Download Calotropis Gigantea ISSN: 2348 –0882 ============================================================================= S SARKAR

ISSN: 2348 –0882
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Int. J. Pharm. Res. Sci., 2014, 02(1), 7-17.
Calotropis Gigantea Linn. - A Complete Busket Of Indian Traditional Medicine
S SARKAR 1*, R CHAKRAVERTY2, A GHOSH3.
1
Department of Pharmaceutical Chemistry, Durgapur, West Bengal, India
2
Department of Pharmacology, Durgapur, West Bengal, India.
3
Department of Pharmaceutics, Durgapur, West Bengal, India.
Bengal College of Pharmaceutical Sciences and Research, B.R.B. Basu Sarani, Bidhannagar, Durgapur713212, W.B, India.
*Corresponding author: SIPRA SARKAR, Email id: [email protected]
-------------------------------------------------------------------------------------------------------------------------Abstract
Calotropis genera comprise of two species, with
90% inhabiting southern Asian country and are
most endemic to the India, Indonesia, Malaysia,
Thailand, and Srilanka, China. Calotropis gigantea
is a weed plant commonly known as giant milk
weed. The plant is belonging to Apocynaceae
family which includes latex bearing plants. C.
gigantea is known for various
medicinal properties in traditional medicinal system
and use to cure a variety of diseases. In last few
decades, C. gigantea is extensively studied for its
medicinal properties by advanced scientific
techniques and a variety of bioactive compounds
have been isolated
from
the different
parts of the plant and were analysed
pharmacologically. The plant is reported for
analgesic
activity,
antimicrobial
activity,
antioxidant
activity,
anti-pyretic
activity,
insecticidal
activity,
cytotoxicity
activity,
hepatoprotective activity, pregnancy interceptive
properties, purgative properties, procoagulant
activity and wound healing activity. The medicinal
properties of this plant represent it as a valuable
source of medicinal compound. This study is
collective information concerning the ethnobotany,
pharmacology, phytochemistry and biological
activities of the C. gigantea.
Keywords: Calotropis gigantea, ethnobotany,
phytochemistry, pharmacological activity, future
prospect.
Introduction
Arka (Calotropis giganteaa) an important
drug of Ayurveda is known in this country from the
earliest time. It is mentioned by the earliest Hindu
writers and the ancient name of the plant which
occurs in the Vedic literature was Arka alluding to
the form of leaves, which was used in the sacrifical
rites. There are two common species of Calotropis,
viz. Calotropis gigantea (Linn.) R.Br. and
Calotropis procera (Ait.) R.Br described by the
Sanskrit writers. [1] C. gigantea is a common
wasteland weed and commonly known as giant milk
weed. This plant is a native of Bangladesh, Burma,
China, India, Indonesia, Malaysia, Pakistan,
Philippines, Thailand and Sri Lanka. C. gigantea is
frequently available in India and used for several
medication purposes in traditional medicinal
system. [2] Most recently C. gigantea is
scientifically reported for several medicinal
properties (Figure 1) viz. the flowers are reported to
possess analgesic activity , antimicrobial and
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cytotoxic activity [3]. Leaves and areal parts of the
plant are reported for anti-diarrhoeal activity [4],
anti-Candida activity [5] and antibacterial activity [6],
antioxidant activity.[ 7] Roots are reported to contain
anti-pyretic activity[ 8], cytotoxic activity [9].
DESCRIPTION OF THE PLANT
Taxonomical classification [10]:Kingdom: Planatae
Subkingdom: Tracheobionta
Superdivision: Spermatophyta
Division: Magnoliophyta
Class: Dicotyledones
Sub class: Asteridae
Series: Bicarpellatae
Order: Gentianales
Family: Apocynaceae
Subfamily: Asclepidiaceae
Genus: Calotropis
Species: Calotropis gigantea
Vernacular Names [11]:Common names: Giant Milkweed, Crown Flower,
Swallow Wort.
Hindi: Safed aak, Aak, Alarkh, Madar, Sveta Arka,
Akanda, Bara Akand.
Gujarati: Aakando
English: Crown flower, giant Indian milkweed.
Bowstring hemp, crownplant, madarMalaysia:
Remiga, rembega, kemengu.
Indonesia: Bidhuri (Sundanese, Madurese), sidaguri
(Javanese), rubik (Aceh).
Philippines: Kapal-kapal (Tagalog).
Laos: Kok may, dok kap, dok hak.
Thailand: Po thuean, paan thuean (northern), rak
(central).
Vietnam: B[oot]ng b[oot]ng, l[as] hen, nam t[it]
b[at].
French: Faux arbre de soie, mercure vegetal.
BOTANICAL DESCRIPTION
Morphology of Calotropis gigantea leaf twig
with oppositely arranged subsessile leaves; Broadly
ovate or elliptical, cottony,pubescent when young
and glabrous on maturity; Portion of the lamina
showing venation pattern]Calotropis gigantea
occurs as a single or
many stemmed soft-wooded shrub, and occasionally
a tree reaching to 6m. All parts of
the plant exude white milky latex when cut.
Botanical description of Calotropis
incudes following parts:
Bark & Branches
The bark is thick, rough and corky and a
yellow-brown colour; twigs are green and
fleshy and may have a covering of tomentum (white
fur like hairs)[Figure 1].
Leaves
Leaves are opposite-decussate, simple,ovate
to obovate with 4-6 pairs of subopposite
nerves prominent on the abaxial surface, an acute
apex, sessile (almost decurrent) base, a pale green
colour, and quite large which is about 30x25
cm[Figure 1] .
Inflorescences
Inflorescences arise from the base of the
leaves in pedunculate (c.7cm) cymes of 3-20[Figure
2].
Flowers
Flowers consist of 5 small triangular dirty
white sepals, 5 thick ovate petals (c1cm x
1cm)which are white at the base and purple at the
tips and 5 purple tipped stamens, which surround a
white 5 lobed stigma 11[Figure 2].
Fruits
Fruits consist of green, spongy ovoid fruits
(follicles), up to 15cm long by 10cm wide. They
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split open to release plumed, papery light brown
seeds with a pappus of white filaments up to 6cm
long on one side. The main flowering period would
be from March to October[Figure 2]. [12]
Figure
1
Bark,
leaves
&
Flowers
Figure2 Fruits
MACROSCOPICAL CHARACTERISTICS
Macroscopical characteristics of various parts of
Calotropis are as follows:
Root
The root occurs in the entire condition. The
bark is separated from the wood 0.5-2.0 cm. in
diameter bearing rootlets with diameter varying
from 0.2 to 0.5 cm. externally whitish grey in
colour, wrinkled in the fresh condition, plenty of
whitish latex exudes from cuts or wounds in the
bark. Fracture is incomplete.
Leaf
Simple, opposite, sub-sessile, slightly thick,
fleshy, coriacious,10-15 cm. long and 4.5 to 6.5 cm.
broad, broadly cuneate, obovate or obovate oblong,
slightly cordate and auricled at base with tuff of
short simple hairs on the upper side near place of
the attachment to the petiole. The tender leaves are
covered with ashy gray pubescence. Mature leaves
are nearly smooth or even glabrous and pale
green[Figure 1]
Flowers
Regular,bisexual, liliac or pale rose, purple
or light greenish yellow and have a faint odour.
They are arranged in simple or rarely compound
cymose corymbs at the ends of
laterally placed or interpetiolar peduncles arising
from alternate sides of the nodes. Each cluster is
surrounded by an involucre of several small oblong
pointed scaly caducous bracts. Flower buds ovoid
[Figure 2].
Calyx
Five lobes broadly ovate with small fleshy
teeth like glands within the base.
Corolla
Regular, gamopetalous, pale rose purple or
liliac, subcordate to broadly sub- campanulate with
a short tube and five broad ovate, lanceolate,
valvate, spreading lobes.
Stamens
Five, inserted at the base of the coro
Filaments united to form a large stamina column
provided with five conspicuous radiating coronal
appendages that are completely adnate to, but
slightly shorter than the column. The appendages
are fleshy, pale
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purplish or yellowish white and laterally
compressed with a circinnately recurved hollow
corsal spur at base and two short obtuse obliquely
divergent cuticles towards the top just below the
apex. Anthers short, broad,somewhat horny with
broadly triangular
membranous anther tips that are inflexed over the
sides of the stigmatic hood.
Root bark
The tap roots are found to be having
prominent tops with rounded head and rest of
the portion spirally curved. These hard roots are
greyish white in colour and exhibit sap
exudations at the places where bark has been cut.
The bark of the older roots is cracked at places. The
bark is yellowish grey outside and yellowish white
inside. The upper cork portion is spongy and rough
while the inner portion of bark is smooth and
mucilaginous. The dried bark is bitter to taste .
MICROSCOPICAL CHARACTERISTICS
Microscopical characteristics of various
parts of Calotropis are as follows:
Stem
(I) Epidermis: This is an outermost layer of
uniseriate cells with thick cuticle. Uni- and
multicellular hairs clothe epidermis almost
completely. Cells are barrel to rectangular and are
compactly arranged.
(II) Cortex: These form a few layers below the
epidermis which are collenchymatous
(thickened corners). A few chloroplasts may also
occur in these cells. Rest of the cortex is
parenchymatous. Intercellular spaces are numerous.
(III) Endodermis: This layer of uniseriate cells
forms a wavy ring around the vascular
tissue(separates cortex from underlying tissues.)
The ells are barrel- rectangular shaped and are
compactly arranged. Characteristic casparian
thickening is lacking. It, however, contain starch
grains (termed as starch sheath).
(IV) Pericycle: It is in the form of small patches of
sclerenchymatous fibres. A few
parenchymatous cells of the original pericycle are
present between these groups.
(V) Vascular tissue system: Secondary growth is
prominent. It shows groups of
primary
phloem,
secondary
phloem,
cambium,secondary xylem, primary xylem and
intraxylary phloem. Primary phloem is completely
obliterated. Patches of secondary
phloem occur above and close to the
cambium.Cambium is unistratose.( but its
derivatives on either side which are alike, give an
appearance of a broad zone of cambium) .
Secondary xylem forms a broad and extensive
region. It compres vessels and tracheids.
The annual rings are feeble. Primary xylem occurs
near the pith and is endarch. A few
groups of phloem are situated just below the
primary xylem in the region of pith and are the
groups of intraxylary or internal phloem.
(VI) Pith: Centre is occupied by thin walled
parenchyma and also many latex vessels.
(VII) Points of ecological interest: A well
differentiated cortex, presence of conjoint,
bicollateral, opens and endarch vascular bundles
indicate that the material is a
dicotyledonous stem. Intraxylary phloem which is
primary phloem of the bicollateral vascular bundle
is characteristic.
Leaf
Transverse sections through the midrib
showed an upper and lower, single- layered
epidermis that was externally covered with a thick,
striated cuticle, a few epidermal cells on both lower
and upper surfaces, parenchymatous cells that were
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thin-walled and isodiametric to circular.
Intracellular spaces were present in ground tissue
and the stele was crescent-shaped and composed of
bicollateral and open vascular bundles. The xylem
consisted mostly of vessels and tracheids, and a
strip of cambium was present between the xylem
and phloem tissues.The lamina which was
dorsiventral with the mesophyll, was seen to be
differentiated into a palisade and spongy tissue. The
upper and lower epidermise were covered externally
with a thick, striated cuticle. Below the upper
epidermis were three rows of elongated,closely
arranged, palisade parenchyma.Spongy parenchyma
tissues were almost radially elongated with
intracellular spaces.Central cells were irregular in
shape; laticifersand vascular bundles were also
present scattered in this region.[13]
CHEMICAL CONSTITUENTS
Phytochemical studies on Calotropis have
afforded several types of
compounds
such
as
Cardenolide,
triterpinoids,alkaloids, resins, anthocyanins and
proteolytic enzymes in latex, flavonoids, tannins,
sterol ,saponins, cardiac glycosides. Flowers contain
-terpenes, multiflorenol, and cyclisadol . [14]
Leaves
The
leaves
contain
mainly
the
amyrin,amyrin acetate, ß-sitosterol, urosolic acid,
cardenolides, calotropin, calotropagenin.
Latex
The
latex
contains
caoutchouc,
calotropin,calotoxin 0.15%, calactin 0.15%,
uscharin
0.45%, trypsin, voruscharin, uzarigenin,syriogenin
and proceroside.[15]
Flower
The flower contains the flavonoids,queretin3- ratinoside, sterol, calactin,
calotoxin,
calotropagenin,
calotropin,
polysaccharides with D-arabinose, glucose,
glucosamine and L-rhamnose. Flowers also contain
enzymes 3-proteinase and calotropain(protease).
Other chemical constituents of C. gigantea flowers
are lupeol, uscharin,proceroside, proceragenin
(cardenolide),syriogenin, taraxast-20(30)-en-3-(4methyl-3-pentenoate), 3-thiazoline cardenolide,
gigantin,giganteol,
isogiganteol,
uscharidin,
uzarigeninvoruscharin
a-calotropeol,
3epimoretenol, alactuceryl acetate an a-lactuceryl
isovalerate [16]
Bark
Root bark of Calotropis
contains
triterpenes, a new norditerpenyl ester, named
Calotropterpenyl ester, and two unknown
pentacyclic triterpinoids, namely
calotropursenyl acetate and calotropfriedelenyl
acetate, akundarol isovalerate, mundarol isovalerate
and quercetin -3- rutinoside. [17,18]
Propagation and management
Propagation methods
The tree seeds freely, and natural
regeneration is common. Vegetative propagation
through half stumps assumes a special importance
as compared with the entire stumps because they
help in faster multiplication of the parent genotype
with plus characters, as each plant gives rise to 2
half stumps. Stumps also help in propagating only
one plant. Vegetative propagation through stem and
root cuttings is very useful in large-scale
multiplication of the superior genotypes.
Tree Management
C. gigantea has been cultivated in South
America and on the Caribbean Islands for the
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production of fibres at a spacing of 1-1.5 m.When
cultivated, annual yields of up to 500
kg/ha are expected. A single harvest per season is
preferable to double(ortriple)harvest; a single
harvest would result in a net saving of energy input
both on the farm and in the processing plant. Well
suited for intensive energy farming in arid or semiarid regions where frost is not a limiting factor.[19]
PHARMACOLOGICAL ACTIVITY
Antimicrobial activity
Aqueous, methanol, ethanol and petroleum
ether extracts of the leaves of C. gigantea were
reported to possess anti-Candida activity against
clinical isolate of Candida albicans, C.
parapsilosis, C.tropicalis and C. krusei.[20]
The aqueous extract of leaves of C. gigantea
was reported to possess antibacterial activity
against Staphylococcus aureus, Escherichia coli,
Bacillus cereus, Pseudomonas aeruginosa,
Micrococcus luteus and Klebsella pneumonia.
[21]
The aqueous extract of the latex of C. gigantea
was reported to exhibit significantly inhibitory
effect on S. aureus, B. cereus, E. coli and C. krusei.
[22]
Antifungal activity of C. gigantea was
reported against plant pathogenic fungi like
Fusarium mangiferae, that causes serious threat in
mango cultivation. [23]
Alam et al. (2008) reported the antibacterial
activity of methanol extract from the root
bark of C. gigantea and its petroleum ether,
chloroform and ethyl acetate fractions. Both of
methanol extract and its chloroform fraction showed
activity against Sarcina lutea, B.
megaterium and P. aeruginosa. Petroleum ether
fraction showed activity against B.
subtilis and Shigella sonnei, whereas ethyl acetate
fraction showed activity against P.
Aaeruginosa and E. coli.[24]
Analgesic activity
The alcoholic extract of the flowers of C.
gigantea was reported for analgesic activity in
chemical and thermal models in mice. The analgesic
activity was performed by acetic acid induced
writhing test and hot plate method. Oral dose of
ethanolic extract of C. gigantea flower produced a
significant decrease in the number of writhings and
delay in paw licking time. [25]
The CNS activity (analgesic activity) of alcoholic
extract of peeled roots of C. gigantea was
tested in albino rats. Analgesic activity was
observed in Eddy’s hot plate method and acetic acid
induced writhings. Oral dose of the extract (250 and
500 mg/kg body weight) significantly delayed the
paw licking time and the numbers of writhings were
greatly reduced. [26]
Wound healing activity
Root bark extract of C. gigantea was
investigated for wound healing activity in Wistar
albino rats.
The rats were topically treated with extract
formulated in ointment for excision wound healing
models and extract was given orally (100, 200 and
400 mg/kg dose) for incision wound healing
models. The results indicate that extract treatment
accelerated wound healing in rats. [27]
The crude latex of C. gigantea was evaluated for its
wound healing activity in albino rats
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using excision and incision wound models. At a
dose of 200 mg/kg/day C. gigantea latex showed
the significant wound healing activity as treated
animals exhibit 83.42 % reduction in wound area
when compared to controls which was 76.22 %. The
extract treated wounds are found to epithelize faster
as compared to controls. [28]
Cytotoxic activity
The cardenolide glycosides collected from
the root C. gigantea were reported to carry
cytotoxic activity against several human and mouse
cell lines. Calotropin, frugoside and 4'–O-βDglucopyransylfrugoside was found as the active
principles.[29]
Two compounds (compound 1 and 2) isolated from
ethanol extract of the roots of C.
gigantea were reported to display inhibitory effects
towards chronic myelogenous leukemia K562 and
human gastric cancer SGC-7901 cell lines.[30]
Crude ethyl acetate extract from the flower of C.
gigantea was reported to inhibit the
Ehrlich’s ascites carcinoma in mice. Intraperitoneal
injection (50, 100 and 200 mg/kg body weight) of
the extract significantly decreases the viable tumour
cells and body weight gain induced by the tumour
burden and prolonged survival time. The extract
also restores the haematological and biochemical
parameters (glucose, cholesterol, triglyceride, blood
urea, ALP, SGPT and SGOT) that was altered
during tumour progression, at 200 mg/kg body
weight dose extract exhibits the best activity. [31]
Anti-diarrhoeal activity
The hydroalcoholic (50:50) extract of aerial
part of C. gigantea was studied for anti-diarrhoeal
activity against castor oil-induced-diarrhoea model
in rats. The extract exhibited significant reductions
in fecal output and frequency of droppings at the
doses of 200 and 400 mg/kg body weight
(intraperitoneal dose). The extract also showed
significant inhibition in weight and volume of
intestinal content. [32]
Anti-pyretic activity
Chitme et al. (2005) reported the anti-pyretic
activity of the water:ethanol (50:50) extract of
C.gigantea roots. Anti-pyretic activity was studied
by using yeast and TAB (Typhoid) vaccineinduced
pyrexia in Albino Swiss rats and rabbits. At the
dose of 200 and 400 mg/kg body weight
(intraperitoneal injection) extract significantly
reduced the fever and body temperature was
normalized. [33]
Insecticidal activity
Methanol extract of C. gigantea root bark
and its chloroform and petroleum ether fractions
were evaluated for residual film toxicity, fumigant
toxicity and repellent effect against several inster of
larvae and adult of Tribolium castaneum. Methanol
extract showed high insecticidal activity against T.
castaneum followed by petroleum ether fraction and
chloroform fraction. None of the sample showed
fumigant toxicity. [34]
Anti-inflammatory
Ethanol extract of C. gigantea was reported
for the anti-inflammatory activity against
carrageenan induced paw edema in Wistar albino
rats. The oral administration of 400mg/kg of C.
gigantea showed significant anti-inflammatory
activity, the activity was found more than that of
100mg/kg of Ibuprofen. [35]
Antioxidant activity
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Leaves of C. gigantea were reported to carry
antioxidant activity. The study reports the DPPH
radical scavenging activity, reducing power activity
and nitric oxide scavenging activity of the
hydroalcohlic extract of C. gigantea leaves. Extract
exhibited the maximum DPPH radical
scavenging activity (85.17%) at 400μg/ml
concentration. At 100μg/ml concentration extract
showed 54.55% nitric oxide scavenging activity.
Reducing power of the extract was found to
increase with increasing the concentration of
extract. [36]
Pregnancy interceptive properties
Different organic solvents of C. gigantea
roots were reported to exhibit pregnancy
interceptive activity in rats. The extract exhibited
100% pregnancy interceptive activity at a dose of
100 mg/kg.The extract also exhibited 100% efficacy
at the dose of 12.5 mg/kg when administered in the
Days 1-5 and 1-7 postcoitum schedules. [37]
Procoagulant activity
The latex of C. gigantea is reported to carry
procoagulant activity. The latex extract hydrolysed
casein, human fibrinogen and crude fibrin clot in a
dose dependent manner. Extract hydrolyses the
subunits of fibrinogen, subunit Aa hydrolyzed first
followed by Bb and g subunit. The crude extract
hydrolysis crude fibrin clot strongly compared to
trypsin and papain. Proteins present in the latex of
C. gigantea are strongly proteolytic and responsible
for procoagulant activity of C. gigantea. [38]
Hepatoprotective effects
Ethanol extract of stems of C. gigantea was
reported for hepatoprotective activity in male
Wistar rats against carbon tetrachloride induced
liver damage. The extract resulted in significantly
decreased of AST, ALT and lipid peroxide levels
and showed effective protection of liver. The extract
also protects the rats from oxidative damage. [39]
Vasodilation Effect:
Effect of latex from Calotropis gigantea in
the green frog R hexadactyla showed a significant
increase in cardiac output. Evidence suggests the
prime action of latex on the
cardiovascular system involves changes in the
cation (Ca, Na) permeability, with consequent
excitation of Ca channels in the heart muscle and an
increase coronary flow. Therefore,
dilatation property is likely responsible for the
pharmacologic actions of the latex.[40]
SOME FORMULATION OF THIS PLANT
Abedi et al published that Production of primary
carbon has involved by the carbonization of
Calotropis Gigantea (Giant Stabragh)in a negligibly
ventilated atmosphere to drive out Comparison of
K2co3 and Khco3 for Preparation of volatiles,
leaving a porous carbon structure with low
Carbonaceous Adsorbent. [41]
Vidya C et al published that green synthesis of ZnO
nanoparticles by zinc nitrate and utilizing the bio
components of leaves extract of Calotropis
Gigantea. The ZnO nano crystallites of average size
range of 30-35 nm have been synthesized by rapid,
simple and ecofriendly method. Zinc nanoparticles
were characterized using scanning electron
microscopy (SEM) and X-ray diffraction (XRD).
[42]
Conclusion
Empirical knowledge about medicinal
plantsplays a vital role in primary health care and
has great potential for the discovery of new herbal
drugs.The pharmacognostical studies including
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macroscopic and microscopic evaluation of various
parts of Calotropis gigantea would be of
considerable use in the identification of this drug.
These findings may be useful to supplement
existing information with regard to the
identification and standardization of Calotropis
gigantea to distinguish it from substitutes and
adulterants. [43]
In recent years, ethnomedicinal studies
received much attention as this brings to light the
numerous little known and unknown medicinal
virtues especially of plant origin. Pharmacological
screenings of C. gigantea revealed its medicinal
potential and represents as a valuable medicinal
plant with several medicinal properties. As the
pharmacologists are looking forward to develop
new drugs from natural sources, development of
modern drugs from C. gigantea can be emphasized
for the control of various diseases. A systemic
research and development work should be
undertaken for the conservation of C. gigantea and
development of products for their better economic
and therapeutic utilization. [44]
In conclusion, the present manuscript may
be useful to supplement information with regard to
its identification and in carrying out further research
of its use in the treatment of various diseases.
ACKNOWLEDGMENT
The authors are thankful to Bengal College
of Pharmaceutical Sciences and Research, for
giving the all facilities, thankful to All Professors of
Bengal College of Pharmaceutical Sciences and
Research for guidance and Botanical Survey of
India, Howrah-2, W.B, India for identification of
the plant.
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