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Therapeutic Utilization of Bioactive Compounds and Phytochemicals
present in the Stevia rebaundiana L. (Yamamoto et al., 1985). The strychnine (Strychnosnux vomica L.)
molecule is a potent stimulator of central nervous system (Muhtadi, 1986).
Figure 2. Vitamin E
Figure 3. Saponin
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Therapeutic Utilization of Bioactive Compounds and Phytochemicals
Figure 4. Tannic Acid (Tannin)
There are some bioactive molecule whose uses in treating diseases have been known from ancient
times, but now-a-days, their range have been extended for treating other diseases. The bioactive molecule
rohitukine present in Dysoxylum binectarifarum L. traditionally used to treat rheumatic disease, however, its characteristics presently exploited for the treating the cancer (Wang, 2000). Likewise, the rutin
compound (Eucalyptus macrorhyncha L.) previously used as insect repellant but its utilization as drugs
for treating the fragileness of capillaries is commendable (Levitan, 1951). The compound gingkolide
A has been exploited for asthma and in present conditions it has been consumed as drug for increasing
the memory which is mostly useful for Alzheimer’s patient (LeBars et al., 1997). The plant bioactive
molecule (hypericin) utilized to combat against depression. Now, it has been used to cure viral diseases
(Gulick, 1999). Though, picroside (Picrorhiza kurroa L.) recommended in fever and dyspepsia but
it can be consumed as protective agent of liver (Vaidya et al., 1996). The sanguinarin extracted from
Sanguinaria canadensis L. traditionally consumed by the people for improving the skin and to purify
their bloods. Besides this, it has been recommended for curing the gum diseases and controlling plaque
(Shamma, 1972). From Taxus baccata L., taxol drug has been isolated and prepared which is utilized in
curing spasms and rheumatid disease problems. But now-a-days, it is used in chemotherapy of patients
(Legha, 1990; Suffness, 1995).
Some of the bioactive molecules have been identified newly from various plants possessing therapeutic
uses. For example, khellin extracted from the plant Ammi visnaga L. is a potent vasodilator (Ubeda &
Villar, 1989). Similarly, the Aristolochia indica L. (Aristolochic acid) used to treat the fertility issues
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Figure 5. Morphine (Alkaloid)
Therapeutic Utilization of Bioactive Compounds and Phytochemicals
(Mathur et al., 1980). Naringenin (Citrus paradisi) prescribed for the persons suffering from bacterial
infections and cancer (Ameer et al., 1996). Hesperidine (Citrus sinensis L.) has been consumed by the
diabetic patients and it is used for curing viral disease (Garg et al., 2001). Forskolin (Coleus forskolii
L.) also used as therapeutic agent in blood pressure related problems as well as in spasm treatment (Ammon & Mueller, 1985; De Souza et al., 1983). The plant of Betula alba possessed betulinic acid which
is effective in the treatment of AIDS and act as tumor suppressor agent (Cichewicz & Kouzi, 2004).
Camptothecin derived from the plant Camptotheca acuminata L. showed impressive activity against
the tumor cells by inhibiting their growth (Wall & Wani, 1980). The skeletal muscle of the body can be
relaxed at the time of disease by using the drug cissampareine (Cissampelos pareira L.) (Kupchan et
al., 1965). The bioactive molecules shikonin, ellipticine, lycopene and lapachol used in the treatment of
cancer which has been derived from Lithspermum erythrorhizon L., Ochrosia elliptica L., Lycoperscion
esculentum L. and Tabebuia avenallanedae L., respectively (Block et al., 1974; Paoletti et al., 1980; Rao
et al., 1998; Chen et al., 2003; Garbett & Graves, 2004). Lycopene, cynarin, resveratrol and carnosol drug
possesses antioxidant activities and these compounds extracted from the following plants: Lycoperscion
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Therapeutic Utilization of Bioactive Compounds and Phytochemicals
esculentum L., Cynara scolymu L., Polygonum cuspldatum L. and Rosmarinus officianalis L. (Aruoma
et al., 1992; Gebhardt, 1997; Rao et al., 1998; Bhat et al., 2001).
Figure 6. Quinine (Alkaloid)
COMMON PLANT-BASED NATURAL BIOACTIVE MOLECULES
Resveratrol
Among all the bioactive molecules, this is one of the molecules which are present in grapes and other
plants also possessing the antioxidant properties (Mukherjee et al., 2010). They act as antioxidants by
inhibiting the production of ROS and RNS in the body and enhance the metabolic pathways which
help in the reduction of harmful radicals. Besides this, they also have the anti-inflammatory properties
(Lastra & Villegas, 2005). They also involved in the repairing of DNA, anti-aging, regulating cell cycle
and other various activities by NAD-dependent protein deacetylases regulation (Borra et al., 2005). In
females, it plays important role as it prevents the bone from losing their bone density due to the increasing age (Baxter, 2008).
Epigallo-Catechin-3-Gallate
Green tea has gained popularity due to its antioxidant properties. Though, they decrease the production
of free radicals which cause damage to the cells but also involved in the prevention of inflammatory
processes in the cell. The bioactive molecule Epigallo-Catechin-3-Gallateextracted from the leaves also
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Therapeutic Utilization of Bioactive Compounds and Phytochemicals
Table 1. Role of Bioactive molecules in treatment of major Chronic Diseases
Diseases Bioactive Molecules Uses References
Polyphenols
Carotenes
Vitamins C
Vitamin E
Diabetes
Cancer
Neurodegenerative
Diseases
CVD
*CVD= Cardiovascular Diseases, BP=Blood Pressure
Cinnamaldehyde Epigallocatechin
Chlorogenic acid
Lycopene
Zeaxanthin
Carotene
β-cryptoxanthin
Curcumin
Lycopene Cell growth inhibitor Kucuk et al., (2002)
6-Shogaol
Ginkgolide B
Quercetin Anti-oxidant, antiviral Li et al., (2016)
Resveratrol Enhance inflammation Tomé-Carneiro et al., (2013)
Lycopene
Vitamin C
Vitamin E
Omega 3 Fatty Acids Reduces BP levels Jain et al., (2015)
Antioxidant Kiec-Wilk & Mykka, (2008)
Reducing Hypoglycemic effect,
protect the inhibition of amylase
and increasing insulin efficiency
Prevent type II diabetes mellitus Coyne et al., (2005)
Preventing the formation of
tumor
Reduces the production of
IL-1β, prostaglandin E2, and
TNF-α
Decreases the NF-κβ and
increasing Bcl2
Reducing bad cholesterol level,
antioxidant
Reducing bad cholesterol level,
antioxidant
Inhibiting or decreases the lipid
peroxidation
He et al., (2006); Zhu et al.,
(2017); Meng et al., (2013)
Dhillon et al., (2008); BayetRobert et al., (2010)
Ha et al., (2012)
Gu et al., (2012)
Hadley et al., (2003); Bohn et
al., (2013); Story et al., (2010)
Chambial et al., (2013)
Saremi & Arora, (2010)
protects the heart related diseases and works against the diseases caused by virus (Chacko et al., 2010;
Singh et al., 2011).
There are several DNA methyltransferase enzymes which targets the Cytosine-phosphate-Guanine
rich areas by introducing methyl groups to them which sometimes acts as transcriptional inhibitors
or inducers depending on the amino acid which gets methylated (Singh et al., 2011). However, these
enzymes are also involved in the aging process. The bioactive molecule Epigallo-Catechin-3-Gallate
works against this and limits the expression of these enzymes and act as anti-aging agent. It has been
known that DNA methylation in the cells sometimes lead to tumor formation in the body as some of
the anti-tumor gene gets suppressed. This molecule also prevents the tumorigenesis by restricting this
enzyme. Another enzyme i.e., Glutathione-S-transferase are known to remove the drugs from the body.
This enzyme expression increases in the presence of this bioactive molecule (Yang et al., 2010).
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Therapeutic Utilization of Bioactive Compounds and Phytochemicals
Curcumin
This is one of the bioactive molecules present in the turmeric plant which has a long history in curing
diseases. The importance of the turmeric in the ancient medicinal system of India provides the diseases
which can be cured from this. In India, it has been used in cooking any meal along with other spices. It
is evident from the recent studies that it provides protection against various diseases (Gupta et al., 2013).
They also inhibit the inflammation and also act as anti-tumor agent (Hatcher et al., 2008).
Lycopene
This is the active compound of tomato plant which provides its characteristics color red to the plant (Story
et al., 2010). It is evident from various studies that it increases the level of good cholesterol in body and
decreases the bad cholesterol levels. It also possesses antioxidant activity (Hadley et al., 2003; Story et
al., 2010; Bohn et al., 2013). One of the studies claimed that consumption of lycopene on a daily basis
improved the condition of cardiovascular diseases (Gajendragadkar et al., 2014).
Ascorbic Acid (Vitamin C)
Vitamins constitute the micronutrient part in the body whose small quantity has been required in the
body. Most of the vitamins have been consumed from the dietary sources such as lemon, orange and
various other fruits and vegetables having the citric acid content is high consists of Vitamin C (Chambial
et al., 2013). They have great antioxidant activity which helps in increasing the metabolic rates as well
as protect the heart from various diseases (Chambial et al., 2013).
Omega 3 Fatty Acids
This is one of the classes of fatty acids which is found in plants and animals both (Tur et al., 2012). They
possess the ability to bind to the membranes of the body along with that they decrease the inflammation
in the body by reducing the cytokine production (Swanson et al., 2012). They are used for maintaining
the B.P. along with decrease in the triglyceride levels and they regulate various metabolic pathways
(Jain et al., 2015).
CONCLUSION
It has been seen that bioactive molecules extracted from either medicinal plants or normal plants act as
therapeutic agents in various diseases. Most of the phytochemicals or bioactive molecules have been
known traditionally, however, their utilization in other diseases extended. The intake of these molecules
either directly or indirectly confers various health benefits. The benefits provided by them such as providing protection against various diseases caused by the microorganisms, CVD, increasing the metabolic
activity, reducing inflammatory activity etc. makes them consumable on a daily basis. Though, they are
known to provide benefits to the human health, still, it have been less known about their mechanism.
Recent studies points out towards the basic pathways of metabolism which have been affected from their
consumption. Such as the inflammation pathway which includes cytokine, the pathway of lipid metabolism
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Therapeutic Utilization of Bioactive Compounds and Phytochemicals
which reduces the level of bad cholesterol and decreasing the risk of heart diseases, reducing the production of free radicals etc. They are the part of diet traditionally and now; they are important constituent of
medicines. The bioactive molecules which have been extracted from the higher plants proven to be more
successful as therapeutic agents in comparison to those extracted from another organism. Though, they
are very beneficial for the human health, still, their mixtures with other molecules are still challenging
as their reaction with other compounds could be either harmful or beneficial.
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