Momordica
Charantia Linn A Comprehensive Review
Sachin
U Rakesh*, Priyanka R Patil and Vijay R Salunkhe
Govt.
Momordica charantia Linn. is a commonly used herb in Ayurvedic medicine. This review
supports all updated information on its phytochemical
and pharmacological activities, traditional uses and scientific approach. The
plant extracts and its chemical marker or target molecule charantin
have been widely used for the treatment of a large number of human ailments.
The chemical entities of this plant has been used as an antidiabetic,
antihelmintic, antimicrobial, hypotriglyceridemic,
hypocholesterolemic, insecticidal, antioxidant,
anticancer, antimalarial, larvicidal,
antiviral, antiulcerogenic agents. Scientifically
proved activities are related with traditional concept. Scientific evidence
exists with respect to their major and minor constituents. M. charantia is the most important
controversial and effective natural origin that has a tremendous future for
research. The novelty and applicability of M.
charantia are hidden. Such things should be
overcome through modern scientific concept.
KEYWORDS: Momordica
charantia, Charantin, antidiabetic, Photochemistry,
Pharmacological activities.
INTRODUCTION:
Momordica charantia Linn. (Cucurbitaceae) is also known as Bitter
melon or Bitter gourd. In
CHEMICAL CONSTITUENTS:
Biologically active chemicals of biter melon are
glycosides, saponins, alkaloids, fixed oils, triterpenes, proteins and steroids10. The
immature fruits are a good source of vitamin C and also provide vitamin A,
phosphorus, and iron11. Charantin is the active principle responsible for the antidiabetic action, composed of a mixture of beta-sitosterol-beta-D-glucoside and
5, 25 stigmadien-3-beta-ol glycoside12. A new cucurbitane triterpenoid
momordicoside P was isolated recently13.
In addition to it the recent work also isolated trinorcucurbitane
and cucurbitane triterpenoids
from the roots of M. Charantia.
From which kuguacins C and kuguacins
E showed14 moderate anti HIV- 1 activity. Recently twenty five
components were identified15 in the seed oil of karela
amounting to 90.9% of the total oil. The constituents are represented by sesquterpenes (71.7%), phenylpropanoids
(11.0%), and monoterpens (7.6%), trans nerolidol (61.6%). Out of which the
trans nerolidol
is responsible for antimicrobial activity. HIV inhibitory proteins like (C.
D. Putnam, 2000) MRK 29 (MW: 26.8 kda),
MAP 30 (MW: 30,000 kda) and lectin
are documented. The presence of trypsin inhibitors16, guanylate
cyclase inhibitors17 slastese
inhibitors18, and alpha- glucoside
inhibitor like D-(+)-trehalose are reported19.
The major constituents, some of active markers of various extract of M. charantia are of great importance.
PHARMACOLOGICAL ACTIVITIES:
The various effects of Momordica charantia are documented in traditional as well as in scientific literature.
Antidiabetic
activity:
M. Charantia is the most widely studied with regards to
its antidiabetic effect20 and all parts
that is fruit pulp, leaves seed and whole plant have shown hypoglycemic effect
in normal individual. The bitter melon has contained10 (A. Raman,
1996) steroidal saponin known as `charantin`,
insulin like peptides and alkaloids that showed hypoglycemic activity. Along
with this, bitter melon has been shown21 to enhance the number of
beta cells of Islets of Langerhans. Various polyherbal preparations containing M. charantia have showed22 a
significant reduction in blood glucose, glycosylated haemoglobin and an increase in plasma insulin and total
hemoglobin in animals. Along with polyherbal
preparation, there are three extracts obtained from karela
showed23 antihyperglycaemic effects (methanolic extract A, chloroform extract B and aqueous
extract C). Karela has shown24,25 promising effects in diabetic complications
(nephropathy, neuropathy, gastroapresis, and cataract
and insulin resistance) in experimental animals.
Antiviral activity:
Various phytoconstituents
isolated26 from Karela that are alpha and
beta momorcharin, lectin
and MAP 30, have been documented to have in vivo antiviral activity against
Epstein- Barr, herpes, HIV, Coxsackies virus B3 and polio virus. Also MAP 30,
GAP 31 acts against sexually transmitted diseases27 and having no
effect on motility or vitality of spermatozoa. Momorcharin
obtained from karela showed anti HIV properties28.
This antiviral activity of MAP 30 is due to inhibition of HIV-1 integrase29.
Also lectin and MRK 29 from M. Charantia act through inhibition of
viral reverse transcriptase30,31. In vitro studies showed that ribosome inactivating proteins and MAP
30 have antiviral against HSV- 2 and HSV- 1. This antiviral activity is due to
inhibition of protein synthesis32,33. Certain in vivo and in vitro studies with karela extract and
its purified fraction including MAP 30 showed anti-cancer activity against
lymphoid leukemia, lymphoma, skin tumor, prostate cancer, squamous
carcinoma of Hodgkins disease34,35,36. Alpha and beta momorcharin, momordin and cucurbitacin B from M.
Charantia have clinically demonstrated ability to
inhibit37 guanylate cyclase
linked to pathogenesis and replication of leukemia and other cancers. It has
been reported38 that bitter melon extracts suppressed lymphocyte proliferation
and macrophage lymphocyte activity through inhibition of cell cycle and G2 and
M phases through inhibition39 of incorporation of thymoidine, leucin and uridine into DNA.
Antioxidant
and chemoprotective activity:
The reactive oxygen species (ROS) and/or free radicals
play an important role in tissue damage and pathological events in organism.
The antioxidant activity40 of Karela has
been reported. Antioxidant and chemoprotective
properties of M. charantia fruit extract have
been reported41 currently. The probable mechanism of action of chemoprotection is found to be increase in both anti-
oxidant enzymes and GST activities while lowering cytochrome
P 450 (CYP1A) dependent enzyme activities.
Antihyperlipidemic
activity:
Besides hypoglycemic properties, Karela
fruit extract has been shown to have a strong hypolipidemic
action42 on diabetic hypertriglyceridemia
and hypercholesterolemia. This activity may be due to an antioxidant potential.
Feeding of conjugated octadecatrienoic fatty acid
isolated from M. charantia
seed for a week significantly lowered the peroxidation,
in sunflower oil fed rat43.
Antibacterial
activity:
Extract obtained from leaf of M. charantia
demonstrated both clinically and experimentally having44 broad
spectrum antimicrobial activity. Extract of entire plant was shown to have antiprotozoal activity against E. histolytica. In
vitro, this extracts acted45,46 against E. coli, S. paratyphi,
S. dysenterae and against S. griseous. H. pylori also showed47 high sensitivity to fruit extract
with MIC between 1.95 and 250mg /ml in phase II study. Leaves extract showed
inhibition of mycobacterium tuberculosis growth using BACTEC- 460
susceptibility taste method15. The seed oil contains trans nerolidol,
apiole, cis dihydrocarveol and germacrene D
was tested for its antibacterial and antifungal activities. S. aureus was
found48 to be the most sensitive microbe with MIC <500mg/ml.
Antiulcerogenic
activity:
M. charantia
has antiulcer49 activity. Momordin Ic (10mg/kg, p.o.) potentially
inhibited ethanol induced gastric mucosal lesions. Dried powdered fruits in
filtered honey shown significant and dose- dependant anti ulcerogenic
activity against ethanol induced ulcerogenesis in
rats. Powdered fruit is also claimed to be useful in healing wounds, leprous
and malignant ulcers. Anti H. pylori
activity which would also beneficially contributes to antiulcer activity50
of bitter melon.
Antilarvicidal
activity:
During the last decade, various studies on natural
plant products against mosquito vectors indicate them as possible alternatives
to synthetic chemical insecticides51,52. The insecticidal activity53
of this plant against mustered saw fly is also found. In laboratory experiment,
karela has shown54 good larvicidal activity against three container breeding
mosquitoes An. Stephensi,
Cx. Quinquefasciatus and Ae. aegypti.:
Fig.
1. Chemical constituents
from various extracts of M. charantia.
Immunomodulatory
activity:
Immunosuppressive and immunomodulatory
effects by karela components have been reported.
There was reduction55 in NK cell activity but increased macrophage
mediated spontaneous cytotoxicity. Intraperitonial administration56 of alpha momorcharin and beta momorcharin
to mice resulted in high levels of IGE production; while no cross immunological
reactivity among these proteins was found. Alpha and beta momorcharin
showed immunosuppressive activity via lymphocytotoxicity.
Its immunostimulant activity has been attributed to
increase in interferon production and natural killer cell activity57.
Abortificient
and antifertility activity:
Several experimental studies demonstrated abortificient property58 of momordic
proteins. Momorcharins produced abortificient
activity in early and midterm pregnancy. Teratogenic
effect59 of momorcharins was seen in the
early organogenesis stage.
Other
activities:
PAF, a potent glycerophospholipid
mediator, is involved in a number of dose- dependent physiological functions
such as platelet and neutraphil aggregation, anaphylaxis
and hypotension60. The methanol extracts of M. charantia were investigated61
for their PAF receptor binding inhibitory effects using rabbit platelets, and
they showed significant inhibitory effect of more than 60%. Preparations from M. charantia
exhibited in vitro anthelmintic
activity against Ascaridia galli worms
and shown62 to be more effective than piperazine
hexahydrate. Karela is used
as an emmenogague63. It
has been traditionally used64 in the treatment of psoriasis. In
Toxicity
studies:
M. charantia
was shown68 to safe (no sign of nephrotoxicity,
hepatotoxicity and any adverse reaction on the food
intake) in experimental animals when ingested in low doses. However, low
toxicity18 of all parts of this plant is reported. When extract is
administered in high doses by intravenously or intraperitonially,
toxicity or even death has been reported in laboratory animals. The toxic
effect69 of the juice extract was more potent than alcoholic
extract. The
red arils around bitter melon seeds are toxic to children. When the juice is
given to a child caused vomiting, diarrhea, and death70. Ingestion of excessive amounts of bitter
melon juice can cause abdominal pain and diarrhea71. The reports
shown72,73 a potential fatal reaction in human being that is
hypoglycemic coma induced in two small children.
CONCLUSION:
The extensive survey of literature revealed that karela is an important source of many pharmacologically and
medicinally important chemicals such as charantin, momordicin, kuguacins C and E,
MAP 30, momordin, alpha and beta momorcharins,
triterpenoids. The charantin
is the most searched chemical constituent or target molecule of M. Charantia.
The plant has also been widely studied for their various pharmacological
activities like, antidiabetic, antioxidant,
antiviral, anticancer, anti-inflammatory, antimicrobial, antiulcreogenic,
larvicidal, immunomodulatory,
hypolipidemic, abortificient
and antifertility, anthelmintic, emmenogogue.
In developing countries like
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Received on 06.02.2009
Accepted on 11.08.2009
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Research Journal of Pharmacognosy and Phytochemistry. 1(2): Sept. - Oct. 2009,
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