Global Journal of Medicinal Plant Research

2016. 4(4): 23-39 ISSN: 2074-0883 Journal home page: http://www.aensiweb.com/GJMPR/

RESARCH ARTICLE

Open Access Journal Published BY AENSI Publication © 2016 AENSI Publisher All rights reserved This work is licensed under the Creative Commons Attribution International License (CC BY). http://creativecommons.org/licenses/by/4.0/

To Cite This Article: Olivier Tene Tcheghebe, Maffo Timoléon, Armel Jackson Seukep, Francis Ngouafong Tatong, Ethnobotanical uses, phytochemical and pharmacological profiles, and cultural value of Momordica chlarantia Linn. : An overview. Glob. J. Med. Plant Res, 4(4): 23-39, 2016

Ethnobotanical uses, phytochemical and pharmacological profiles, and cultural value of Momordica chlarantia Linn. : An overview

1Olivier Tene Tcheghebe, 2Maffo Timoléon, 3Armel Jackson Seukep, 4Francis Ngouafong Tatong 1University of Yaounde I, Inorganic Chemistry Department, Faculty of Science, P.O. Box 812. Yaounde. Cameroon 2University of Yaounde I, Department of Organic Chemistry, Faculty of Science, P.O. Box 812. Yaounde, Cameroon. 3University of Dschang, Biochemistry Department, Faculty of Science, P.O Box 67. Dschang, Cameroon. 4 University of Dschang, Chemistry Department, Faculty of Science, P.O Box 67. Dschang, Cameroon. ABSTRACT Background: Traditional medicine plays a crucial role in the developing countries as it provides primary health care needs for a large majority of their populations. Momordica charantia is among the plants popularly used in the traditional medicine with a proved effectiveness. Objective: This article aims to provide a comprehensive review on ethnobotanical uses, phytochemical and pharmacological profiles, and cultural value of Momordica chlarantia Linn. Results: In the folkloric medicine, this plant is particularly involved in the treatment of cancers, diabetes, and to fight viruses; cardiac, liver and kidney diseases, and gynaecological problems. Pharmacological tests carried out on this plant for its antioxidant, antimalarial, hypocholesterolemic, trypanocidal, hepatocurative and hepatoprotective, gastroprotective and anti-ulcer, anthelmintic, immunomodulatory, anti-inflammatory and analgesic, antiviral, anti-genotoxic, anti-tumour and anticancer, anti-hepatitis B virus, abortifacient, antimicrobial and antibacterial, hypoglycemic and anti-diabetic, cardiovascular, wound healing, body weight decrease, antifeedant, neuroprotective, antipyretic, anti-diarrheal, larvicidal, antifertility, anti-gout activities; its effect on haemoglobin concentration and on diabetic complications revealed positive results. Some bioactive constituents such alkaloids, tannins, flavonoids, saponins, glycosides, sterols, mucilages and oleanolic acids significantly present in the plant extracts support its numerous properties and uses in traditional medicine, while its rich content in moisture, ash, crude lipid, crude fibre, crude protein, carbohydrates, minerals and vitamins validate its high nutritional value. Moreover, this plant has powerful medico-spiritual properties, providing protection against curses, diseases, evil spirits, spells and madness. Conclusion: It is now obvious that Momordica chlarantia can help as a natural source product in the treatment process of many diseases and in particular diabetes, cancers, cardiac, liver and kidney problems. Even more interesting, many scientific studies have proved that this plants extract can be consumed without a risk of toxicity. However pregnant women should not eat bitter melon or take this plant extracts as it stimulates the uterus and may cause premature birth. We sincerely hope that we have provided a data base for proper evaluation of Momordica charantia extracts which could lead to the discovery of new and more effective drugs. Key words: Momordica chlarantia, Ethnobotanical, pharmacological, toxicity Address for Correspondence: Olivier Tene Tcheghebe, University of Yaounde I, Inorganic Chemistry Department, Faculty of Science, P.O. Box 812. Yaounde. Cameroon E-mail: tetcholi@yahoo.com Received 3 October 2016; accepted 16 December 2016; published 26 December 2016

INTRODUCTION

Medicinal plants have recently become a focus of interest because they may play key roles in treating a

majority of diseases with minimal or no side effects. Momordica chlarantia is one of those popularly known

plants for its numerous medicinal virtues. This plant is a member of the cucurbitaceae family. It grows in

tropical areas of the Amazon, Africa, Asia, India, South America, and the Caribbean and is used traditionally as

24 Olivier Tene Tcheghebe et al., 2016/ Global Journal of Medicinal Plant Research, 4(4): 23-39, 2016

both food and medicine (Perumal et al., 2015). The plant is a climbing perennial with elongated fruit that

resembles a warty gourd or cucumber. The unripe fruit is white or green in colour and has a bitter taste that

becomes more pronounced as the fruit ripens (Langner et al., 1998). Momordica charantia is a flowering vine

cultivated its intensely bitter fruits that are commonly used in cooking and as a natural remedy for treating

antioxidant, diabetes like disorders (Abascal and Yarnell, 2005). This herbaceous, tendril-bearing vine grows to

5 meters. It bears simple, alternate leaves 4-12cm across, with 3-7 deeply separated lobes. Each plant bears

separate yellow male and female flowers. In the Northern Hemisphere, flowering occurs during June to July and

fruiting during September to November. As the fruit ripens, the flesh becomes tougher, bitterer, and too

distasteful to eat. On the other hand, the pith becomes sweet and intensely red; it can be eaten uncooked in this

state and is a popular ingredient in some Southeast Asian salads. When the fruit is fully ripe it turns orange and

mushy, and splits into segments which curl back dramatically to expose seeds covered in bright red pulp (Md.

Alamgir et al., 2012). Male flower stalks slender with bract midway or toward base; peduncle 2-5 cm long, bract

reniform, 5-11 mm diameter, green, pedicel 2-6 cm long; receptacle-tube cupshape, 2-4 mm long and 2-3 men

wide; sepals ovate-elliptic, 4-6×2-3 mm, pale green; petals obovate, 10-20×7-15 mm, mucronate at apex, scales

2; filaments 1.5-2 mm long, inserted in the throat of the receptacle tube: Anthers coherent. Female flower

peduncle 1-6 cm long; bract 1-9 mm diameter; pedicel 1-8 cm long: Sepals narrow, oblong lanceolate, 2-5 mm

long; petals smaller than or equal to that in male, 7-10 mm long; ovary fusiform, narrowly rostrate, 5-11×2-3

mm, muricate, tuberculate or longitudinally ridged; style 2 rare long (Aparna et al., 2015). Pendulous, stalk 2-8

cm long; fruit discoid, ovoid, ellipsoid to oblong or blocky, often narrowed at ends, sometimes finely rostrate, 3-

20×2-5 cm, white or green turning orange on maturity, soft tuberculate with 8-10 broken or continuous ridges,

splitting from base in to 3 irregular valves (Aparna et al., 2015). The Seed, 5-30, squarish rectangular, ends

subtridentate, faces compressed, sculptured, 5-9×3-6 rare, margins grooved; testa brown or black (Aparna et al.,

2015). Momordica chlarantia is commonly known as either bitter melon or bitter gourd but there is other

synonyms which include: Momordica chinenus, Momordica elegans, Momordica indica, Momordica operculata,

Momordica sinenuns and Silyos fauriei, and its common names bitter Melon, papailla, melaode sao caetano,

bittergourd, balsam apple, balsam pear, karela or corilla, ku kua karela, kor-kuly, ku gua, para-aki, salsamino,

Soru, Sorossis borossieb, pare, peria La at, peria. Bitter melon as fondly called has been implicated

experimentally to achieve a positive sugar regulatory effect by suppressing the neural response to sweet taste

stimuli and also keep the body functions operating normally (Bakari et al., 2010). It is one of the most

promising antioxidant plant (Ghosh et al., 2014; Rezaeizadeh et al., 2011), and can therefore serve in the

prevention and treatment of oxidative stress relating diseases such as malaria, diabetes, etc. All parts of the

plant, including the fruit, taste very bitter. This plant is used in the treatment of many diseases, but diabetes,

cancers, cardiac, liver and kidney problems are the most cited. Momordicin, Chlarantin, Vicine, Kuguacin J,

EMCDO, Cucurbitacin are the most important purified bioactive constituents isolated from this plants which

justify its multiple pharmacological activities.

Scientific Classification

Kingdom: Plantae

Class: Dicotyledonae

Order: Cucurbitales

Family: Cucurbitaceae

Genus: Momordica

Species: Momordica chlarantia

Scientific name: Momordica chlarantia

Linn.

Plant and fruits images

Traditional Uses:

Extracts of various parts of Momordica chlarantia are used extensively in traditional African medicine.

Clinical conditions for which Momordica chlarantia extracts (primarily from the fruit) are currently being used

include diabetes, dyslipidemia, microbial infections, and as a cytotoxic agent for certain types of cancer

(Chrubasik et al., 2007; Oishi et al., 2007; Chaturvedi et al., 2004; Ahmed et al., 2001). The seeds, fruit, leaves,

and root of the plant have been used in traditional medicine for microbial infections, sluggish digestion and

intestinal gas, menstrual stimulation, wound healing, inflammation, fever reduction, hypertension, and as a

laxative and emetic (Leung, 1984). In Guyana traditional medicine, a leaf tea is used for diabetes, to expel

intestinal gas, to promote menstruation, and as an antiviral for measles, hepatitis, and feverish conditions. It is

used topically for sores, wounds and infections, internally and externally for worms and parasites (Jagessar et

al., 2008). Leaves of Momordica charantia (Karela) are effective in bilious affections as emetic and purgative.

Leaves are administered internally in leprosy, piles, jaundice. It is active as galactogogue, it is also applied

round the eye orbit for night blindness. Leaf juice is rubbed to soles in burning of the feet, and used in liver

complaint of childrens. In Cambodia and in Gold coast, leaves are also considered to be antipyretic (Nadkarni

25 Olivier Tene Tcheghebe et al., 2016/ Global Journal of Medicinal Plant Research, 4(4): 23-39, 2016

and Nadkarni, 1998). Leaves are used in treatment of menstrual troubles, burning sensation, constipation, fever

(malaria), colic, infections, worms and parasites, as an emmenogogue, measles, hepatitis and helminthiases

(Kumar et al., 2010). Fruits of Momordica charantia are used in asthma, burning sensation, colic, constipation,

cough, diabetes, fever (malaria), gout, helminthiases, inflammation, leprosy, skin diseases, ulcer and wound. It

has also been shown to have hypoglycaemic properties (antidiabetic) in animal as well as human studies. Juice

of the plant leaves used to treat piles completely. It is used as a blood purifier due to its bitter tonic properties. It

can heal boils and other blood related problems that show up on the skin. Juice of karela is also beneficial in

treating and preventing the liver damage (Agharkar, 1953; Garau et al., 2003). While the root decoctions have

abortifacient properties, leaf and stem decoctions are used in treatment of dysentery, rheumatism and gout

(Subratty et al., 2005). Roots are used in the treatment of syphilis, rheumatism, boils, ulcer, septic swellings,

opthelmia, and in Prolapsus vagenae (Agharkar, 1953; Jadhav, 2008). In addition, juice of Momordica charantia

drawn directly from fruit has traditionally been used for medicinal purposes worldwide. Likewise, the extracted

juice from leaf, fruit and even whole plant are routinely used for treatment of wounds, infections, parasites (e.g.,

worms), measles, hepatitis and fevers (Behera et al., 2008). In Uganda, an infusion of the leaf and roots is used

as an abortifacient and ecbolic (Chhabra et al., 1989) and in Tanzania the fruit pulp is regarded as being

poisonous to weevils, moths and ants and is used as a repellant (Bryant, 1909). In India, Momordica charantia is

used by tribal people for abortions, birth control, increasing milk flow, menstrual disorders, vaginal discharge,

constipation, food, diabetes, hyperglycemia, jaundice, stones, kidney, liver, fever (malaria), gout, eczema, fat

loss, hemorrhoids, hydrophobia, intestinal parasites, skin, leprosy, pneumonia, psoriasis, rheumatism, scabies,

snakebite, vegetables, piles, tonic, anthelmintic, purgative (Grover and Yadav, 2004). However, it is commonly

consumed as vegetable (Grover and Yadav, 2004). Momordica charantia has been used by indigenous people to

treat diabetes, urethra discharge, dysentery, colitis, wounds, infections, hepatitis, rheumatism, gout and mild

purgative for children (Lotikar et al., 1996; Plattel and Srinivasan, 1997). Momordica charantia is used by

traditional healers in Togo for gastrointestinal, childhood viral diseases, skin problems, malaria and food uses.

However, gynecological aid, fevers, and diabetes are three uses much more commonly cited by the healers

[Beloin et al., 2005]. In Cameroon, Momordica chlarantia juice is claimed to reduce the problem of Pyorrhea.

This plant decoction is used for the treatment of diabetes, viruses, cancer, tumors, high cholesterol and psoriasis,

rheumatism, typhoid fever, malaria,fever, worms, ulcer and hepatitis. This plant’s leaves are squeeze and drink

to clear fallopian tube blockage.

Reported Phytoconstituents:

The nutritional and chemical compositions of Momordica chlorantia were investigated using standard

analytical methods (Bakare et al., 2010). The proximate analysis showed the percentage moisture, ash, crude

lipid, crude fibre, crude protein, carbohydrates content of the material plants. The calorific values for leaf, fruit

and seed were 213.26, 241.66 and 176.61 Kcal/100g respectively. The elemental analysis of this plant leaf

revealed the presence of potassium (413ppm), sodium (2200ppm) and calcium (20510ppm). Other elements

found present in leaf include magnesium (255ppm), manganese (156ppm), zinc (120ppm), iron (98ppm) and

copper (32ppm). Vitamin A (0.03ppm), vitamin E (800ppm), folic acid (20600ppm), cyanocobalamin

(5355ppm), and ascorbic acid (66000ppm) were present. Trace amount of some other vitamin such as vitamin

B3, vitamin B6, vitaminD, and vitamin K were also found in the methanol and pet-ether leaf extract of

Momordica chlorantia. Phytochemicals like alkaloids, tannins, flavonoids, saponins, glycosides, sterols,

mucilages and oleanolic acids (Bakare et al., 2010; Harinantenaina et al., 2006; Venkat et al., 2011) were also

found present. The study conducted by Bakare et al (Bakare et al., 2010) also indicates the presence of

nutritional and chemical compounds that are beneficial in addition to numerous medicinal values of the plants.

Researches indicate the Active purified constituents responsible for the properties of Momordica. They are

charantin (insulin-like peptide or plant-insulin) (Harinantenaina et al., 2006), Momordicin I, Momordicin IV,

Aglycone of Momordicoside I, Aglycone of Momordicoside L and Karavilagenin D (Wen et al., 2015),

kuguacin J (3,7,23-trihydroxycucurbita-5,24-dien-19-al) , a Triterpenoid from Momordica charantia (Pitchakarn

et al., 2012), 3β,7β,25-trihydroxycucurbita-5,23(E)-dien-19-al (TCD), another triterpenoid, EMCDO (5β,19-

epoxy-25-methoxycucurbita-6,23(E)-dien-3β-ol) (Chang et al., 2015), Vicine (Dutta et al., 1981), momordin,

stigmasta-5, 25-dien-3-β-O-glucoside, β-sitosterol-β-D-glucoside, momordicoside G, momordicoside F1,

momordicoside F2, momordicoside I, momordicoside K, momordicoside L (Wu and Ng, 2008; Kokate et al.,

2008; Chatterjee and Prakashi, 1995). Some structures of these actives constituents are given below. Charantin

can be used as substitute to insulin (Cunnick and Takemoto, 1993). Momordin may have anticancer properties

(Leung, 1984). Flavonoids have been shown to have diuretic, laxative, antispasmodic, anti-hypertensive and

anti-flammatory actions (Okuda 1962), and antimalarial activity (Konziase, 2015). Isolated pure form of

alkaloids and their synthetic derivatives are used as basic medicinal agents for their analgesic and bacterial

effects (Blytt et al., 1988), antihypertensive, antiarrhythmic, antimalarial and anti-cancer activities [Wink et al.,

1998]. Tannin rich medicinal plants are used to heal a lot of illnesses; such as leucorrhoea, rhinorrhea and

26 Olivier Tene Tcheghebe et al., 2016/ Global Journal of Medicinal Plant Research, 4(4): 23-39, 2016

diarrhea. More recently, tannins have gained medical interest, because of the high prevalence of deadly ailments

such as AIDS and numerous cancers (Ibikunle and Ogbadoyi, 2011).

Kuguacin J EMCDO Cucurbitacin

Vicine Chlarantin Momordicin

Chemical structures of some purified bioactive constituents extracted from Momordica chlarantia:

Pharmacological Profiles:

Scientific investigations on Momordica charantia demonstrated the tremendous pharmacological and

nutritional values of this plant which support its various traditional uses for the management of health problems.

The most important are:

Antioxidant activity:

A study aimed to determine and compare the antioxidant activity of methanol and chloroformic extracts of

Momordica charantia fruit was carried out by Rezaeizadeh et al (Rezaeizadeh et al., 2011). In this study, the

total antioxidant and free radical scavenging activities in methanol and chloroform extracts were measured by

ferric thiocyanate (FTC), Thiobarbituric acid (TBA) and 1,1-diphenyl-2-picryl-hydrazyl(DPPH) methods. Total

phenol and flavonoid contents of the plant’s extracts were also evaluated. The total antioxidant activity results

indicated that, the inhibition percent of methanol extract was significantly higher than the inhibition percent of

chloroform extract in the FTC and TBA methods. Methanol extract exhibited a higher IC50 value for free

radical scavenging, a higher concentration of total phenols and flavonoids and was found to contain more potent

antioxidant and high polyphenol compounds when compared with chloroform extract. The results also

confirmed that, the type of solvent has an important role in detecting plant compounds. In another study, the

antioxidant activity of Momordica charantia was studied in some in-vitro antioxidant models like DPPH radical

scavenging activity, Superoxide radical scavenging activity, Ferric reducing power and Hydrogen peroxide

scavenging activity (Ghosh et al., 2014). The plant’s extract showed antioxidant activity by inhibiting DPPH,

scavenging superoxide and hydrogen peroxide. It also showed reducing power ability in ferric reducing model.

Total antioxidant capacity was found to be 19.22 mg/gm expressed as L-Ascorbic acid. Significant antioxidant

activity of Water extract of this plant was found and might be due to the presence of Acidic compounds,

Flavonoids, Phenols, Saponins, Tannins and Triterpenoids present in the plant. This plant can be used as an

accessible source of natural antioxidants and to cure some diseases associated with oxidative stress like malaria.

Antimalarial activity: The anti-malarial activity of Momordica charantia has been reported (Mothana et al.,

2009; Jayapal et al., 2012; Munoz et al., 2000). A study conducted by Munoz et al showed moderate in vivo

activity of the this plant’s extract against rodent malaria Plasmodium vinckei petteri and an excellent

anitimalarial activity in vitro on Plasmodium falciparum (Munoz et al., 2000). This plant’s extract, a bacterial

insecticide also has good larvicidal and pupicidal properties against potent malarial vector, Anopheles stephensi

and can be recommended as a potent bio-pesticide (Jayapal et al., 2012).

Hypocholesterolemic activity: Experiments carried out in normal as well diabetic animals have shown

hypo-cholesterolemic effects by Momordica charantia (Dhar et al., 1999). In a study conducted by Dhar et al,

sunflower fed rats were fed with conjugated octadecatrienoic fatty acid isolated from Momordica charantia

seeds for 4 weeks. After 4 weeks, these rats showed significant lowering of the plasma lipid peroxidation and

erythrocyte membrane lipid peroxidation as well as non enzymatic liver tissue lipid peroxidation (Dhar et al.,

1999).

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Trypanocidal activity:

The effective concentration of ethanolic extract of Momordica charantia leaves, capable of killing 50% of

Trypanosoma cruzi parasites (IC50) was 46.06μg/mL. The Minimum Inhibitory Concentration (MIC) was

≤1024 μg/mL. Metronidazole showed a potentiation of its antifungal effect when combined with an extract of

Momordica charantia (Santos et al., 2012).

Food preservative:

A study was carried out systematically to isolate and characterize peptides having antibacterial activity from

different parts of Momordica charantia (Jabeen and Khanum, 2014). Crude aqueous extracts of seeds, pulp and

skin were prepared in phosphate buffer saline (PBS) and antibacterial activity was checked on Luria Bertani

(LB) broth agarplates against a number of bacteria such as Escherichia coli, Staphylococcus aureus, Salmonella

typhi and Pseudomonas aeruginosa. The results of this study suggested that antibacterial peptide obtained from

seeds the plant may be used as an alternative natural bio-preservative source for minced meat products.

Hepatocurative and Hepatoprotective activity:

An analysis of different serum enzymes including ALT, AST, ALP and LDH was carried out to evaluate

the hepatoprotective and hepatocurative effects of Momordica charantia (Zahra et al., 2012). The study was

divided in two phases. In first the phase, liver toxicity was induced in rabbits with administration of

acetaminophen, and then Momordica extract was given and hepatocurative effects were observed. The results

indicated significant decrease in the elevated concentrations of these enzymes in acetaminophen-intoxicated

rabbits. In the second phase, the extract of Momordica was given to the rabbits orally for 10 and 15 days

respectively. Then, the animals were administered with acetaminophen and hepatoprotective effects of

Momordica were observed. The hepatoprotective effects of Momordica extract was found to be more effective

after 15 days as there was less elevation of the serum enzymes after liver damage. Chaudhari et al (Chaudhari et

al., 2009) also demonstrated the hepatoprotective activity of hydroalcoholic extract of Momordica charantia

leaves against carbon tetrachloride induced hepatotoxicity in albino wistar rats (Chaudhari et al., 2009). This

plant can then be used as a protective and/or therapeutic remedy against liver diseases.

Gastroprotective and anti-ulcer activity:

Gastroprotective potential of alcoholic and aqueous fruit extracts of Momordica charantia against pylorus

ligation, aspirin and stress induced ulcer in rats has been evaluated (Venkat et al., 2011). Both aqueous and

alcoholic fruit extracts of this plant were used at three different doses (100, 200 and 400 mg/kg). Results of the

study demonstrated the dose dependent antiulcer activity of Momordica charantia. There was a significant

decrease in ulcer score, ulcer area, total acid output and gastric volume in plant extract treated groups.

Phytochemical analysis of plant extracts showed the presence of active constituents including glycosides,

saponins, alkaloids, sterols, steroidal saponins and mucilages which might participate in gastroprotective

potential of the plant. In another study (Alam et al., 2009) methanol extract of Momordica charantia fruit

increases healing of gastric ulcer and also prevents development of gastric ulcers and duodenal ulcers in rats.

Effect on diabetic complications: Complications are frequently encountered in diabetes and these are

associated with irreversible functional and structural changes in various organs particularly the kidneys, eyes,

nerves, blood vessels and insulin resistance (American Diabetes Association 1998). Momordica chlarantia has

shown promising effects in prevention as well as delay in progression of these complications in experimental

animals (Grover et al., 2001; Rathi et al., 2002; Vikrant et al., 2001). In a study aimed to evaluate the effect of

this plant on diabetic neuropathy, its aqueous extract (200 mg/kg) was given to diabetic animals for 50 days.

The treatment caused reduction in tail flick latency by 43.6% in comparison to diabetic control animals where it

increased by 73.6% compared to normal animals (Grover et al., 2002 ).In another experiments, Momordica

chlarantia treatment (aqueous extract 200 mg/kg) of alloxan diabetic rats inhibited development of cataract

(observed up to 120 days) that (Rathi et al., 2002). With a view to assessing the effect of Momordica charantia

treatment on development of nephropathy in diabetic animals, certain renal functions parameters were measured

by Grover et al (Grover et al., 2001). STZ diabetic mice had several times higher mean values of serum

creatinine (50.0mol/l), urinary albumin (1411.3g/24 h), urine volume (31.9 ml/24 h) and renal weight (0.59 gm)

compared to normal mice. However, in parallel, these values were significantly less (47.5mol/l, 1072g/24 h,

20.0 ml/24 h and 0.51 g, respectively) in Momordica chlarantia treated animals (Grover et al., 2001). Bhaskar

Sharma et al also proved that Momordica charantia exhibited significant rejuvenating capacity of kidney tissues

activities in alloxan-induced diabetic mice (Sharma et al., 2014).These results are very important since diabetic

patients are 17 times more prone to kidney disease as compared to healthy patients. Komolafe et al investigated

the effects of Momordica charantia on histological changes of the left ventricle of the heart in streptozotocin-

induced diabetic Wistar rats (Komolafe et al., 2012). Momordica charantia and glimperide (a standard drug)

attenuated the morphological alterations and reduced the glycogen deposits (Komolafe et al., 2012). All these

evidences suggest cardio-protective effects of this plant against anatomical derangements observed in the

28 Olivier Tene Tcheghebe et al., 2016/ Global Journal of Medicinal Plant Research, 4(4): 23-39, 2016

diabetic rats. This later result showed the usefulness of Momordica chlarantia to diabetic patients who are

particularly prone to cardiovascular diseases including hypertension, atherosclerosis, diabetic cardiomyopathy,

congestive heart failure and cardiac autonomic neuropathy (Komolafe et al., 2012).

Anthelmintic study: Preparations from Momordica charantia exhibited in vitro anthelmintic activity against

Ascaridia galli worms and shown to be more effective than piperazine hexahydrate, a conventional drug used

against helminths (Lal et al., 1976). In another work the anthelmintic property of Momordica charantia seeds

extracts against Indian adult earthworm Pheretima posthuma was evaluated, while Albendazole was used as the

standard drug (Vedamurthy et al., 2015). Petroleum ether, chloroform, ethanol and aqueous extracts at

concentration of 20 mg/mL each were evaluated for anthelmintic activity. The time taken for each worm for

paralysis and death were determined. Among all the extracts chloroform extract showed best anthelmintic

activity by inducing paralysis within 3 min and death within 8 min. The extracts even showed better result when

compared to the standard drug Albendazole. Thus, this plant extracts can be used for the treatment of worms.

Immunomodulatory activity: Studies have shown immunosuppressive as well as immunostimulatory effect

of Momordica charantia components (Leung et al., 1987; Spreafico et al., 1983; Zheng et al., 1999; Huang et

al., 1990; Oladele et al., 2009). During an in vivo study, Leung et al. (Leung et al., 1987) observed that

microgram injections of Momordica charantia inhibitory protein (MCI) to mice delayed H2-incompatible skin

allograft rejection, splenocyte responsiveness to concanavalin A (ConA) and phytohemoglobin (PHA). It also

abrogated PFC response to T-dependent (SRBC) antigen but completely spared response to a T-independent (S

III) stimulus. There was reduction in NK cell activity but increased macrophage-mediated spontaneous

cytotoxicity. In vitro, MCI inhibited lymphoid cell responsiveness to PHA and ConA, but not to LPS and

markedly enhanced macrophage-dependent cytotoxicity (Spreafico et al., 1983). Intraperitoneal administration

of alpha-momorcharin and beta-momorcharin (50g weekly for 5 weeks) to BALB/cAn or C57BL/6N mice

resulted in high levels of IgE production (PCA titer), while no cross-immunological reactivity among these

proteins was found (Leung et al., 1987; Spreafico et al., 1983; Zheng et al., 1999). In another in vivo study, a

leaf extract demonstrated the ability to increase resistance to viral infections as well as to provide an

immunostimulant effect in humans and animals (increasing interferon production and natural killer cell activity)

(Oladele et al., 2009).

Anti-inflammatory and analgesic activity:

Many scientific studies have revealed the anti-inflammatory activity of momordica chlorantia (Oladele et

al., 2009; Leelaprakash et al., 2012; Che-Yi et al., 2014). The in vitro anti-inflammatory activity of Momordica

charantia was studied by inhibiting the action of lipoxygenase (LOX) enzymes, involved in the mechanism of

inflammation (Leelaprakash et al., 2012). A protein free Momordica charantia extract was also used to

characterise the chemical component which is responsible for inhibition of lipoxygenase activity. It was

observed that the plant extract had anti-inflammatory activity as it inhibited the activity of lipoxygenase. The

study also showed that the activity of LOX in the presence of plant extract was less when compare to control.

Thus the plant extract was responsible for the inhibition of LOX activity. Moreover, the study gave a clear

picture that a protein is not responsible for the activity as removal of protein from the extract also gave the same

result. Another study reports the anti-inflammatory and analgesic properties of aqueous leaf extracts of

Momordica charantia in rats and mice in a carrageenan-induced rat paw oedema (Oladele et al., 2009). The

result of the study revealed that the leaf extract of the plant possesses anti-inflammatory property as they were

found to significantly (p<0.05) inhibit oedema induced by carrageenan in the rat paws. The leaf extract of

Momordica charantia was also found to significantly (p<0.05) increase the reaction time of the mice in hot plate

test method, while the number of writhing movement of the mice was also significantly(p<0.05) reduced in

dose-dependent manner. The results of the study suggest the anti-inflammatory and analgesic effects of the

aqueous leaf extract of the plant. Che-Yi Chao et al also indicate that this plant in diets promoted lipid

metabolism, reducing fat accumulation, and improving low blood glucose in sepsis (Che-Yi et al., 2014).

Antiviral activity:

Momordica chlarantia is active against viruses. In fact, its extract can inhibit transcription and

transactivation, and can also inhibit viral integrase (Lee-Huang et al., 1990). MAP 30 (Momordica Anti HIV

Protein) present in seed and fruit extracts; Alpha and beta momorcharin from seeds, fruits and leaf extracts, all

have Anti-HIV (Human Immunodeficiency Virus) activity (Lee-Huang et al. 1990; Au et al. 2000). In fact, in a

study HIV-infected cells treated with alpha- and beta-momocharin showed a nearly complete loss of viral

antigen while healthy cells were largely unaffected (Lee-Huang et al., 1990), and in 1996 the inventors of the

chemical protein along MAP-30 filed a U.S. patent, stating it was “useful for treating tumors and HIV

infections. He added that in treating HIV infection, the protein is administered alone or in conjunction with

conventional AIDS therapies (Lifson et al., 1989).This plant’s extract is also effective against polio virus as it

inhibits polio virus replication by inhibiting protein synthesis (Schreiber et al., 1999). In a study conducted by

Prasero et al (Prasero et al., 1997), the in vitro activity of Momordica chlorantia against herpes simplex virus

29 Olivier Tene Tcheghebe et al., 2016/ Global Journal of Medicinal Plant Research, 4(4): 23-39, 2016

type 2 (HSV2) was evaluated by standard method of plaque reduction assay. The result showed that the total

inhibition of plaque formation on HSV2-infected Vero cell line was achieved at concentration of 8% v/v of

crude extract, whereas the concentration of 1% v/v was capable of reducing the number of plaques by

approximately 50% (inhibitory dose 50 = ID50). This result is very interesting as even with only small amount

of crude extract, they got ID 50. We can then use Momordica chlarantia extract to treat genital organ infection

caused by HSV2. Recently, the new antiviral activity of the protein extracted from Momordica charantia seed

was determined with different subtypes of influenza A by Pongthanapisith et al (Pongthanapisith et al.,

2013).Using 5, 25, and 100 TCID50 of influenza A/New Caledonia/20/99H1N1, A/Fujian/411/01 H3N2 and

A/Thailand/1(KAN-1)/2004 H5N1, the IC50 was calculated to be 100, 150, and 200; 75, 175, and 300; and 40,

75, and 200µg/mL, respectively. The present finding indicated that the plant protein inhibited not only H1N1

and H3N2 but also H5N1subtype. As a result of the broad spectrum of its antiviral activity, this plant protein

holds a great promise to be developed as a potent therapeutic against various and even new emerging subtypes

of influenza A such as H7N9, which is now pandemic in China.

Anti-Genotoxic Activity:

Balboa and Lim-Sylianco have reported that Momordica charantia decreases the genotoxic activity of

methylnitrosamine, methanesulfonate and tetracycline, as shown by the decrease in chromosome breakage

(Balboa et al., 1992).

Anti-tumour and anticancer activities:

Plants are an invaluable source of potential new anti-cancer drugs. Early examples of anticancer agents

developed from higher plants are the antileukemic alkaloids (vinblastine and vincristine), which were both

obtained from the Madagascar periwinkle (Catharanthus roseus) (Voss et al., 2005). Momordica charantia is one

of these plants with both edible and medical value and reported to exhibit anticancer activity. Many scientific

studies have proved the effectiveness of this plant’s extracts against almost all types of cancer cells. Its crude

extract inhibits tumor formation in CBA/DI tumour cell line of mice (Jilka et al., 1983). MAP 30 extracted from

Momordica chlarantia is effective against lymphoid leukemia, lymphoma, squamous carcinoma of tongue,

larynx, human bladder carcinoma, Hodgkin’s disease (Licastro et al., 1980; Ng et al., 1994; Battelli et al., 1996;

Basch et al., 2003; Soundararajan et al., 2012), This plant’s extract is also effective against colon cancer cells

(Kohno et al., 2002), human nasopharyngeal carcinoma CNE-1 and CNE-2 cells (Fang et al., 2012) in inhibiting

breast cancer cell growth (Li-Yuan et al., 2016; Ray et al., 2010; Shobha et al., 2015) and prostate cancer

progression in vitro and in vivo (Ru et al., 2011; Pitchakarn et al., 2011). Fruit and seed extract activates natural

killer cells in mice (Cunnick et al., 1990). To explore the potential effectiveness of Momordica charantia, its

methanol extract was used to evaluate the cytotoxic activity on four human cancer cell lines: Hone-1

nasopharyngeal carcinoma cells, AGS gastric adenocarcinoma cells, HCT-116 colorectal carcinoma cells, and

CL1-0 lung adenocarcinoma cells (Chia-Jung et al., 2012). This extract showed cytotoxic activity towards all

cancer cells tested; with the approximate IC50 ranging from 0.25 to 0.35 mg/mL at 24 h. The extract induced

cell death was found to be time-dependent in these cells. Apoptosis was demonstrated by DAPI staining and

DNA fragmentation analysis using agarose gel electrophoresis. The same extract also activated caspase-3 and

enhanced the cleavage of downstream DFF45 and PARP, subsequently leading to DNA fragmentation and

nuclear condensation. The apoptogenic protein, Bax, was increased, whereas Bcl-2 was decreased after treating

for 24 h in all cancer cells, indicating the involvement of mitochondrial pathway in extract-induced cell death.

These findings indicate that, ethanol extract of this plant has cytotoxic effects on human cancer cells and

exhibits promising anti-cancer activity by triggering apoptosis through the regulation of caspases and

mitochondria. Another study investigated the anti-cancer effect of an active water-soluble extract (s) of

Momordica charantia on cell viability and its cellular mechanism(s) of action in inducing cell death (Manoharan

et al., 2014). The results show that the crude water soluble extract of this plant can evoke both time-course (800

μg/ml) and dose-dependent (200μg/ml -800 μg/ml) decreases in cell viability (cell death) with maximal

increases in cell death employing 800 μg/ml over a period of 24 hours following incubation. The results of this

study have also shown that the crude water-soluble extract of the plant (800 μg/ml) can elicit marked and

significant (p < 0.05) increases in the activities of caspase -3 and caspase -9 in all the cell lines. The crude water

soluble extract of Momordica charantia can stimulate the release of cytochrome-c and elevated intracellular free

calcium concentrations [Ca2+] in the different cancer cell lines compared to untreated cell lines. These results

clearly show that Momordica charantia is exerting its anti-cancer effect via an insult to the mitochondria

resulting in apoptosis, calcium overloading and subsequently, cell death. More recently, Mohammed conducted

a study focused on the in vitro effect of crude methanol extract of Momordica charantia on liver cancer

(HepG2), Human colon cancer (HCT116) and breast cancer (MCF-7) (Alshehri et al., 2016). The results showed

that the effect of this plant’s extract was highly significant in HepG2 cells (IC50: 0.77 μ g/ml) and HCT116 cell

(IC50: 0.81μ g/ml) than MCF-7 (IC50: 1.35μ g/ml). Thus the methanol extract of this plant has a potential effect

to decrease the proliferation rate of different cancer cell lines specially HepG2 liver cancer and HCT116 Human

30 Olivier Tene Tcheghebe et al., 2016/ Global Journal of Medicinal Plant Research, 4(4): 23-39, 2016

colon cancer. The study suggested that the mechanism of action of Momordica chlarantia plant extract is due to

its chemical contents like triterpenoid, which is confirmed as anti-proliferative ingredient (Akihisa et al., 2007).

Also, the in vivo antitumor activity of a crude extract from the bitter melon (Momordica charantia) was

determined (Jilka et al., 1983). The extract inhibited tumor formation in CBA/H mice which had been given i.p.

injections of 1.0 x105 CBA/DI tumor cells (77% of the untreated mice with tumors versus 33% of the treated

mice with tumors after 6 weeks). The extract also inhibited tumor formation in DBA/2 mice which had been

given i.p. injections of either 1x105 P388 tumor cells (0% of untreated mice survived after 30 days versus 40%

survival of the treated mice) or 1x105 L1210 tumor cells (0% survival of untreated mice versus 100% of treated

mice after 30days). The in vivo antitumor effect required both the prior exposure of tumor cells to the extract

(2hr) in vitro and i.p., biweekly injections of the extract into the mice. The optimum dose for tumor inhibition (8

µg protein, biweekly) was not toxic to mice for at least 45 days of treatment. Nylon wool-purified spleen cells

from these same bitter melon-treated mice exhibited an enhanced mixed lymphocyte reaction when exposed to

irradiated P388 stimulator cells (186% of the untreated control mice). These data indicate that in vivo

enhancement of immune functions may contribute to the antitumor effects of the bitter melon extract. This

antitumor activity was later confirmed by Li-Yuan Bai et al (Li-Yuan et al., 2016). They investigated the

antitumor activity of 3β, 7β, 25-trihydroxycucurbita-5, 23(E)-dien-19-al (TCD), a triterpenoid isolated from

wild bitter gourd, in breast cancer cells. TCD suppressed the proliferation of MCF-7 and MDA-MB-231 breast

cancer cells with IC50 values at 72 h of 19 and 23 μM, respectively, via a PPARγ−independent manner. TCD

induced cell apoptosis accompanied with pleiotrophic biological modulations including down-regulation of Akt-

NF-κB signaling, up-regulation of p38 mitogen-activated protein kinase and p53, increased reactive oxygen

species generation, inhibition of histone deacetylases protein expression, and cytoprotective autophagy.

Together, these findings provided the translational value of TCD and wild bitter gourd as an antitumor agent for

patients with breast cancer. Kuguacin J, another Triterpenoid from Momordica charantia have shown potent

anticancer capabilities to induce apoptosis/cell cycle arrest in pre-initiated/initiated tumor cells, while in more

advanced tumors, this compound could block resistance to anticancer drugs, tumor progression and metastasis,

especially against human prostate cancer (Pitchakarn et al., 2012; Pitchakarn et al., 2011). These findings

provide evidence of the anticancer effects of kuguacin J and suggest the strong possibility that this purified

compound from natural product can be developed for cancer chemoprevention and chemotherapy. It is

henceforth evident that, Momordica chlarantia is effective against many types of cancer and gains very high

attention to be one of the strong candidates for the elaboration of potent anticancer drugs.

Anti-hepatitis B virus activity:

EMCDO (5β,19-epoxy-25-methoxycucurbita-6,23(E)-dien-3β-ol), a purified compound isolated from

Momordica chlarantia extract exhibited the most efficient effect in terms of reducing HBV surface antigen, e

antigen and viral DNA levels in HBV particles or surface antigen-producing cells 2.2.15 and PLC/PRF/5,

respectively (Chang et al., 2015). Tumor suppressor p53 played a significant role in EMCDO-mediated anti-

HBV effects. Pretreatment with EMCDO prevented 2.2.15 cells-induced tumor formation in a nude mice

subcutaneous model. The anti-HBV and anti-tumor activities of EMCDO were better than those of oltipraz, an

inhibitor of HBV transcription. In fact, the EC50 of HBV DNA suppression was 4.58 g/ml for oltipraz and

1.31 g/ml for EMCDO. EMCDO also reduced the pro-inflammatory cytokines and mediates in LPS-treated

RAW264.7 cells in a dose-dependent manner. Thus, EMCDO have potential beneficial effects against HBV and

inflammation response, subsequently preventing hepatocellular carcinoma development.

Abortifacient activity:

Alpha and beta momorcharin in seeds extract Induces mid term abortion in mice (Yeung et al., 1986).

Anti-typhoid fever:

Adeyi et al investigated the antimicrobial potency of methanol extract of Momordica charantia leaves on

Salmonella typhi in male albino rats (Sprague dawley) and the effects of treatment on liver function (Adeyi et

al., 2013). There were 5 groups of 10 rats each. 1ml aliquot of the 4th dilution of Salmonella typhi was

administered orally to rats in four of the groups to be infected with typhoid, while the last group served as the

control. Infected groups were thereafter treated with 100 and 200mg/kg of M. charantia and 10mg/kg of

chloramphenicol, respectively for seven days, while the remaining group was not treated after infection. The

effect of treatment on infection level, body weight and liver enzymes were thereafter investigated. Marked

reduction in infection level was observed in all treated rats. Rats treated with 200mg/kg of the plant extract had

total clearance by the sixth day, while significantly lower (p<0.05) infection level was recorded in rats treated

with the plant extract than those treated with the standard drug. Mean body weight of all treated rat groups

increased during treatment. Concentrations of total and direct bilirubin, alanine aminotransferase (ALT),

alkaline phosphatase (ALP), aspartate aminotransferase (AST) and gamma glutamyl transferase (GGT) were

higher (p<0.05) in untreated rats than the treated rats. These results suggest that leaf extract of Momordica

31 Olivier Tene Tcheghebe et al., 2016/ Global Journal of Medicinal Plant Research, 4(4): 23-39, 2016

charantia is a potent antimicrobial drug against Salmonella typhi with hepato-ameliorative potentials. This result

is of great importance since typhoid fever is a disease prevalent in the tropics. In fact, despite the availability of

antibiotics, treatment of patients with the disease has been quite challenging in the face of resistance to those

drugs.

Antimicrobial and antibacterial activity:

The antibacterial and antifungal activities of Momordica charantia, was investigated against Staphylococcus

aureus (gram+ve), Escherichia coli (gram-ve) and Candida albicans (fungi) using the Stokes disc diffusion, the

pour plate, well diffusion and streak plate methods (Jagessar et al., 2008). The solvent type extracts were

obtained by three extractions with hexane, dichloromethane, ethyl acetate and ethanol respectively. Solvents

were removed in vacuo to yield viscous oils and paste which were made up to a concentration of 0.03g in 10 mL

of the respective solvents. These were tested in varying volumes of 100-600uL/plate (i.e. concentrations of 0.03-

0.18mg/10mL agar). The solvents were used as control whereas ampicillin and nystatin were used as references

for bacteria and fungal species respectively. The solvents had no effect on the microorganisms whereas

ampicillin and nystatin inhibited microbial growth. Momordica Charantia showed antimicrobial inhibitory

activity at 0.18mg/10mL plate of medium with activity most prominent with the ethanol extracts and negligible

with the hexane. This study suggests that the ethanol extracts of Momordica Charantia, can be used in the

control of theses micro-organisms-induced diseases. In another study, this plant’s extracts also appeared to

inhibit the growth of numerous gram-negative and gram-positive bacteria including Escherichia coli, Salmonella

typhi, Shigella dysenteriae, Staphylococcus aureus, Pseudomonas aeruginosa, Streptobacillus moniliformis,

Streptococcus pneumoniae, Helicobacter pylori, and parasitic organisms Entamoeba histolytica and Plasmodium

falciparum (Anonymous, 2007).

Hypoglycemic and anti-diabetic activity:

Over 1000 herbal products have been used by various cultures to lower blood glucose and treat diabetes.

Among them, Momordica charantia is the most popular herbal resource (Marles and Farnsworth, 1995). A study

was conducted in order to evaluate changes in urinary metabolite profile of the normal, streptozotocin-induced

type 1 diabetes and Momordica charantia extract (100 and 200 mg/kg body weight) treated diabetic rats, using

proton nuclear magnetic resonance (1H-NMR) -based metabolomics profiling, for one week (Perumal et al.,

2015). Blood glucose level after administration was measured to examine hypoglycemic effect of the extract.

The results obtained indicated that Momordica charantia was effective in lowering blood glucose level of the

diabetic rats. Administration of the plant’s extract was found to be able to regulate the altered metabolic

processes. Thus, it could be potentially used to treat the diabetic patients. Charantin isolated from fruits of

Momordica charantia was also tested for its hypoglycemic activity. In fasting rabbits, it gradually lowered blood

sugar within one to four hours and recovered slowly to initial level. At an oral dose of 50 mg/kg, blood sugar

level was declined by 42% at the 4th hour. The average blood sugar fall during 5 hours was 28%. Charantin was

found to be more potent than tolbutamide however both compounds produced similar pattern of blood sugar

change. The hypoglycaemic activity of charantin in depancreatixed cats was less, but abolished, indicating a

pancreatic as well as extra-pancreatic action (Desai and Tatke, 2015). The possible modes of the hypoglycemic

actions are insulin secretagogue effect, stimulation of skeletal and peripheral muscle glucose utilization,

inhibition of glucose intake and hexokinase activity, inhibition of key gluconeogenic enzymes, glycose-6-

phosphatase and fructose-1,6-bisphosphate dehydrogenase (due to the depressed activity of these enzymes, the

glucose synthesis would decrease and as a result blood glucose level would be reduced), stimulation of key

enzyme of HMP pathway (The increased activity of this regulatory enzyme reflects an increased glucose

oxidation through this pathway and thus contributes partially to the overall blood glucose decreasing),

preservation of islet β cells and their functions or prevention of insulin resistance (Md. Alamgir et al., 2012;

Bailey and Day, 1989; Meir and Yaniv, 1995; Yang et al., 2015).

Cardiovascular effects:

Effect of charantin (a pure chemical from Momordica chlarantia) was studied on cardiovascular system

(Desai and Tatke, 2015). At the dose of 800 mg/kg, 5-10% of blood pressure lowering of anaesthetized cat was

observed. In another study aimed at evaluating possible cardio-protective properties of Momordica charantia by

determining its effect on blood cholesterol levels in albino rats was carried out by Sheriff and Yusuf (Sheriff et

al. 2013). Results indicated that the plant’s extract significantly reduced low density lipoprotein (LDL) levels

(P<0.05) in the experimental group A (80mg/kg), when compared to the control group. Together, these studies

showed that Momordica charantia plant extract has cardio-protective properties by its dose-dependent effects on

blood cholesterol and blood pressure. However, there is an indication that higher doses should be discouraged,

since it is rather increase low density lipoprotein (LDL) levels in the blood.

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Wound healing activity:

Researchers (Sankaranarayanan et al., 1993) found that Momordica charantia fruit powder, in the form of

an ointment (10% w/w dried powder in simple ointment base), showed a statically significant response (P <

0.01), in terms of wound-contracting ability, wound closure time, period of epithelization, tensile strength of the

wound and regeneration of tissues at wound site when compared with the control group, and these results were

comparable to those of a reference drug povidone iodine ointment in an excision, incision and dead space

wound model in rats.

Body weight decrease activity:

In a study, Farhat Bano et al administered orally the aqueous extract of Momordica charantia fruit to

overweight rats in order to assess the effect of this extract on body weight of the rats (Farhat Bano et al., 2011).

Five weeks treatment not only showed significant decrease in body weight of rats but there was also significant

decrease in blood glucose, total cholesterol, triglyceride and LDL-cholesterol. Moreover, there was increase in

HDL-cholesterol levels in serum. This result clearly showed a decrease in body weight with many other

advantages. Hence, this plant’s extract can be used against obesity, which not only increases the risk of

cardiovascular diseases but is also responsible of certain types of cancer and osteoarthritis.

Antifeedant activity:

Yaqui (Yaqui, 2002) demonstrated that methanolic extract of M. charantia leaves inhibited feeding of two

armyworm larvae, Spodoptera litura and Pseudaletia seperata. Momordicin II, a triterpene monoglucoside from

the plant extract was identified as an antifeedant compound.

Neuroprotective effect:

Momordica charantia possesses neuroprotective effects on High-Fat Diet-associated blood brain barrier

disruption, stress and neuro-inflammatory cytokines [Nerurkar et al. 2011]. In fact, Malik et al. (Malik et al.,

2011) showed that cerebral oxidative stress and damage, and neurological deficits were dose dependently

attenuated by pre-treatment with the lyophilized this pant’s juice (200-800 mg /kg).

Antipyretic effect:

The ethanolic extracts (500 mg/ kg) of Momordica charantia fruit showed antipyretic effect in a study

which was carried out using yeast-induced pyrexia in rats. The authors stated that the antipyretic activity of

Momordica charantia may be due to the individual or combined action of bioactive constituents present in it

(Patel et al., 2010).

Anti-diarrheal activity:

The anti-diarrheal activity of aqueous leaf extract of Momordica chlorantia was evaluated on castor oil-

induced diarrhea, gastro-intestinal transit, intestinal fluid accumulation and gastric emptying in rats (Bakare et

al., 2011). The aqueous extract of the plant showed inhibitory activity against castor oil-induced diarrhea. A

significant reduction (p<0.05) in the gastro-intestinal mobility in charcoal meal test in rats was observed. The

extract decreased the volume of intestinal secretion induced by castor oil with a significant effect (p<0.05) on

the gastric emptying of the test animals compared to the control rats. Inhibition of the gastro-intestinal

propulsion and fluid by the extract suggest it might exert its anti-diarrheal activity by anti-secretory mechanism.

Larvicidal activity:

Bioassays with crude extract of Momordica charantia against larvae of Anopheles stephensi, Culex

quinquefasciatus and Aedes aegypti revealed the LC50 values of 0.50, 1.29 and 1.45%, respectively (Singh et

al., 2006). Further, in bioassays hexane extract showed more potent larvicidal activity than the crude extract,

indicating the non-polar characteristics of larvicidal components (Singh et al. 2006). The LC50 values of hexane

extract against larvae of Anopheles stephensi, Culex quinquefasciatus and Aedes aegypti were 66.05, 96.11 and

122.45 ppm, respectively. The results revealed that the larvae of Anopheles stephensi were more susceptible in

comparison to the larvae of Culex quinquefasciatus and Aedes aegypti. However, further studies to identify the

larvicidal components are needed. Hence the larvicidal action of the fruits extract of this plant could be

exploited for use in potable waters against mosquito larvae. This plant’s activity against Anopheles stephensi

has recently been confirmed by Jayapal et al (Jayapal et al., 2012).

Antifertility effects:

Tumkiratiwong et al investigated the antifertility effect of Momordica charantia ethanol seed extracts on

reproductive male Wistar rats (Tumkiratiwong et al., 2014). Their data showed that high dose of this plant seed

extracts caused infertility in male rats. They said that the interruption in the fertility is probably attributed to the

direct toxic to seminiferous tubules, epididymis and the lowered testosterone level which might impact on sperm

33 Olivier Tene Tcheghebe et al., 2016/ Global Journal of Medicinal Plant Research, 4(4): 23-39, 2016

parameters. This plant has also shown to have potent male antifertility effects when ethanol seed extracts were

administered to dogs (Dixit et al., 1978) and guinea pigs (Udoh et al., 2001). The plant extract also has

antifertility effect on female animals. In fact in an experiment aimed at determining the effect of graded doses of

aqueous leaf extracts of Momordica charantia on fertility hormones of female albino rats (Adewale et al., 2014).

Twenty adult, healthy, female Wistar rats were divided into four groups: low dose (LD), moderate dose (MD)

and high dose (HD) groups which received 12.5 g, 25.0 g, 50.0 g of the leaf extract respectively and control

group that was given with water ad libatum. The result showed reduction of estrogen levels by 6.40 nmol/L,

10.80 nmol/L and 28.00 nmol/L in the LD, MD and HD groups respectively, while plasma progesterone of rats

in the LD, MD and HD groups reduced by 24.20 nmol/L, 40.8 nmol/L and 59.20 nmol/L respectively. This

study has shown the antifertility effect of Momordica charantia, achieved in a dose dependent manner. Stepka et

al also demonstrated an in vivo antifertility effect of fruit and leaf of bitter melon in female animals (Stepka et

al., 1974). Hence, cautious use of such medication should be advocated especially seed extract at high doses,

when managing couples for infertility.

Anti-gout:

Intisar Reehem et al carried out a study, in order to screen some plant species growing wild with respect to

their xanthine oxidase inhibition activity which may be potentially useful for the treatment of gout or other

xanthine oxidase - induced diseases (Alsultanee et al., 2014). Their aqueous extracts, prepared from used parts,

were tested in vitro, at 100 μg/mL concentrations, for their inhibition potencies expressed as % inhibition of

xanthine oxidase activity. Two of the test plants were found inhibition % activity of xanthine oxidase, namely

Zingiber officinale (81.56±3.76) and Momordica charantia (96.5±2.17). Total Phenolic of Momordica

charantia(80.83±0.30) was more than Zingiber officinat(62.18±0.65). Fraction of Momordica charantia

(coumarin) was achieved the highest activity (inhibition activity of xanthine oxidase 97%) based on analysis

HPLC. Data showed that coumarin (0.5 mg/kg) treatment cause significant reduction in the serum uric acid level

of hyperuricemia in normal mice. These finding suggest that Momordica charantia extracts possess prominent

medicinal properties and can be exploited as natural drug to treat gout and other diseases associated with

inflammation, free radical formation, oxidative stress, xanthine oxidase activity and hyperuricemia.

Effect on Haemoglobin Concentration:

A research work was carried out to investigate the effect of the aqueous extract of Momordica charantia on

hemoglobin concentration in albino rats (Adedeji et al., 2014). The aqueous extract of the plant’s leaves was

prepared and given orally at doses of 80, 100, 120 and 140 mg/kg body weight daily to the experimental

animals. Hemoglobin concentration was then determined after two weeks of administration. The results of the

work showed a significant (p<0.05) decrease in mean hemoglobin concentration in test animals, in comparison

with the control. Hence, oral administration of aqueous extract of Momordica charantia causes a decrease in

hemoglobin concentration which can lead to anemia.

Cultural values:

Many healers in Togo indicated that the plant has powerful medico-spiritual properties, providing

protection against curses, diseases, evil spirits, spells and madness (Beloin et al., 2005). It is also claimed to aid

in obtaining favors. It is claimed to be a purifying plant that is used before the manipulation of sacred objects.

Many original details concerning the ritual and historical aspects of Momordica charantia were recounted by

some healers from Southern Togo. The plant is used in traditional ceremonies linking the living to the ancestors,

particularly among the Guin tribe of coastal Togo. The ancestors of the Guin lived on the coast of Ghana near

what is today the area of Elabadi in Accra. In mid-1600, they fled intertribal warfare fueled by the slave trade

and moved to the east into what is now Togo [Cornevin, 1969]. According to oral tradition, they wore a

necklace of Momordica vines which repelled their enemies and allowed the tribe to journey in safety to their

new home at Glidji-Kpodji on the northern side of Lake Togo. The plant is considered a powerful charm to this

day and is worn as a necklace, wrist or ankle bracelet or crown at traditional ceremonies. Its name in Mina, the

dialect language of the Guin, is ‘guinsika’ (gold of the Guin) or ‘guingbe’ (plant of the Guin). The plant is

widely used in traditional ceremonies, including the famous consultation of the oracle named Epe-Ekpe or

Ekpessosso, during which a sacred stone is uncovered to predict the fortunes of the coming year (Piraux, 1977).

The king of the Guin, which is also the fetish priest of the sacred forest of Glidji-Kpodji, and his male attendants

(vodussi) at the ceremony wear Momordica vine for its purification properties. The ritual ceremonial importance

of the plant is accompanied by its considerable reputation as a medicinal plant for the treatment of disease.

Reported toxicity:

A work aimed to assess the acute oral toxicity effects of Momordica charantia in Sprague Dawley rats was

conducted by Husna et al (Husna et al., 2013). The extract was administered orally at two different doses of 300

mg/kg and 2000 mg/kg of body weight. The toxicity signs were recorded within the first 24 hours after forced

34 Olivier Tene Tcheghebe et al., 2016/ Global Journal of Medicinal Plant Research, 4(4): 23-39, 2016

feeding. Both of the treated groups showed dizziness and depression during the first 30 minutes. However, no

significant difference of feeding patterns which included water, food intake and body weight gain were

observed. Haematological evaluations did not show significant differences in white blood cells count, mean

corpuscular volume and mean corpuscular haemoglobin concentration levels. However, red blood cells count

and packed cell volume percentage was significantly lower in rats that received 2000 mg/kg than those of the

other two groups. Meanwhile, haemoglobin count and the relative liver weight of rats received 2000 mg/kg

body weight of extract decreased significantly (p<0.05) as compared with the control group. This result was

previously found by two studies which proved that Momordica chlorantia is safe (no signs of nephrotoxicity and

hepatotoxicity and any adverse influence on the food intake, growth organ weights and hematological

parameters) in experimental animals when ingested in low doses up to 2 months (Platel et al., 1993; Virdi et al.,

2003). Thus, these studies are expected to be beneficial for clinical and traditional applications, for safe

consumption and to utilize Momordica charantia as a remedy at a recommended dosage.

Conclusion:

More than 80% of the population in developing continues to use folkloric medicine in their primary medical

problems. Therefore, researches have been focused on scientific evaluation of traditional drugs of plant origin

for the development of new and more potent drugs. Momordica charantia is among those plants currently

involved in the treatment of various diseases, and particularly diabetes and cancers. In the traditional medicine,

Momordica chlarantia is involved in the treatment of almost all the diseases of the human body and sometime

to cure animal and plants infections. The cases where it is most involved include the treatment of cancers,

diabetes, and to fight viruses; the treatment of cardiac, liver and kidney diseases, as well as gynaecological

problems. Many traditional practitioners consider it as a powerful medico-spiritual plant since it is said to

provide protection against curses, diseases, evil spirits, spells and madness. It is also claimed to aid in obtaining

favors or to be a purifying plant that is used before the manipulation of sacred objects. Pharmacological tests

carried out on this plant for its antioxidant, antimalarial, hypocholesterolemic, trypanocidal, hepatocurative and

hepatoprotective, gastroprotective and anti-ulcer, anthelmintic, immunomodulatory, anti-inflammatory and

analgesic, antiviral, anti-genotoxic, anti-tumour and anticancer, anti-hepatitis b virus, abortifacient,

antimicrobial and antibacterial, hypoglycemic and anti-diabetic, cardiovascular, wound healing, body weight

decrease, antifeedant, neuroprotective, antipyretic, anti-diarrheal, larvicidal, antifertility, anti-gout activities; its

effect on haemoglobin concentration and on diabetic complications revealed positive results without significant

adverse side effects. Some bioactive constituents such alkaloids, tannins, flavonoids, saponins, glycosides,

sterols, mucilages and oleanolic acids significantly present in the plant extracts support its numerous properties

and uses in traditional medicine, while its rich content in moisture, ash, crude lipid, crude fibre, crude protein,

carbohydrates, minerals and vitamins validate its high nutritional value. Momordicin, Chlarantin, Vicine,

Kuguacin J, EMCDO, Cucurbitacin figure among the most important purified bioactive constituents isolated

from this plants which support its traditional use for the treatment of various diseases and justify its multiple

pharmacological activities. It is however notable that, pregnant women should not eat bitter melon or consume

this plant’s extracts as it stimulates the uterus and may cause premature birth. We do not pretend to have

examined all the studies related to this medicinal plant. However, we sincerely hope that we have provided a

data base for proper evaluation of Momordica charantia extracts which could lead to the discovery of new and

more effective drugs.

ACKNOWLEDGEMENTS

Authors sincerely thank their respective families’ members and friends for their kind encouragements.

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