Momordica Charantia Linn – A Comprehensive Review

 

Sachin U Rakesh*, Priyanka R Patil and Vijay R Salunkhe

Govt. College of Pharmacy, Karad- 415 124, Dist. Satara. (MS) India

 

 

ABSTRACT

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 India, it is commonly called as ‘Karela’. It is prominently used for treatment of various aliments and in the form of various preparations especially in powdered form. It is one the crude material of Indian system of medicine. M. charantia was cited for its various medicinal properties, speciously antidiabetic. It has been used as one of the food material. The fresh and dried juice of M. charantia contents very complex and controversial chemical entities having variable properties1. M. charantia is perennial or annular climber with angled and grooved stems and hairy or villous young part, cultivated up to an altitude of 1,500 meter. Leaves are alternate, petiole, the blade with 5-7 deep palmate lobes and quite variable in size. Flowers are unisexual, tubular, 5-lobed, moderate sized, pale yellow to oranges while fruit a pepo with black seeds embedded in a reddish pulp2,3. The native country of Momordica charantia is uncertain, but the plant is cultivated throughout the tropics, particularly in India, China, East Africa and Central and South America4. It is occasionally grown as an ornamental creeper, but more commonly cultivated for the use of the unripe fruit as a vegetable. The fruit has a number of different local names – bitter gourd, bitter-melon, balsam-pear, Cundeamor (South America), Karela (India), carilla or goo-fah (Jamaica); the reported spelling of the local names is often variable. The wild variety (M. Charantia var. Abbreviata) grows as a weed in the West Indies, where the plant is known as cerasee (Jamaica) or sorossie (Dominican Republic). In addition to its major use as an anti-diabetic agent, karela has been used in India and Sri Lanka as a tonic, emetic and laxative5.  Both the cultivated and wild forms are used for this purpose6. In South / Central America, cerasee fruit or tea is used for diabetes, colds and fevers, stomach aches, constipation in children and the induction of abortion7. In India, traditionally it has been used for piles and jaundice8. Traditional Chinese uses for the fruit, seeds, vines and leaves include gastroenteritis, diabetes, tumors and some viral infections9.

 

 


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, Coxsackie’s 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 Hodgkin’s 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 Colombia, fruit of bitter melon is used65 for snakebite. Momordin Ic and its aglycone oleanolic acid are active principles34 with antirheumatoid activity. Wang and Ng have observed66 mild hypotensive response of momordin. Rather than this, ribosome inactivating proteins of M. Charantia inhibited poliovirus replication by inhibiting protein synthesis67.

 

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 India and Africa where both M. Charantia and AIDS are ubiquitous, it could bring enormous hope to the suffering and it can be advocated as a dietary aid. Since, studies have displayed the abortificient and weak uterine stimulant activity of M. Charantia therefore; use of karela during pregnancy is not advocated. Further, the use of karela by both male and female persons opting for future conception should account the antifertility activity of karela. While M. Charantia has been used successfully in Ayurvedic medicine for centuries, more clinical trials should be conducted to support its therapeutic use. It is also important to recognize that M. Charantia extracts may be effective not only when used singly, but may actually have a modulating effect when given in combination with other herbs or drugs. This review aims to highlight the main medicinal properties of MC with a view to focus on future studies of this plant.

 

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Received on 06.02.2009

Accepted on 11.08.2009     

© A & V Publication all right reserved

Research Journal of Pharmacognosy  and Phytochemistry. 1(2): Sept. - Oct. 2009, 98-102