International Journal of Biomedical Research

MOMORDICA CHARANTIA LINN.: A MINI REVIEW

Sahu Rishabh Kumar*, Jain Ashish, Nayak Satish Bansal College of Pharmacy, Kokta, Anand Nagar, Bhopal-462021 *Corresponding Author: [email protected] This article is available online at www.ssjournals.com ABSTRACT Momordica charantia Linn. is herbal drug that has been mentioned in many medicinal literature. This article discuss about the medicinal values of Momordica charantia Linn. In this communication, we reviewed the Phytochemistry and its applications in the treatment of various ailments like diabetes mellitus, cancer, obesity, Researchers also reported about its teratogenic activity, antigenotoxic, viral, anti inflammatory, anti depressant, anxiolytic, wound healing activity anti feedent activity. The major constituent of the plant are Terpenoids, Proteins, and Fatty acids, Volatile constituents are identified and isolated active chemical moieties from this plant are α, β and γ momorcharins , momordins a and b , , charantin. This review discusses the investigation by various workers related to chemical constituents, pharmacological action and toxicological studies of this plant since years till date.

Keywords: Momordica charantia Linn.; Diabetes mellitus; Terpenoids; Charantin

1. INTRODUCTION and female flowers bracteate at the base The plant Momordica charantia Linn with a fusiform and muricate ovary5 as (family- Cucurbitaceae) is also known as shown in figure 1. bitter gourds, karela, bitter melon and balsam pear. These species include M. angustisepala, M. balsamina (Linn), M. cochinchinensis (Spreng), M. cabrei, M. dioica (Roxb), M. elaterium, M. foetida, M. grosveroni, M. tuberosa or cymbalaria 1 . It is a tropical vegetables is a common Fig. 1 Momordica Charantia Linn. Fruit food in India. Other vernacular names of Momordica charantia have been listed later under the heading of vernacular name Seeds are brownish 13.0-16.0 mm long. 2-3. The plant is cultivated throughout India A monoecious climber or scrambling and widely grown as a vegetable crop all harbaceous vine found throughout India in over the tropical countries especially in the family curcubitaceae. Stem slender, India, china, Africa and various part of more or less pubescent, leaves Africa at an altitude of 1500 m. 2. suborbicular, alternate, the blade with 5-7 The fruit of the plant is reported to posses deep palmate lobes and quite variable in tonic, stomachic, antibilious, stimulant, their size 4. emetic, laxative, fruit pulp, leaf juice, and Fruits are 5.0-25.0c.m.long, ovoid, seed are showed anthelmintic activity (in ellipsoid or spindle shaped usually ridged lumbrici) 6. The fruits and leaves are useful or warty, dehiscent irregularly as a 3 in piles, jaundice, diabetes, leprosy, snake valved fleshy capsule or indehiscent. bite and it is found to have vermifuge and Flower monoecious, unisexual, tubular 5 antioxidant property. Fruit is also useful in lobed, moderate sized, pale yellow to gout, rheumatism and sub acute cases of orangish in colour. Male flower solitary spleen and liver 7.

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The general description and analytical Guna -Laghu parameters of plant M. charantia has been Virya -Usna summarized below. 8-9 Vipaka -Katu Karma -Vatahara, Kaphaharr, 1.1. Vernacular names4, 9- Raktadosahara, Dipana, Sanskrit - Sushavi, Karavella Hrdya, Bhedi English - Bitter gourd, Balsam pear, Balsam apple. 2. Phytochemistry: M. charantia Hindi - Karela, Kardi primarily consists of glycosides, Proteins, Bengali - Karela, Uchchhe, Kerula Sterols and fatty acids and volatile Tamil - Pakal, Pavaka,Chedi,Paharkai constituents 10. The fruit and leaves of the Kannada- Hagal plant contain two alkaloids one of them Malayalam-Kaipp, Kaippavlli, Paval being momordicine. The plant contains a Guajarati -Karela glycoside, a soponin like substance a resin Bombay -Kurela, Jangro with an unpleasant taste, an aromatic Telgu -Koekara, Kaaya volatile oil and mucilage. The seeds Arab -Quisaul – barri contain an alkaloid (m.p. 236) and an Urdu -Karela anthelmintic principle in the germ; they Oria -Kalara, Salara also contain urease 11. The fruit contains Assam -Kakiral, Kakral ascorbigen a bound from ascorbic acid 12. The free amino acids present in the fruit 1.2 General description- are aspartic acid, serine, glutamic acid, threonine, alanine, g-amino butyric acid 1.2.1. Habitat - Common in coastal and pipecolic acid. The green fruit thickets, along creeks & streams and contains luteolin, Carotene is the principal liwland food margins also pigments of carpels 13-14. The fruit pulp has occasionally cultivated. soluble pectin but no free pectic acid. 1.2.2. Parts used - fruits, leaves, seeds. Research has found that the leaves are 1.2.3. Leaves - Alternate, petiolate, the nutritious sources of calcium, magnesium, blade with 5-7 deep palmate lobes potassium, phosphorus and iron; both the and quite variable in size. edible fruit and the leaves are great sources 1.2.4. Flowers – Flower are unisexual, of the Vitamin B 15. tabular, 5-lobed moderate sized, Momordica charantia Linn. has a non- pole yellow to orangish. nitrogenous neutral principle charantin, 1.2.5. Fruits – Fruits a pepo with black and on hydrolysis gives glucose and a seeds embedded in a reddish pulp. . Charantin having 266ο melting 1.2.6. Propagation – By seeds and point16. The fruit pulp of Momordica vegetative method9. charantia has soluble pectin but not having free pectic acid. Galactouronic acid 1.3. Analytical parameters – is also obtained from the pulp. Momordica 1.3.1 Foreign matters-Nil charantia Linn. fruits also contain 1.3.2. Total ash - Not more than – 8.5% saponins, alkaloids, reducing sugars, resins 1.3.3. Acid Insoluble ash - Not more than and phenolic constituents. The presence of – 0.6% an unidentified alkaloid and 5- 1.3.4. Alcohol soluble extractive value- hydroxytryotamine is also reported. The Not less than – 6% ether extract residue of the alcoholic 1.3.5. Water soluble extractive value- concentrate from the leaves of Momordica Not less than – 28% charantia is reported to reveal hypoglycemic activity comparable to that 1.4. Properties and Action – of tolbutamide 17-18. Rasa -Tikt, katu IJBR 2[11] [2011]579‐587 580

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2.1. Terpenoids : Terpenoids are natural product and derived from five – carbon isoprene units. Terpenoids are having c-30 skeleton more extensive backbone rearrangement of the protostane cation affords the curcubitane skeleton. Curcubitacins are typical group of curcubitane type triterpenoids which are found in cucumber family (cucurbitaceae).They are generally known for their bitterness and toxicity 10. There triterpenoids I, II and III isolated from leaves along with the momordicine I and II 19. A series of cucurbitane type- triterpene glycosides called Goyaglycosides have been isolated along with momordicosides. The pyrimidine, arabinopyanosides, charine, vicine and others along with the triterpene momordicin, momordicinin reported. Charantin is cucurbitane type triterenoids in M. charantia and potential substanes which have antidiabetic properties. Charantin is mix of two compound sitosteryl glucoside and stigmasteryl gluciside 20. 2.2. Proteins: α, β and γ momorcharins with N – glycosides activity and momordins a and b were identified along with ribosome – inactivating proteins and lectins 21. 2.3. Sterols and fatty acids: Mainly palmitic acid and oleic acid are major components with trace constitued such as steric acid, lauric acid, linoleic acid, arachidic acid, myristic acid and capric acids. β – sitosterol, compesterol , daucosrerol and momordenol identified in seed oil as the sterol. The four mono methylsterols are also present known as obtusifoliol, cycloeucalenol, 4 – α – methylzymosterol, lophenol and the desmethylsterols 22. 2.4. Volatile constituents – Voleris acid, aldehydes mainly pentanal, 2 hexenal, 2 heptenal and nonadienal. 2 butylfusan, menthol, nerolidol, pentadecanol , hexadecanal , mystenol , 3 hexanol are present as volatile constituent in Momordica charantia Linn. Fruit. 5

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3. T.L.C. profile – tolerance. M. charantia fruit juice can also T.L.C. of alcoholic extract of the drug on inhibit glucose uptake by the gut and silica gel G paste using stimulate glucose uptake by skeletal (90:10) shows under U.V. muscle cells 26. Saxena et al. (2004) (366nm) four fluorescent zones at Rf. reported that Momordica charantia is 0.23(red), 0.61(light sky blue), 0.96(sky beneficial for treating type II diabetes. blue), and 0.98(red and sky blue). On Mechanisms such as the stimulating or exposure to Iodine vapour four spots show regenerating effect on beta cells or at Rf 0.17, 0.46, 0.67 and 0.98 (all yellow). extrapancreatic effects are proposed for the On spraying with 5% methanolic hypoglycaemic action of these herbs 27. phosphomolybaic acid reagent nine spots Huang et al. (2007) reported that the show at Rf. 0.03, 0.16, 0.34, 0.43, 0.50, different fractions of extract have cell 0.60, 0.75, 0.81 and 0.98 (all blue) 9. repairing activity and its ability of 4. Pharmacological Studies – stimulating insulin secretion 28. Singh et From literature survey it was found that al. (2008) studied that the anti diabetic the whole plant leaves and mainly fruits of properties of alcoholic extract of the plant M. Charantia Linn. is used in the Momordica charantia showed blood sugar treatment of various diseases. never fell below normal values even with a 4.1. Antidiabetic activity: Leung et al. high dose in pancreatic islets, beta cells (2009) elucidated the M. charantia is showed definite improvement 29. Mishra et choice of fruit used for the complementary al. (2009) reported that the inhibition on and alternative medicine 23. Srivastava et the postprandial rise in hyperglycaemia in al. (1993) reported that water extract of M. normoglycaemic rats by the M. Charantia charantia was tested on alloxan induced powder 30. Leung et al. (2009) reported diabetic rats experimentally a fall of blood further that the pre-clinical studies have sugar level after 3 weeks treatment 18. documented the anti-diabetic and Abdollahi et al. (2010) reported further hypoglycaemic effects of M. charantia that the aqueous extract of Momordica through various mechanisms 31. Miura et charantia fruit tested on the streptozocin al. (2009) studied that the water extract of induced diabetes mellitus type II rats. The the fruits of M. Charantia produced a results showed that a reduction of blood hypoglycaemic effect 32. glucose and increment in insulin level 24. 4.2. Anti cancer activity: Semiz et al. Raman et al. (1996) studied that the oral (2007) elucidated the aqueous extract administration of fresh Fruit juice (dose 6 killed human leukaemia lymphocytes in c.c. /kg. body wt.) lowered the blood sugar dose-dependent manner. Bitter Melon and level in normal and alloxan-diabetic Bitter Melon Extracts inhibit cancer and rabbits. Oral administration of alcoholic tumor. An inhibitory action on both viral extracts of the plant to some diabetic and host cell RNA and protein synthesis. patients did not produce any One clinical trial found very limited hypoglycaemic action. Karela preparations evidence that bitter melon might improve have been shown to significantly improve immune cell function in people with glucose tolerance without increasing blood cancer, but this needs to be verified and insulin levels and to improve fasting blood amplified in other research. Cytotoxic glucose levels. Blood and urine sugar activity are a group of ribosome- levels and postprandial (after eating) blood inactivating proteins named alpha- and glucose levels also fell 25. Garau et al. beta-momorcharins, momordins, and (2003) studied that the effects in diabetes cucurbitacin B. Experimental studies mellitus treatment with M. charantia fruit reported that, water extract blocked the juice reduced blood glucose levels, growth of rat prostate carcinoma and hot improved body weight and glucose water extract of the entire plant inhibited

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Sahu et al Review Article the development of mammary tumors in by Carrageenin-induced edema in rats and mice 33. 60 % oedema inhibitions was observed 4.3. Antiobesity activity: Kumar et al. with 300 mg/kg methanol extract of dried (2010) reported that the Momordica leaves of Momordica charantia Linn, charantia increase the activity of which was nearly equivalent to that of 10 adenosine 5 monophosphate kinase mg/kg of indomethacin. The anti- (AMPK), an enzyme that facilitates inflammatory effect was significant cellular glucose uptake and fatty acid (p<0.001) in the dose of 100, 200 and 300 oxidation. Compounds in bitter melon mg kg-1 of methanol extract when improve lipid profiles. They reduce liver compared to the control Group 7. secretion of apolipoprotein B (Apo B) - the 4.7. Anti viral activity: Puri et al. (2009) primary lipoprotein of low-density "bad" studied that in vitro antiviral activity cholesterol reduce apolipoprotein C- III against numerous viruses including expression, the protein found in very-low Epstein-Barr, herpes, and HIV viruses. An density cholesterol which turns into in vivo study a leaf extract have the ability LDL/Bad Cholesterol and increases the to increase resistance to viral infections as expression of apolipoprotein A-1 (ApoA1) well as to provide an immunostimulant the major protein component of high effect in humans and animals (increasing density "good" cholesterol 3. interferon production and natural killer cell 4.4. Anxiolytic activity: Ganesan et al. activity). Anti-viral activities of ribosome (2008) studied that the oral Administration inactivating proteins from M. charantia an of 5 ml kg-1 of propylene glycol (vehicle interesting paradigm emerges which may control) Methanol extract of dried leaves safely be used in treating viral diseases. It of Momordica charantia Linn has been reported that ribosome (Cucurbitaceae) was investigated for inactivating proteins are member of the anxiolytic activities in animal models. single chain ribosome inactivating protein Anxiolytic activity of methanol extract of (SCRIP) family which act irreversibly on dried leaves of Momordica charantia Linn ribosome by removing adenine residue was tested by elevated plus maze test. The from eukaryotic ribosomal RNA. Various results showed a significant anxiolytic activities of ribosome inactivating proteins effect comparable, with diazepam in all the include anti-tumor, broad anti-viral, tested doses 7. ribonuclease and deoxyribonuclease. 4.5. Antidepressant activity : Ganesan et MAP30 (Momordica Anti-HIV Protein), al. (2008) elucidated the propylene glycol α- and β-momorcharins inhibit HIV as vehicle control (5 ml kg-1); 100, 200 replication in acutely and chronically and 300 mg kg-1 of methanol extract of M. infected cells and thus are considered charantia Linn leaves were administered potential therapeutic agent in HIV orally to the groups I to IV respectively infection and AIDS 34. and 5 mg kg-1 of imipramine (drug 4.8. Mosquito larvicidal activity : Singh control) was administered intraperitonealy. et al. (2006) studied that the Momordica The extract treatment showed charantia was shown good larvicidal antidepressant effect by decreasing activity. The mosquito larvicidal property mobility time of subjected rats to forced of Momordica charantia against three swimming dose of 300 mg/kg extract, the mosquito species— anopheles stephensi, swimming behaviour of the animals was Culex quinquefasciatus and Aedes aegypti comparable to the standard drug (Diptera: Culicidae) 35. imipramine 7. 4.9. Antifeedent and antioviposition 4.6. Anti inflammatory activity : activity : Lee et al. (2009) reported that Ganesan et al. (2008) reported further that the methanol extract of bitter melon leaves the anti-inflammatory activity was studied exhibited strong oviposition deterrent

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Sahu et al Review Article activity against Liriomyza trifolii females 4.13. Wound healing activity: Sharma et on the host plant leaf when it was dipped al. (2009) reported that Momordica in the methanol extract at a concentration charantia Linn. fruit powder, in the form of 1 gm of fresh leaf equivalent/ml 10. of an ointment (10% w/w dried powder in 4.10. Teratogenic activity: Nwachi et al. simple ointment base) showed a statically (2010) reported that the safety of its use significant response (P < 0.01) in terms of during pregnancy has not been fully wound contracting ability, wound closure investigated. The water extract of the time, period of epithelisation, tensile unripe fruit was given to pregnant Sprague strength of the wound and regeneration of Dawley rats on days 7, 8, 9, 10, 11, 12, 13 tissues at wound site when compared with and 14 of gestation. The litter size was the control group, and these results were determined for each group and the litters comparable to those of reference drug were examined for gross malformations. povidone iodine ointment in an excision, The gross and histological examinations of incision and dead space wound model in various organs of the litters were also rats 38. carried out. Results show that 8.65% of the 5. Toxicological studies: Panda et al. litters from experimental animals were (2000) elucidated the alcoholic extract of malformed as against 1.62% of control. It Momordica charantia fruits was found to also showed that 31.2% of all the enhance T3, T4 was reduced. Since two malformed litters had multiple congenital higher doses inhibited thyroid hormone malformations. It also showed that the concentrations and increased hepatic lipid experimental rats had nine resorption sites peroxidation so Panda et al. suggest that while control had none. This demonstrates M. Charantia fruit extract, when used in that the water extract of Momordica excess may prove to be harmful with charantia is teratogenic in Sprague respect to thyroid function and lipid Dawley rats and should be used with peroxidation 39. Abalaka et al. (2009) caution in man 36. reported that the administration of 4.11. Anti fertility activity : Kumar et al. Momordica charantia extract up to (2010) elucidated that the ethanol and 800mg/kg-1 body weight is safe water extracts of the fruit and leaf (P>5mg/kg) and tolerated by the body. (ingested orally) to be safe during Momordica charantia is therefore safe to pregnancy However the seeds have use as Ethnochemotherapeutic agent 40. demonstrated the ability to induce Krawinkel et al. (2006) reported that the abortions in rats and mice and the root has plant contains substances with antidiabetic been documented with a uterine stimulant properties such as charantin, vicine, and effect in animals. The fruit and leaf of polypeptide-p as well as other unspecific bitter melon has demonstrated an in vivo bioactive components such as antioxidants. antifertility effect in female animals in Metabolic and hypoglycaemic effects of male animals it was reported to affect the bitter gourd extracts have been production of sperm negatively. The demonstrated in cell culture, animal, and momorcharins are effective in inducing human studies 41. Sumant et al. (2010) early and mid term abortions, but have reported that there was a significantly teratogenic effects 3. decreased the formation of micronucle, 4.12. Anti-genotoxic activity : Paul et al. inhibited the formation of chromosomal (2010) studied that the Momordica aberrations and increased the mitotic charantia decrease the genotoxic activity index. Hence, Momordica charantia has of methylnitrosamine, methanesulfonate significant antimutagenic activity 42. Basch and tetracycline, as shown by the decrease et al. (2003) reported that the Bitter melon in chromosome breakage 37. may have hypoglycaemic effects but data are not sufficient to recommend its use in

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