on immune system and thus regulate it to avert many maladies. They serve as antioxidants, anti-bacterial, anti-fungal, anti-aging, anti-cancer, anti-spasmodic, antiinflammatory and anti-allergic [29]. ...
Full-text available
Introduction: Medicinal plants have been the source of medicine to all civilizations for hundreds of years. In classical medicine, Elymus repens (Poaceae) is consumed as a diuretic, emollient and tonic. It also soothes the pain and spasm in the urinary tract as well as treats the condition of urolithiasis (formation of kidney stones) and urinary tract infections (UTI). In Chinese folk medicine, T. angustifolia is employed to improve the microcirculation, improve body’s defense mechanism, activate contractions of uterus, heal atherosclerosis, treat wounds and promote the differentiation and trigger the division of keratinocytes in humans. The traditional healers recommend C. edulis to cure hypertension, rheumatism, leprosy, diabetes, infections, gastric issues and Alzheimer disease. Objectives: This study was aimed to investigate different phytochemical constituents in methanolic extracts of E. repens (plant body and roots), T. angustifolia (stem and fruiting body) and C. edulis. Methodology: Phytochemical potentials of methanolic extracts of plants were investigated using standard procedures. Results: Phytochemical analysis of E. repens crude methanol extract confirmed the existence of tannins, saponins, flavonoids and anthraquinones. However, phenols were absent in methanol extract of roots. T. angustifolia stem contained anthraquinones. Tannins, saponins, phenols and flavonoids were absent from T. angustifolia stem. C. edulis contains saponins, tannins, flavonoids and anthraquinones except phenols. Conclusion: Results of this study shows that E. repens, T. angustifolia and C. edulis are enriched with different phytochemical constituents hence validating their uses for the treatment of various diseases.
... ADT drugs include inhibitors of androgen synthesis and androgen receptor activation [4]. However, continuous ADT results in castration-resistant prostate cancer, with an increased risk of mortality [5]. In this regard, development of therapeutic adjuvants with fewer side effects to complement traditional treatment methods for prostate cancer is important [6,7]. ...
Full-text available
Although androgen deprivation therapy is mainly used for its treatment, the mortality rate of prostate cancer remains high due to drug resistance. Hence, there is a need to discover new compounds that exhibit therapeutic effects against prostate cancer with minimum side effects. Hesperidin is a flavonoid carbohydrate isolated from citrus fruits. It has antiproliferative effects in various cancer types; however, whether it can modulate cell proliferation by modulating the key targets of cancer therapy, including intracellular signaling pathways and oxidative stress, remains unknown. Therefore, we confirmed that hesperidin suppressed the proliferation of prostate cancer cells, PC3 and DU145. Hesperidin induced cell death by regulating the cell cycle and inhibited the expression of proliferating cell nuclear antigen, a cell proliferation marker. Hesperidin also promoted the generation of reactive oxygen species and induced mitochondrial membrane depolarization and endoplasmic reticulum stress in prostate cancer cells. Moreover, as hesperidin increased Ca2+ levels in prostate cancer cells, we co-treated the inositol 1,4,5-trisphosphate receptor inhibitor, 2-aminoethyl diphenyl borate (2-APB), with hesperidin. Notably, 2-APB restored cell proliferation, which was reduced to control levels by hesperidin. In addition, hesperidin inhibited the activation of the phosphoinositide 3-kinase and mitogen-activated protein kinase signaling pathways. Hesperidin also enhanced the anticancer effects of the chemotherapeutic agent, cisplatin, in both PC3 and DU145 cells. Taken together, these results suggest that hesperidin can be used as a potential therapeutic adjuvant in prostate cancer as it can inhibit cell proliferation by mediating oxidative stress and increasing Ca2+ levels.
... Flavonoids and isoflavonoids are wellknown natural products with extensive pharmacological activities and extremely low toxicity (Wang et al., 2020). More importantly, they possess a wide range of biological activities, such as antibacterial, antifungal, antiviral (Dastidar et al., 2004;Orhan et al., 2010), antitumour (Kopustinskiene et al., 2020), antiinflammatory (Sychrová et al., 2020) and antiaging activities (Gupta et al., 2014). ...
Full-text available
The leaves and bark of Ficus sagittifolia have been used as a cure for stomach and pulmonary disorders, respectively. The bark is edible and is taken against colic. From the leaves of F. sagittifolia, a steroidal glycoside named Stigmast-5,22-diene-3-O-β-D-glucopyranoside 1 and three isoflavonoids named 5-hydroxy-3-(4-hydroxyphenyl)-7-methoxy-4H-chromen-4-one 2, 5-hydroxy-3(4-hydroxylphenyl)-8,8-dimethylpyrano[2,3-f]-chromen-4(8H)-one 3 and 5-hydroxy-3-(4-hydroxyphemyl)-8,8-dimethylpyrano[3,2-g}-chromen-4(8H)-one 4 were isolated, and this is the first report of the isolation of these compounds from this plant. The structural elucidation of the compounds was based on 1D and 2D NMR, IR and MS data analyses. Compounds 1 and 2 inhibited the growth of Pseudomonas aeruginosa and Aspergillus Niger at 6.25 mg/mL, respectively while compounds 2 and 4 were active against Helicobacter pylori at 6.25 mg/mL. These findings corroborate the ethno-medicinal use of F. sagittifolia leaves as a treatment for stomach disorders.
There is a diverse array of berries found wild in tropical, temperate and arid ecosystems or cultivated in both field and control environments across the globe. It is evident berry genetics, species, growth environment, cultivation techniques, postharvest management practices, packaging and processing affect the nutritional and functional properties of berries. The level and composition of functional and nutritional compounds in berries are primarily responsible for their health promotive properties. In particular, anthocyanins and flavonoids are shown to be very effective in managing, treating and reducing CVD risks in humans; and the effects are even more pronounced when combined with personalized nutrition or diets and physical activities. Globally, there is a steady increase in CVD incidences and associated deaths. There is a need for interventive strategies to reduce these CVD incidences and associated deaths. Personalized nutrition and diets containing increase levels or consumption of fresh berries, berry-based functional foods, nutritional products, or nutraceuticals could be an effective long-term strategy to reduce CVD disease risks, as well as improve population health globally.
Even as this phase marks the possibility of new beginnings, the patient and caregiver’s transition to survivorship is often fraught with anxiety, feelings of abandonment by the oncology team, and fears of a cancer recurrence. Individuals must adjust to changes in their relationships with healthcare providers, family caregivers, and family. This chapter covers the typical concerns of new survivors and family caregivers and the clinical need for nursing interventions to provide knowledge, skills, and support so they may transition to a new normal future with confidence. A psychosocial program is also proposed. It would offer self-management knowledge and skills to deal with residual side effects and identify early changes in physical health. Other topics would include coping and behavioral strategies to maintain emotional equanimity and to reduce fears of a cancer recurrence, strategies to maintain supportive relationships, and critical information about adopting healthy lifestyle behaviors. Meta-analyses and RCTs serve as the scientific predicate for suggested nursing interventions.KeywordsCognitive-behavioral strategiesMindfulness stress reducing interventionsSelf-management skillsStrategies of communicationLoss of professional securityFear of cancer recurrenceSide effectsSymptomsMeaning making
Plants taken as food provide the body with nutrients that strengthen the immune system. The immune system recognizes, tolerates, and resists infections or toxins by activating specific antibodies or sensitized white blood cells. COVID-19 is a severe acute respiratory disorder that is caused by the virus SARS-CoV-2. It has been reported that innate immunity plays a role in mitigating the severity of the disease, thus strengthening the immune system is paramount to resisting the infection. This study aimed to identify and document foods commonly consumed in Northern Nigeria that are claimed to possess immune-stimulatory effects. Literature of plants that are commonly used as food was studied. Data was collected from literature searches of the PubMed, PubChem, and Google Scholar databases using keywords that include immunity, immune-stimulatory, phytochemicals, and micronutrients. Thirty commonly consumed plants belonging to eighteen families were selected based on how widely used they are in the region. They are reported to contain immune-boosting phytonutrients such as carotenoids, flavonoids, and micronutrients such as Vitamin C and Zinc, which have antioxidant and anti-inflammatory properties. The study showed that the plants that are commonly consumed in Northern Nigeria contained phytochemicals and micronutrients, which are necessary for boosting immunity and thus could be the reason for the low COVID-19morbidity experienced in the region.
The growing global population demands increased food production, and the demand for plant- and animal-based foods is rising. The modern food and agricultural industries globally contribute about 17.3 billion metric tonnes of carbon dioxide per year, 57% of which is from animal-based and 29% from plant-based food production. Thus, the animal-based food we consume significantly contributes to greenhouse gas emissions that have far-ranging environmental and health impacts. This has led to a big drive worldwide toward sustainable food sources, which can meet the growing demands for food in future reducing animal-based food consumption. Plant-based foods that use markedly fewer natural resources and are less demanding on the environment than animal-based foods are considered excellent sustainable food source. This chapter discusses the current trend of plant-based foods, the nutrients and health benefits obtained from plant-based food, and their potential as a sustainable food source for the future.
Flavonoids are bioactive compounds isolated from a variety of plants. The most interesting property of these phenolic compounds is their ability to reduce free radicals or antioxidant activity. Increased free radicals drive the pathology for a number of chronic diseases. They can be prevented or managed by the judicious use of antioxidants. The proven benefits of flavonoid‐rich diet have encouraged scientists to explore the possible pathways through which these compounds exhibit their action. Flavonoid content of food is affected by the methods of harvesting and processing, making isolation of these compounds an important aspect. Additionally, isolation helps to formulate these compounds as targeted agents for pharmacotherapy. The major concern, however, is the amount of flavonoids actually reaching the systemic circulation. The structural configuration, number of hydroxyl groups, and position of functional groups largely determine the bioavailability, metabolism, and mechanism of action of the flavonoids. Hence, scientists have made continuous attempts to modulate the uptake and metabolism of these phytoantioxidants to improve their bioavailability and strengthen their activity. Coadministration with substances that enhance absorption and improve water solubility, structural alterations, and nanotechnology is one of the methods used to achieve the target. Nutraceuticals are a promising therapeutic area with flavonoids as a major contributor. Their antioxidant properties are claimed to improve anything from skin conditions to cardiac and metabolic disorders. However, their regulated and meticulous use as therapeutic agents is required to ensure the benefit of the end users.