Download 3-Punicalagin, a polyphenol in pomegranate juice, downregulates

Kingdom of Saudi Arabia
Ministry of Higher Education
University of Tabuk
Prepared by / Amjad Mofdi Alhamadi
Academic No/ 321002174
Under supervision of /
Dr/ Zahed Khorshid
Definition
Plants have the ability to synthesize a wide variety of chemical
compounds that are used to perform important biological functions, and to
defend against attack from predators such as insects, fungi and
herbivorous mammals.( Tabsell CL et al ,2006 )
Introduction
medicinal plants include a various types of
plants used in herbalism and some of these
plants have a medicinal activities. These
medicinal plants consider as a rich resources of
ingredients which can
be used in drug
development and synthesis. Besides that these
plants play a critical role in the development of human cultures around
the whole world. Moreover, some plants consider as important source of
nutrition and as a result of that these plants recommended for their
therapeutic values. These plants include ginger, green tea, walnuts and
some others plants. Other plants their derivatives consider as important
source for active ingredients which are used in aspirin and toothpaste.
(Rasool Hassan BA,2012)
Characteristics of Medicinal Plants
Medicinal plants have many characteristics when used as a treatment, as
follow:
• Synergic medicine- The ingredients of plants all interact simultaneously,
so their uses can complement or damage others or neutralize their
possible negative effects.
• Support of official medicine- In the treatment of complex cases like
cancer diseases the components of the plants proved to be very
effective.
• Preventive medicine- It has been proven that the component of the
plants also characterize by their ability to prevent the appearance of
some diseases. This will help to reduce the use of the chemical remedies
which will be used when the disease is already present i.e., reduce the
side effect of synthetic treatment. (Rasool Hassan B A , 2012)
Prevalence of use
A survey released in May 2004 by the National Center for
Complementary and Alternative Medicine focused on who used
complementary and alternative medicines (CAM), what was used, and
why it was used. The survey was limited to adults, aged 18 years and
over during 2002, living in the United States. According to this survey,
herbal therapy, or use of natural products other than vitamins and
minerals, was the most commonly used CAM therapy (18.9%) when all
use of prayer was excluded.( Barnes ,at el, 2004)
Herbal remedies are very common in Europe. In Germany, herbal
medications are dispensed by apothecaries (e.g., Apotheke). Prescription
drugs are sold alongside essential oils, herbal extracts, or herbal
teas.(James A,2000)
Scientific Classification:
Kingdom:
Plantae
(unranked):
Angiosperms
(unranked):
Eudicots
(unranked):
Rosids
Order:
Myrtales
Family:
Lythraceae
Genus:
Punica
Species:
P. granatum
botanical name Punica granatum, is a fruitbearing deciduous shrub or small tree growing
between 5 and 8 m (16–26 ft) tall. In the
Northern Hemisphere, the fruit is typically in
season from September to February, and in the
Southern Hemisphere from March to May. As intact arils or juice,
pomegranates are used in cooking, baking, meal garnishes, juice blends,
smoothies, and alcoholic beverages, such as cocktails and wine.The
pomegranate is considered to have originated in the region between the
himalayas and Egypt, and has been cultivated since ancient times in
India, Persia, Mesopotamia, Turkey and the Arabian Peninsula. It is
mentioned in many ancient texts, notably in Babylonian texts and the
Book of Exodus. It was introduced into Latin America and California by
Spanish settlers in 1769. Today, it is widely cultivated throughout the
Mediterranean region of southern Europe, the Middle East and Caucasus
region, northern Africa and tropical Africa, the Indian subcontinent,
Central Asia, and the drier parts of southeast Asia. It is also cultivated in
parts of California and Arizona. In recent years, it has become more
common in the commercial markets of Europe and the Western
Hemisphere.( Larua,1980)(Morton,1987)
Description
An attractive shrub or small tree growing 6 to 10 m high, the
pomegranate has multiple spiny branches, and is extremely long-lived,
with some specimens in France surviving for 200 years. Punica granatum
leaves are opposite or subopposite, glossy, narrow oblong, entire, 3–
7 cm long and 2 cm broad. The flowers are bright red, 3 cm in diameter,
with three to seven petals. Some fruitless
varieties are grown for the flowers alone.
The edible fruit is a berry and is between a
lemon and a grapefruit in size, 5–12 cm in
diameter with a rounded shape and thick, reddish skin. The number of
seeds in a pomegranate can vary from 200 to about 1400 seeds. Each
seed has a surrounding water-laden pulp — the edible sarcotesta that
forms from the seed coat — ranging in color from white to deep red or
purple. The seeds are "exarillate", i.e., unlike some other species in the
order, Myrtales, there is no aril. The sarcotesta of pomegranate seeds
consists of epidermis cells derived from the integument. The seeds are
embedded
in
a
white,
(Morton,1987)(Dahlgren,1984)
spongy,
astringent
membrane.
Cultivation
Punica granatum is grown as a fruit crop plant, and as ornamental trees
and shrubs in parks and gardens. Mature specimens can develop
sculptural twisted bark multiple trunks and a distinctive overall form.
Pomegranates are drought-tolerant, and can be grown in dry areas with
either a Mediterranean winter rainfall climate or in summer rainfall
climates. In wetter areas, they can be prone to root decay from fungal
diseases. They can be tolerant of moderate frost, down to about −12°C
(10°F). (M.L. et al, 2012)
Uses of pomegranate In traditional medicine:
In the Indian subcontinent's ancient Ayurveda
system
of
traditional
medicine,
the
pomegranate has been used extensively as a
source of traditional remedies.(K.K.Jindal,200)
The rind of the fruit and the bark of the pomegranate tree are used as a
traditional remedy against diarrhea, dysentery, and intestinal parasites.
The seeds and juice are considered a tonic for the heart and throat, and
classified as having bitter-astringent taste plus a, range of taste from
sweet to sour, depending on ripeness. Thus, pomegranate is considered
a healthful counterbalance to a diet high in sweet-fatty (kapha or earth)
components. Especially when sweet, pomegranate fruit is nourishing for
(pitta or fire) systems and is considered a blood builder. The astringent
qualities of the flower juice, rind, and tree bark are considered valuable
for a variety of purposes, such as stopping nose bleeds and gum bleeds,
toning skin, (after blending with mustard oil) firming-up sagging breasts,
and treating hemorrhoids. Pomegranate juice (of specific fruit strains) is
also used as an eyedrop, as it is believed to slow the development of
cataracts. Pomegranate extracts (alkaloids) are used to treat intestinal
parasite infestations in some nations. (Vasent Lad,2002)
health benefits of pomegranates :
Pomegranate ellagitannins, also called punicalagins, have shown freeradical scavenging properties in laboratory experiments and with potential
effects on humans. Punicalagins are absorbed into the human body and
may have dietary value as antioxidants, but conclusive proof of efficacy in
humans has not been shown. During intestinal metabolism by bacteria,
ellagitannins and punicalagins are converted to urolithins, which have
unknown biological activity in vivo.
(Kulkarni,etal,2007)(Heber,2008)(Seeram,etal,2006)(Mertens,etal,2006)(B
ialonsks,et al,2006)(Larrosa, et al, 2009)
In preliminary laboratory research and clinical
trials, juice of the pomegranate may be effective
in reducing heart disease risk factors, including
LDL oxidation, macrophage oxidative status, and
foam cell formation. In mice, "oxidation of LDL
by peritoneal macrophages was reduced by up to 90% after pomegranate
juice consumption...".(Aviram,et al,2004)(Esmailzadeh,et al,2004(Kaplan,
et al.2001)(Aviram, et al,2000)
In a limited study of hypertensive patients, consumption of pomegranate
juice for two weeks was shown to reduce systolic blood pressure by
inhibiting serum angiotensin-converting enzyme. Juice consumption may
also inhibit viral infections while pomegranate extracts have antibacterial
effects
against
dental
plaque.(Aviram,
Despite
limited research data, manufacturers and
al,2004)(Menezes, et al,2006)
et
al,2001)(Neurath,
marketers
et
of
pomegranate juice have liberally used evolving research results for
product promotion, especially for putative antioxidant health benefits. In
February 2010, the FDA issued a Warning Letter to one such
manufacturer, POM Wonderful, for using published literature to make
illegal
claims
of
benefits.(Starling,2010)
unproven
antioxidant
and
antidisease
Chemical composition of pomegranate :
A 100-g serving of pomegranate seeds provide 12% of the Daily Value
(DV) for vitamin C and 16% DV for vitamin K, and contains polyphenols,
such as ellagitannins and flavonoids.Pomegranate seeds are excellent
sources of dietary fiber which is entirely contained in the edible seeds.
People who choose to discard the seeds forfeit nutritional benefits
conveyed by the seed fiber and micronutrients.(Schubert,1999)
Pomegranate seed oil contains punicic acid (65.3%), palmitic acid
(4.8%), stearic acid (2.3%), oleic acid (6.3%), and linoleic acid (6.6%).
( Shay, et al,1999)
Juice, seeds, and peel apparently contain steroid hormones, including
estrone, although this is debated between Korean teams.
(Erich,et al,1999)(Young,et al,2010)(Don Woong,et al,2006)
Phenolic content:
In juice :
The
most
abundant
polyphenols
in
pomegranate juice are the hydrolyzable
tannins called ellagitannins formed when
ellagic acid and/or gallic acid binds with a
carbohydrate.
The
different
pomegranate
ellagitannins (also known as punicalagins) are: granatin A and B,
punicacortein A, B, C and D, 5-O-galloylpunicacortein D, punicafolin,
punigluconin, punicalagin, 1-alpha-O-galloylpunicalagin, punicalin and
2-O-galloyl-punicalin.The red color of juice can be attributed to
anthocyanins, such as delphinidin, cyaniding, and pelargonidin glycosides
(delphinidin 3-glucoside and 3,5-diglucoside, cyanidin 3-glucoside and
3,5-diglucoside and pelargonidin 3-glucoside and 3,5-diglucoside).
Generally, an increase in juice pigmentation occurs during fruit ripening.
(F. Hernández, et al,1999)
In the peel :
Compared to the pulp, the inedible pomegranate peel contains as much
as three times the total amount of polyphenols, including condensed
tannins and catechins, gallocatechins and prodelphinidins. The higher
phenolic content of the peel yields extracts for use in dietary supplements
and food preservatives.( Singh, R. et al,2002)( C. Ben Nasr, et al,1993)( De
Pascual, et al ,2002)
Researchs:
Some Therapeutic applications of pomegranate
In 2014, 58 clinical trials were registered with the National Institutes
of Health to examine effects of pomegranate extracts or juice
consumption on a variety of human disorders, including:
prostate cancer
lymphoma
,
prostatic hyperplasia
rhinovirus infection,
,
common cold
diabetes
, oxidative stress in
diabetic, hemodialysis ,atherosclerosis ,coronary artery disease,
brain injury ,hemodialysis for kidney disease,
infant
male infertility , aging ,
memory
,pregnancy complications ,osteoporosis , erectile dysfunction.
In
past
the
decade,
numerous
studies
,
on
the
antioxidant,
anticarcinogenic, and anti-inflammatory properties of pomegranate
constituents have been published, focusing on treatment and prevention
of cancer, cardiovascular disease, diabetes, dental conditions, erectile
dysfunction, bacterial infections and antibiotic resistance, and ultraviolet
radiation-induced skin damage. Other potential applications include infant
brain ischemia, male infertility, Alzheimer's disease, arthritis, and obesity.
(Jurenka JS.2008)
Punica granatum L. (Punicaceae) has been used for centuries in many
cultures for the prevention and treatment of a wide number of health
disorders such as inflammation, diabetes, diarrhea, dysentery, dental
plaque and to combat intestinal infections and malarial parasites.
(Ismail ,et al,2012)
colonic inflammation :The present study was designed to investigate
the ameliorative potential of Punica granatum in dextran sulfate sodium
(DSS) induced ulcerative colitis. DSS (2%) was administered orally in
drinking water for 7 days to induce ulcerative colitis. The extent and
severity of ulceration was analysed macroscopically, histopathologically
and using a disease activity index. Myeloperoxidase (MPO), a specific
marker of inflammation; histamine, a marker of mast cell degranulation;
superoxide anion generation and, lipid peroxides were analysed.
Administration of DSS resulted in a significant development of ulceration
in the colon along with a rise in histamine, MPO activity and oxidative
stress. Treatment with Punica granatum extract and its ellagic acid rich
fraction (100 mg/kg and 200 mg/kg p.o.) significantly attenuated DSSinduced colonic inflammation along with attenuation of histamine, MPO
and oxidative stress. The antiulcerative effect of Punica granatum extract
and its ellagic acid rich fraction were comparable to sulphasalazine (100
mg/kg, p.o.) and sodium cromoglycate (40 mg/kg i.p). It is concluded
that Punica granatum has a potential for ameliorating DSS-induced colitis
and its ellagic acid rich fraction may be responsible for this effect.
Further, the antiulcerative effects may be attributed to mast cell
stabilizing, antiinflammatory and antioxidant actions.(Singh K, et al,2009)
Role of pomegranate in treatment of cancer :
1- prostate cancer :There is currently a shifting focus towards finding
natural compounds that may prevent or treat cancer, due to the problems
that exist with current chemotherapeutic regimens. The fruit of the Punica
granatum (pomegranate) contains hundreds of phytochemicals and
pomegranate extracts have recently been shown to exhibit antioxidant
properties, thought to be due to the action of ellagic acid, the main
polyphenol in pomegranate. In this mini review the effects of
pomegranate extracts and ellagic acid on the proliferation of prostate
cancer cells and their future potential are discussed.(Bell C,et al,2008)
2-Colon cancer is one of the major causes of cancer-related death in
the Western world. Although cytotoxic chemotherapeutic agents are
available to treat the disease, these agents become ineffective as the
disease advances to an invasive state. An alternative but viable approach
to reduce the incidence of this deadly disease is then, to increase the
dietary intake of relatively non-toxic fruits and vegetables. An example of
a fruit with antioxidant, antidiabetic and anti-atherosclerotic properties is
pomegranate. Pomegranate produces anticancer effects in experimental
models of lung, prostate and skin cancer. More recently, pomegranate
has been found to be anti-carcinogenic in the colon. This communication
discusses pomegranate's effect in colon cancer.(Khan S A,2009)
Some researches:
1-Breast
cancer
chemopreventive
properties
of
pomegranate
(Punica granatum) fruit extracts in a mouse mammary organ culture
We previously reported anticancer effects of pomegranate extracts in
human breast cancer cells in vitro and also chemopreventive activity of
pomegranate fermented juice polyphenols (W) in a mouse mammary
organ culture (MMOC). In the present study we decided to expand the
MMOC investigations to also include an evaluation of the potential
chemopreventive efficacy of a purified chromatographic peak of W (Peak
B), and also of whole pomegranate seed oil. In brief, an MMOC was
established according to a known method. For the first 10 days of
culture, the glands were treated with pomegranate fermented juice
polyphenols (W), a high-performance liquid chromatographic (HPLC)
peak separated from W (peak B), or pomegranate seed oil (Oil, and on
day 3, exposed to the carcinogen 7,12-dimethylbenz[a]anthracene
(DMBA), and for 10 days treated with the putative pomegranate
chemopreventive. The glands were subsequently harvested and tumours
counted by visual inspection. While W effected a 42% reduction in the
number of lesions compared with control, peak B and pomegranate seed
oil each effected an 87% reduction. The results highlight enhanced breast
cancer preventive potential both for the purified compound peak B and for
pomegranate seed oil, both greater than that previously reported for
pomegranate fermented juice polyphenols.( Mehta R,et al,2004)
2-Pomegranate
Ellagitannin–Derived
Compounds
Exhibit
Antiproliferative and Antiaromatase Activity in Breast Cancer Cells
Abstract
Estrogen stimulates the proliferation of breast cancer cells and the growth
of estrogen-responsive tumors. The aromatase enzyme, which converts
androgen to estrogen, plays a key role in breast carcinogenesis. The
pomegranate fruit, a rich source of ellagitannins (ET), has attracted
recent attention due to its anticancer and antiatherosclerotic properties.
On consumption, pomegranate ETs hydrolyze, releasing ellagic acid,
which is then converted to 3,8-dihydroxy-6H-dibenzo[b,d]pyran-6-one
(“urolithin”) derivatives by gut microflora. The purpose of this study was to
investigate the antiaromatase activity and inhibition of testosteroneinduced breast cancer cell proliferation by ET-derived compounds
isolated from pomegranates. A panel of 10 ET-derived compounds
including ellagic acid, gallagic acid, and urolithins A and B (and their
acetylated, methylated, and sulfated analogues prepared in our
laboratory) were examined for their ability to inhibit aromatase activity and
testosterone-induced breast cancer cell proliferation. Using a microsomal
aromatase assay, we screened the panel of ET-derived compounds and
identified six with antiaromatase activity. Among these, urolithin B (UB)
was shown to most effectively inhibit aromatase activity in a live cell
assay. Kinetic analysis of UB showed mixed inhibition, suggesting more
than one inhibitory mechanism. Proliferation assays also determined that
UB
significantly
proliferation.
The
inhibited
testosterone-induced
remaining
test
compounds
MCF-7aro
also
cell
exhibited
antiproliferative activity, but to a lesser degree than UB. These studies
suggest that pomegranate ET–derived compounds have potential for the
prevention of estrogen-responsive breast cancers. (Adams ,et al,2010)
3-Punicalagin, a polyphenol in pomegranate juice, downregulates
p53 and attenuates hypoxia-induced apoptosis in cultured human
placental syncytiotrophoblasts:
Abstract
Oxidative stress is associated with placental dysfunction and suboptimal
pregnancy outcomes. Therapeutic interventions to limit placental injury
from oxidative stress are lacking. Punicalagin is an ellagitannin and a
potent antioxidant in pomegranate juice. We showed that both
pomegranate juice and punicalagin decrease oxidative stress and
apoptosis in cultured syncytiotrophoblasts p53 is involved in the oxidative
stress-induced apoptosis in trophoblasts. We now test the hypothesis
that punicalagin limits trophoblast injury in vitro by regulating the levels of
p53. We examined the expression of p53, mouse double minute 2
homolog, p21, hypoxia-inducible factor (HIF) α, and selected members of
the B cell lymphoma 2 (BCL2) family of proteins in cultured
syncytiotrophoblasts exposed to ≤1% oxygen in the absence or presence
of punicalagin. We found that punicalagin attenuated hypoxia-induced
apoptosis in syncytiotrophoblasts, as quantified by levels of cleaved polyADP ribose polymerase. This protective effect was in part mediated by
reduced p53 activity shown by decreased expression of p21, lower HIF1α
expression, and limited activity of caspases 9 and 3. There was no
change in expression of proteins in the BCL2 family, which are also
important in apoptosis. The data support a role for downregulation of p53
in the protection of human trophoblasts by punicalagin.
( Baosheng, et al,2013)
Role of pomegranate in treatment of bronchial asthma :
*-(Therapeutic potential of biodegradable microparticles containing
Punica granatum L. (pomegranate) in murine model of asthma)
Objective and design
Among the options for treatment of diseases affecting the respiratory
system, especially asthma, drug delivering systems for intranasal
application represent an important therapeutic approach at the site of
inflammation. The present study aimed to evaluate the therapeutic effect
of biodegradable microparticles formed by poly lactic-co-glycolic acid
(PLGA) containing encapsulated pomegranate extract on a murine model
of asthma.
Material
The extract was acquired from the leaves of P. granatum and
characterized qualitatively by
HPLC. A w/o/w emulsion solvent
extraction–evaporation method was chosen to prepare the microparticles
containing pomegranate encapsulated extract (MP).
Treatment
OVA-sensitized BALB/c mice were used as asthma model and treated
with dexamethasone and P. granatum extract in solution form or
encapsulated into microparticles.
Results
MP were able to inhibit leukocytes’ recruitment to bronchoalveolar fluid,
especially, eosinophils, decreasing cytokines (IL-1β and IL-5) and
protein levels in the lungs.
Conclusions
This approach can be used as an alternative/supplementary therapy
based on the biological effects of P. granatum for managing inflammatory
processes, especially those with pulmonary complications.
(de Oliveirira J F, et al,2013)
Scientific Classification :
Kingdom :; Plantae
(unranked) :; Angiosperms
(unranked) :; Eudicots
(unranked) :; Rosids
Order :; Rosales
Family :; Moraceae
Tribe :; Ficeae
Genus :; Ficus
Subgenus :; Ficus
Species :; F. carica
Ficus Caria (Moraceae) comprises one of the largest genera of
angiosperms with more than 800 species of trees, shrubs, hemiepiphytes,
climbers, and creepers in the tropics and subtropics worldwide. This genus
is an important genetic resource due to its high economic and nutritional
values and also an important part of the biodiversity in the rainforest
ecosystem. It is also a good source of food for fruit-eating animals in
tropical areas. The genus is divided into six subgenera based on
preliminary morphology. The monoecious subgenus Urostigma is the
largest with about 280 species all inclusive, and most of them display
distinctive hemiepiphytic habits. Ficus includes 23 species of
hemiepiphytes and lithophytes which produce aerial and creeping root
systems. F. carica L. is an important member of the genus Ficus. It is
ordinarily deciduous and commonly referred to as “fig”. The common fig
is a tree native to southwest Asia and the eastern Mediterranean,
and it is one of the first plants that were
humans.(D.G.Frodin,2004)( N. Rønsted, et al,2007)
cultivated
by
(N. Rønsted, et al,2008)(M. Dueñas,, et al,2008).
Description
The fig is a tree of small dimensions, 10 to
30 ft (3-9 m) high, with numerous
spreading branches and a trunk rarely more
than 7 in (17.5 cm) in diameter. It contains
copious milky latex. The root system is
typically shallow and spreading, sometimes covering 50 ft (15 m)
of ground, but in permeable soil some of the roots may descend to
20 ft (6 m). The deciduous leaves are palmate, deeply divided into
3 to 7 main lobes, these more shallowly lobed and irregularly
toothed on the margins. The blade is up to 10 in (25 cm) in length
and width, fairly thick, rough on the upper surface, softly hairy on
the underside. What is commonly accepted as a "fruit" is
technically a synconium, that is, a fleshy, hollow receptacle with a
small opening at the apex partly closed by small scales. It may be
obovoid, turbinate, or pear-shaped, 1 to 4 in (2.5-10 cm) long, and
varies in color from yellowish-green to coppery, bronze, or darkpurple. Tiny flowers are massed on the inside wall. In the case of
the common fig discussed here, the flowers are all female and
need no pollination. There are 3 other types, the ''Caprifig'' which
has male and female flowers requiring visits by a tiny
wasp, Blastophaga grossorum; the "Smyrna" fig, needing
crosspollination by Caprifigs in order to develop normally; and the
"San Pedro" fig which is intermediate, its first crop independent
like the common fig, its second crop dependent on pollination.
The skin of the fig is thin and tender, the fleshy wall is whitish,
pale-yellow, or amber, or more or less pink, rose, red or purple;
juicy and sweet when ripe, gummy with latex when unripe. Seeds
may be large, medium, small or minute and range in number from
30 to 1,600 per fruit.(Morton,J,1987)
Cultivation:
The fig can be grown on a wide range of soils; light sand, rich
loam, heavy clay or limestone, providing there is sufficient depth
and food drainage. Sandy soil that is medium-dry and contains a
good deal of lime is preferred when the crop is intended for
drying. Highly acid soils are unsuitable. The pH should be
between 6.0 and 6.5. The tree is fairly tolerant of moderate
salinity.(Morton,J,1987)
Chemical composition:
Ficus species contain flavanoid glycosides , alkaloids ,phenolic
acids , steroids , saponins , coumarins ,tannins , triterpinoids –
oleanolic acid , rusolic acid , α-hydroxy ursolic acid ,
protocatechuic acid , maslinic acid . The nonenzymatic
constituents include phenolic compounds , flavanoids , vitamin C.
The enzymatic constituents present are ascorbate oxidase ,
ascorbate peroxidise , catalase , peroxidise . The phenolic
compounds present are gallic acid and ellagic acid .
Furanocoumarins that are reported are psoralen ,bergapten
.(Ram.P., et al ,1970-1979)
β-sitosterol and a new tetracyclic tritepene – glaunol acetate are
reported from the leaves , bark and heartwood of F.palmata .
Besides , ceryl behenate , lupeol , α-amyrin acetate are reported
from the stem bark of F.palmata . Taraxasterol tiglate in
heartwood , quercitin-3-glucoside, rutin from leaves and three
new methyl ethers of leucoanthocyanins (delphinidin-3-o-α- Lrhamnoside , pelargonidin-3-o-α-Lrhamnoside , leucocyanidin3-o-β-D-glactosyl cellobioside) , methyl ether of
leucoanthocyanidin ,20-tetra triaconten-2-one , pentatriacontan5-one , 6-heptatriaconten-10-one , β-sitosterol-α-D-
glucoside , meso-inositol were reported from the stem bark of
F.benghalensis.(Ram, et al ,1970-1979)(Subramanian, et al, 1978)
Triterpinoid constituents rhoiptelenol , 3α-hydroxyisohop-22(29)en-24-oic acid were isolated from the methanolic extracts of fresh
leaves and stems of Ficus thumbergii . This species also contains
lupenyl acetate β-amyrin acetate , α-amyrin acetate , lupeol , βamyrin , α-amyrin , glutinol , ursolic acid, betulinic acid in its
leaves and stems (Janichi, et al ,1994)
Besides the leaves , bark and fruits of F.benjamina contains
cinnamic acid , lactose , naringenin quercetin , caffeic acid ,
stigmasterol .(Hassan, et al, 2002)
Two new pentacyclic triterpenes 8,26-cyclo-urs-21-en-3β,20β-diol
and 3β-acetoxy-8,26-cyclo-ursan-20β-ol and also 3-friedelanone,
oleanolic acid, betulinic acid lupeol acetate, αand βamyrine,
3,5,7,4’-tetra hydroxyl flavones, 3,5,7,3’,4’-pentahydroxy
flavanate are reported from the stem bark of Ficus cordata
(Herve, et al, 2008)
Fruit of F.carica shows spasmolytic activity, mediated through
the activation of K+ ATP channels- along with anti platelet activity
Hence, it can be used in gut motility and inflammatory disorders .
(Anwarul, et al ,2008).
Traditional and Current Uses:
F. carica has been traditionally used for its medicinal benefits as
metabolic, cardiovascular, respiratory, antispasmodic, and antiinflammatory remedy.(J.A.Duketal, et al,2002)( M. Werbach,1993)
It is commonly referred to as “Fig”. Leaves, fruits, and roots
of F.carica are used in native medicinal system in different disorders such
as gastrointestinal (colic, indigestion, loss of appetite, and diarrhea),
respiratory (sore throats, cough, and bronchial problems), inflammatory,
and cardiovascular disorders.( I. H. Burkill,1935)( O. Penelope,1997)
Fruits of F. carica can be eaten fresh or dried or used as jam. Figs are
used as an excellent source of minerals, vitamins, carbohydrates, and
dietary fibre because it is fat and cholesterol free and contain high
number of amino acids.( A. Slatnar, et al,2011)( R. Veberic, et al,2008)
(R. Veberic, et al,2008)
It is also reported that figs have been conventionally used for their
therapeutic benefits as laxative, cardiovascular, respiratory,
antispasmodic, and anti-inflammatory remedies.( P. M. Guarrera,2005)
Uses and health benefits:
Biological Activities:
Anticancer Activity:
A mixture of 6-O-acyl-β-d-glucosyl-β-sitosterols has been isolated as an
effective cytotoxic agent from fig (F. carica) latex that showed in
vitro inhibitory effects on proliferation of various cancer cell
lines.(S.D.Yancheva,et al,2005)(S.Rubnov, et al,2001)
Hepatoprotective Activity:
The petroleum ether extract from leaves of F. carica was evaluated for
hepatoprotective activity on rats treated with 50 mg/kg of rifampicin
orally, and significant reversal of biochemical, histological, and functional
changes induced by rifampicin on rats indicated potential hepatoprotective
activity.(N.Y.Gond, et al,2008)
Hypoglycamic Activity:
The leaf extract induced a significant hypoglycamic effect in oral or
intraperitoneal administration in streptozotocin-diabetic rats. Weight loss
was prevented in treated diabetic rats, and plasma insulin levels
considerably altered the survival index. Results indicated that the aqueous
extract of F. carica has an obvious hypoglycemic activity.
(C.Perez, et al,1998)
ntibacterial Activity and Anti-Fungal Activity:
The methanol extract of F. carica (MICs, 0.156 to 5 mg/mL; MBCs, 0.313
to 5 mg/mL) showed a strong antibacterial activity against oral bacteria.
The combination effects of methanol extract with ampicillin or gentamicin
were synergistic against oral bacteria that showed that figs could act as a
natural antibacterial agent. Hexane, chloroform, ethyl acetate, and
methanol extracts of F. carica latex were investigated for their
antimicrobial proprieties in vitro against five bacterial species and seven
strains of fungi using disc-diffusion method. The minimal inhibition
concentration (MIC) of the methanol fraction showed a total inhibition
against Candida albicans (100%) at a concentration of 500 μg/mL and a
negative effect against Cryptococcus neoforman; methanolic extract (75%)
strongly inhibited Microsporum canis and ethyl acetate extract at a
concentration of 750 μg/mL .(M.-R, et al,2009)(H.L, et al,2010)
Antipyretic Activity:
The ethanol extract of F. carica, at doses of 100, 200, and 300 mg/kg,
showed significant dose-dependent reduction in normal body temperature,
and yeast provoked elevated temperature. The effect extended up to five
hrs after drug administration while compared to that of standard antipyretic
agent, paracetamol (150 mg/kg.b.wt., p.o.) . (V. V. Patil, et al,2010)
Antituberculosis Activity:
The 80% methanol extract from the leaves of F. carica has been screened
against Mycobacterium tuberculosisH37Rv using a colorimetric
microplate-based assay. The result exhibited anti-tuberculosis activity with
MIC value of 1600 µg/mL . (S. S. Khadabadi, et al,2007)
Anthelmintic:
The anthelmintic activity of the latex of F. carica was investigated in NIH
mice naturally infected with Syphacia obvelata, Aspiculuris
tetraptera, and Vampirolepis nana. The latex was administered in doses of
3 mL/kg/day during three successive days, was effective in the removal
of S. obvelata (41.7%), and did not produce significant elimination of A.
tetraptera (2.6%) and V. nana (8.3%). High acute toxicity with
hemorrhagic enteritis was observed; additional to a weak anthelmintic
efficacy, was not recommended the use of this lattice in traditional
medicine.( A. De Amorin, et al,1999)
Antimutagenic:
Antimutagenic activity of the plant extract of F. carica on environmental
xenobiotics was investigated. The plant extract decreased the level of
mutations induced by N-metil-N′-nitro-N-nitrosoguanidine (MNNG)
inVicia faba cells, chlorophyll mutations in Arabidopsis thaliana, and NAF
induced mutability in rat marrow cells. The extract verified the ability to
decrease the genotoxicity of environmental mutagens .
(R. A. Agabeǐli, et al,2005)
Anti-HSV:
The water extract of the leaves of F. carica has been studied on anti-HSV
effect and observed on Hep-2, BHK21, and PRK cells. The water extract
possessed low toxicity and directly killing-virus effect on HSV. The MTC
was 0.5 mg/mL, TDO was 15 mg/mL, and TI was 30.0 mg/mL.
(G. Wang, et al, 2004)
In vitro cytotoxic and antiviral activities of Ficus carica latex
extracts.
The latex of fig fruit (Ficus carica) is used in traditional medicine for the
treatment of skin infections such as warts and also diseases of possible
viral origin. Five extracts (methanolic, hexanic, ethyl acetate, hexaneethyl acetate (v/v) and chloroformic) of this species were investigated
in vitro for their antiviral potential activity against herpes simplex type 1
(HSV-1), echovirus type 11 (ECV-11) and adenovirus (ADV). To
evaluate the capacity of the extracts to inhibit the replication of viruses,
the following assays were performed: adsorption and penetration,
intracellular inhibition and virucidal activity. Observation of cytopathic
effects was used to determine the antiviral action. The hexanic and
hexane-ethyl acetate (v/v) extracts inhibited multiplication of viruses by
tested techniques at concentrations of 78 µg mL(-1). These two extracts
were possible candidates as herbal medicines for herpes virus, echovirus
and adenovirus infectious diseases. All extracts had no cytotoxic effect on
Vero cells at all tested concentrations.( Lazreg Aref H1, et al, 2011)
FICUS CARICA ANTI-CANCER PROPERTIES (role of ficus carica
in treatment of cancer )
In this research, we examined the antiprolifrative effect of fig tree
latex in different concentrations including 2.5,5 and 10 mg/ml on
esophageal cancer line. Experimental studies established that
different natural agents, plant crude and extracts act as
antioxidants and chemopreventive potential in various animal
investigations having relationto human beings.( Aziz, et al,2003)
Fig tree latex includes high amount of polyphenols, flavonoids,
and anthocyanins which are the major components in
Mediterranean diet in improving health disorders.
(Solomon, et al,2006)
Fig tree latex has also been reported to have a therapeutic effect
on skin tumors and warts both in modern and traditional medicine.
(Avicenna,1998)(Rubnov S, et al,2001)
In a recent study, Lazreg Aref H et al. have reported that fig tree
latex extracts are possible candi- cells without cytotoxic effects on
normal cells. Our current research elucidates that fig tree latex
affects the esophageal cancer line in a dose-dependent manner. In
this relation, 10 mg/ml was the optimum concentration in culture
media in prevention of cancer cells growth.(Lazerg, et al,2011)
In vitro antimicrobial activity of four Ficus carica latex
fractions against resistant human pathogens (antimicrobial
activity of Ficus carica latex):
Methanolic, hexanoïc, chloroformic and ethyl acetate extracts of
Ficus carica latex were investigated for their in vitro
antimicrobial proprieties against five bacteria species and seven
strains of fungi. The green fruit latex was collected from Chott
Mariam Souse, Middle East coast of Tunisia. The antimicrobial
activity of the extracts was evaluated and based respectively on
the inhibition zone using the disc-diffusion assay, minimal
inhibition concentration (MIC) for bacterial testing and the
method by calculating inhibition percentage (I%) for fungiinhibiting activities. The methanolic extract had no effect against
bacteria except for Proteus mirabilis while the ethyl acetate
extract had inhibition effect on the multiplication of five bacteria
species (Enterococcus fecalis, Citobacter freundei,
Pseudomonas aeruginosa, Echerchia coli and Proteus
mirabilis). For the opportunist pathogenic yeasts, ethyl acetate
and chlorophormic fractions showed a very strong inhibition
(100%); methanolic fraction had a total inhibition against
Candida albicans (100%) at a concentration of 500 microg/ml
and a negative effect against Cryptococcus neoformans.
Microsporum canis was strongly inhibited with methanolic
extract (75%) and totally with ethyl acetate extract at a
concentration of 750 microg/ml. Hexanoïc extract showed
medium results.( Aref, et al, 2010)
Researches
1-Ficus spp. (fig): Ethnobotany and potential as anticancer and
anti-inflammatory agents
Abstract:This review explores medieval, ancient and modern sources for
ethnopharmacological uses of Ficus (fig) species, specifically for
employment against malignant disease and inflammation. The close
connection between inflammatory/infectious and cancerous diseases is
apparent both from the medieval/ancient merging of these concepts and
the modern pharmacological recognition of the initiating and promoting
importance of inflammation for cancer growth. Also considered are
chemical groups and compounds underlying the anticancer and antiinflammatory actions, the relationship of fig wasps and fig botany,
extraction and storage of fig latex, and traditional methods of preparing fig
medicaments including fig lye, fig wine and medicinal poultices.
(Ephraim, et al,2008)
2-Aerobiological and immunochemical studies on Carica an
aeroallergen from India(role of ficus carica in treatment of bronchial
asthma )
Abstract
Background: Carica L. is a fruit yielding tree, wildly grown or cultivated
in the tropics and subtropics. Its pollen grain has been reported to be
airborne and cause immunoglobulin E (IgE)-mediated hypersensitivity.
Objective: To conduct long-term aerobiological study on Carica pollen,
along with aeroallergenic particles originating from it and to identify visà-vis characterize an important IgE-reactive component present in this
pollen.
Methods:
The seasonal and diurnal periodicities of airborne carica
pollen were recorded in a 5-year survey using a Burkard volumetric
sampler. The allergenic potential was studied by skin prick tests, IgEenzyme-linked immunosorbent assay (ELISA) and also by aeroallergen
immunoblotting. The total pollen extract was fractionated by Sephacryl S200 column, and out of the eluted five fractions, the maximum IgEreactive fraction (as found in ELISA inhibition) was resolved into five
major
subfractions
in
reverse-phase
high-performance
liquid
chromatography (RP-HPLC). The subfraction with optimum IgE reactivity
was studied by activity gel, native and nonreducing sodium dodecyl
sulphate
polyacrylamide
gel
electrophoresis
(SDS-PAGE).
The
homogeneity of the isolated protein fraction was checked by crossed
immunoelectrophoresis with rabbit antisera and IgE reactivity was
confirmed by ELISA inhibition and immunoblotting using individual patient
sera.
Results: The Carica pollen occurred in the air round the year with
peaks during January and September–October. Among a patient
population of 1000, skin-test results showed 27.8% +1 level and 5.6%
+2/+3 level reactions. In aeroallergen immunoblotting of exposed Burkard
tape segments, the detected allergen spots showed a significant
correlation with airborne pollen count recorded. The pollen extract elicited
loss of IgE reactivity when treated with reducing agent-like βmercaptoethanol and heat, but showed six IgE-reactive components in
nonreducing IgE-immunoblot. The fraction 1 eluted from Sephacryl S200 column showed highest IgE reactivity and resolved into five major
components in RP-HPLC. Out of these, the fraction showing optimum
IgE reactivity in IgE-ELISA inhibition and immunoblotting with patient
antisera, elicited esterase activity and found to be a homogenous protein
of 100 kDa.
Conclusion: Carica papaya tree contributes significantly to the
aeropollen and aeroallergen load of the suburban outskirts of Calcutta
metropolis, India. The pollen extract contains an important IgE-reactive
protein component of 100 kDa molecular weight with esterase activity.
(P.Chakraborty, et al, 2005)
3-PHYTOPHARMACOLOGICAL
AND
PHYTOCHEMICAL
PROPERTIES OF THREE FICUS SPECIES - AN OVERVIEW ,
ABSTRACT
Ficus plants are found throughout the world as moderate woody plants or
trees. It has a vast traditional role in indigenious system of medicine like
ayurveda, siddha, unani and homoeopathy. Ficus species, namely F.
racemosa, , F. religiosa and F. benghalensis, are important ingredients in
many Ayurvedic and traditional formulations. The barks ,leaves,fruits and
latex are considered to be very effective in various treatments, such as
diabetes, skin diseases, ulcers, dysentry, diarrohoea, stomachache, piles
and as carminative ,astringent , anti inflammatory, antioxidant and
anticancer agent. The present review is therefore, an effort to give a
detailed survey of the literature on its phytochemical and pharmacological
properties.(Baby Joseph, et al ,2010)
**************************************
Summary :
These days the treatment by medicinal plants became very common in
western culture, it focus on the idea of using the plants for medicinal
purpose. But the current belief that medicines which come in capsules
or pills are the only medicines that we can trust and use. Even so most
of these pills and capsules we take and use during our daily life came
from plants. Medicinal plants frequently used as raw materials for
extraction of active ingredients which used in the synthesis of different
drugs. Like in case of laxatives, blood thinners, antibiotics and antimalaria
medications, contain ingredients from plants. Moreover the active
ingredients of Taxol, vincristine, and morphine isolated from foxglove,
periwinkle, yew, and opium poppy, respectively.
****************************************
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