Capsule Karela

Latin name: Momordica Charantia
Family: Cucurbitaceae
Common name: karela
English name: bitter gourd, bitter melon

Habitat: Bitter gourd, also known as balsam pear, is a tropical vegetable widely cultivated in Asia, Africa and South America

Macroscopic identification: a monoecious climber with oblong,green colored fruit that is extensively ribbed.

Parts used: fruits, seeds and leaves

Pharmacological action:
Fruit is tonic, stomachic, stimulant, emetic, anti bilious, laxative and alterative. Fruit pulp, leaf juice and seeds are antihelimintic. Leaves act as galactogogue. Root is astringent.

Anthelmintic, antibacterial, antibiotic, antidiabetic, anti-inflammatory, anti microbial, antileukemic, antimutagenic, antimycobacterial, antioxidant, antitumor, antiulcer, antiviral, aperitive, aphrodisiac, astringent, carminative, cytostatic, cytotoxic, depurative, hormonal, hypocholesterolemic, hypotensive, hypotriglyceridemic, hypoglycemic, immunostimulant, insecticidal, lactagogue, laxative, purgative, refrigerant, stomachic, styptic, tonic, vermifuge

Action and uses in Ayurveda: kustha, prameha, kamala, pandu, krimiroga, raktvikara, jvara, svasa, kasa, aruchi.

Indications: skin disorders and diabetes

Photochemical:
At least three different groups of constituents in bitter melon have been reported to have hypoglycemic (blood sugar lowering) or other actions of potential benefit in diabetes mellitus. These include a mixture of steroidal saponins known as charantin, insulin-like peptides, and alkaloids. It is still unclear which of these is most effective or if all three work together. Two proteins, known as alpha- and beta-momorcharin, inhibit the AIDS virus, but this research has only been demonstrated in test tubes and not in humans
Alkaloids, charantin, charine, cryptoxanthin, cucurbitins, cucurbitacins, cucurbitanes, cycloartenols, diosgenin, elaeostearic acids, erythrodiol, galacturonic acids, gentisic acid, goyaglycosides, goyasaponins, guanylate cyclase inhibitors, gypsogenin, hydroxytryptamines, karounidiols, lanosterol, lauric acid, linoleic acid, linolenic acid, momorcharasides, momorcharins, momordenol, momordicilin, momordicins, momordicinin, momordicosides, momordin, momordolo, multiflorenol, myristic acid, nerolidol, oleanolic acid, oleic acid, oxalic acid, pentadecans, peptides, petroselinic acid, polypeptides, proteins, ribosome-inactivating proteins, rosmarinic acid, rubixanthin, spinasterol, steroidal glycosides, stigmasta-diols, stigmasterol, taraxerol, trehalose, trypsin inhibitors, uracil, vacine, v-insulin, verbascoside, vicine, zeatin, zeatin riboside, zeaxanthin, zeinoxanthin
Amino acids-aspartic acid, serine, glutamic acid, thscinne, alanine, g-amino butyric acid and pipecolic acid

Properties and action:
Rasa: tikta, katu
Guna: laghu
Virya: usna
Vipaka: katu
Karma: mutrsangrehiya

Preparations: extract, oil, and powder

Therapeutic classification index:

• Central nervous system: it dissipates melancholia and gross humors.
• Liver and biliary system: fruit is useful in sub acute cases of liver and spleen.
• Blood and haemopoeitic tissue: The ripe fruit of bitter melon has been shown to exhibit some remarkable anticancer effects, especially leukemia. It purifies the blood
• Digestive system: leaf juice is purgative and emetic.
• Respiratory system:
• Skin: fruit and leaves are used in leprosy. Bitter melon inhibits the enzyme guanylate cyclase, that may benefit people with psoriasis
• Reproductive system: leaves act as a galactogogue

Use Of Bitter Gourd In Reducing Blood Sugar:

1. Charantin is more powerful than the drug tolbutamide, which is sometimes used in the treatment of diabetes to lower the blood sugar levels Bitter melon is composed of several compounds with confirmed anti-diabetic properties. Charantin, extracted by alcohol, is a hypoglycemic agent composed of mixed steroids that is more potent than the drug tolbutamide, which is often used in the treatment of diabetes. Momordica also contains an insulin-like polypeptide, polypeptide-P, which lowers blood sugar levels when injected subcutaneously into type 1 diabetic patients. The oral administration of 50-60 ml of the juice has shown good results in clinical trials.
   Excessively high doses of bitter melon juice can cause abdominal pain and diarrhea. Small children or anyone with hypoglycemia should not take bitter melon, since this herb could theoretically trigger or worsen low blood sugar, or hypoglycemia. Furthermore, diabetics taking hypoglycemic drugs (such as chlorpropamide, glyburide, or phenformin) or insulin should use bitter melon with caution, as it may potentiate the effectiveness of the drugs, leading to severe hypoglycemia.
2. Improvement in glucose tolerance due to Momordica charantia (karela).
   Leatherdale BA, Panesar RK, Singh G, Atkins TW, Bailey CJ, Bignell AH.
   The effect of karela (Momordica charantia), a fruit indigenous to South America and Asia, on glucose and insulin concentrations was studied in nine non-insulin-dependent diabetics and six non-diabetic laboratory rats. A water-soluble extract of the fruits significantly reduced blood glucose concentrations during a 50 g oral glucose tolerance test in the diabetics and after force-feeding in the rats. Fried karela fruits consumed as a daily supplement to the diet produced a small but significant improvement in glucose tolerance. Improvement in glucose tolerance was not associated with an increase in serum insulin responses. These results show that karela improves glucose tolerance in diabetes. Doctors supervising Asian diabetics should be aware of the fruit's hypoglycaemic properties.
3. Effect of Momordica charantia on the glucose tolerance in maturity onset diabetes.
   Welihinda J, Karunanayake EH, Sheriff MH, Jayasinghe KS.
   Investigations were carried out to evaluate the effect of Momordica charantia on the glucose tolerance of maturity onset diabetic patients. The fruit juice of M. charantia was found to significantly improve the glucose tolerance of 73% of the patients investigated while the other 27% failed to respond.

Anti cancerous effect of bitter gourd:
A novel phytochemical in bitter melon has clinically demonstrated the ability to inhibit an enzyme named guanylate cyclase. This enzyme is thought to be linked to the pathogenesis and replication of not only psoriasis, but leukemia and cancer as well. Other phytochemicals that have been documented with cytotoxic activity are a group of ribosome-inactivating proteins named alpha- and beta-momorcharin, momordin, and cucurbitacin B. A chemical analog of bitter melon proteins was developed and named MAP-30 and its inventors reported that it was able to inhibit prostate tumor growth. The phytochemical momordin has clinically demonstrated cytotoxic activity against Hodgkin's lymphoma in vivo, and several other in vivo studies have demonstrated the cytostatic and antitumor activity of the entire plant of bitter melon. In one study, a water extract blocked the growth of rat prostate carcinoma; another study reported that a hot water extract of the entire plant inhibited the development of mammary tumors in mice. Numerous in vitro studies have also demonstrated the anti-cancerous and anti-leukemic activity of bitter melon against numerous cell lines including liver cancer, human leukemia, melanoma and solid sarcomas.

Anti-viral effect of bitter gourd-esp in HIV Virus

1. Bitter melon (and several of its isolated phytochemicals) also has been documented with in vitro antiviral activity against numerous viruses including Epstein-Barr, herpes, and HIV viruses. In an 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). Two proteins known as alpha- and beta-momorcharin (which are present in the seeds, fruit, and leaves) have been reported to inhibit the HIV virus in vitro. In one study, HIV-infected cells treated with alpha- and beta-momorcharin showed a nearly complete loss of viral antigen while healthy cells were largely unaffected. In 1996 the inventors of the chemical protein analog MAP-30 filed a U.S. patent, stating it was "useful for treating tumors and HIV infections . . . In treating HIV infections, the protein is administered alone or in conjunction with conventional AIDS therapies." Another clinical study showed that MAP-30's antiviral activity was also relative to the herpes virus in vitro.
2. An abstract from an article published by Eric von Wettberg Biological and sociological aspects of the use of Momordica Charantia to treat HIV infection
   The use of Momordica Charantia. M. Charantia, a member of the Cucurbitaceae family, is a tropical plant currently distributed across the globe. It is used both as a food item and as a wide-ranging Materia medical in many traditional medical systems. Because of its widespread use and economic importance, the plant has long been a research focus for scientists at scientific institutions in countries where it is found. One of these researchers, T.B. Ng at the Chinese Medicinal Material Research Center of the Chinese University of Hong Kong, found a series of proteins, dubbed the alpha and beta momorcharins, that have anti-HIV activity, among other things. More recently, Sylvia Lee-Huang, a biochemist at the NYU School of medicine, isolated another protein, MAP30 (Momordica anti-viral protein of 30 Daltons) that also has anti-HIV activity. These two discoveries have considerable potential for the treatment of HIV, possibly providing new drugs to complement those already used to treat HIV or cheaper alternatives for those who can't access the drugs already available
   Instead, the only published literature since then on the anti-HIV properties of constituents of M. charantia has been done by Sylvia Lee-Huang at the New York University medical school. This work has focused on MAP30, a Momordica Anti-HIV protein of 30 kDa. This protein is 48% homologous to alpha momorcharin, but is distinct in its properties (Lee-Huang, et. al. 1995a gene). This work has illuminated more specific details of how MAP30 acts against HIV than the equivalent work on alpha momorcharin. Preliminary work showed that MAP30 can both block the infection of T lymphocytes and monocytes by HIV, and inhibit the replication of HIV in already infected cells in vitro (Lee-Huang, et. al., 1990). Furthermore, MAP30 appears to have very limited toxicity to uninfected cells (Lee-Huang, et. al., 1990). Although MAP30 has a translational inhibitory power, it appears to be unable to enter uninfected cells (Lee-Huang, et. al., 1995a).
3. Inhibition of the integrase of human immunodeficiency virus (HIV) type 1 by anti-HIV plant proteins MAP30 and GAP31.
   Lee-Huang S, Huang PL, Huang PL, Bourinbaiar AS, Chen HC, Kung HF.
   Department of Biochemistry, New York University School of Medicine, NY 10016, USA.
   
   MAP30 (Momordica anti-HIV protein of 30 kDa) and GAP31 (Gelonium anti-HIV protein of 31 kDa) are anti-HIV plant proteins that we have identified, purified, and cloned from the medicinal plants Momordica Charantia and Gelonium multiflorum. These antiviral agents are capable of inhibiting infection of HIV type 1 (HIV-1) in T lymphocytes and monocytes as well as replication of the virus in already-infected cells. They are not toxic to normal uninfected cells because they are unable to enter healthy cells. MAP30 and GAP31 also possess an N-glycosidase activity on 28S ribosomal RNA and a topological activity on plasmid and viral DNAs including HIV-1 long terminal repeats (LTRs). LTRs are essential sites for integration of viral DNA into the host genome by viral integrase. We therefore investigated the effect of MAP30 and GAP31 on HIV-1 integrase. We report that both of these antiviral agents exhibit dose-dependent inhibition of HIV-1 integrase. Inhibition was observed in all of the three specific reactions catalyzed by the integrase, namely, 3' processing (specific cleavage of the dinucleotide GT from the viral substrate), strand transfer (integration), and "disintegration" (the reversal of strand transfer). Inhibition was studied by using oligonucleotide substrates with sequences corresponding to the U3 and U5 regions of HIV LTR. In the presence of 20 ng of viral substrate, 50 ng of target substrate, and 4-microM integrase, total inhibition was achieved at equimolar concentrations of the integrase and the antiviral proteins, with EC50 values of about 1 microM. Integration of viral DNA into the host chromosome is a vital step in the replicative cycle of retroviruses, including the AIDS virus. The inhibition of HIV-1 integrase by MAP30 and GAP31 suggests that impediment of viral DNA integration may play a key role in the anti-HIV activity of these plant proteins.

Broad spectrum anti microbial activity of bitter gourd

1. In addition to these properties, leaf extracts of bitter melon have clinically demonstrated broad spectrum antimicrobial activity. Various water, ethanol, and methanol extracts of the leaves have demonstrated in vitro antibacterial activities against E. coli, Staphylococcus, Pseudomonas, Salmonella, Streptobacillus and Streptococcus; an extract of the entire plant was shown to have antiprotozoal activity against Entamoeba histolytica. The fruit and fruit juice has demonstrated the same type of antibacterial properties and, in another study, a fruit extract has demonstrated activity against the stomach ulcer-causing bacteria Helicobacter pylori.
2. The activity of plant-derived antiretroviral proteins MAP30 and GAP31 against herpes simplex virus in vitro.
   Bourinbaiar AS, Lee-Huang S.
   Department of Biochemistry, New York University School of Medicine, New York 10016, USA.
   
   We examined the effect on anti-HIV proteins MAP30 and GAP31, from Momordica Charantia and Gelonium multiflorum, on the infection and replication of Herpes Simplex Viruses (HSV). Human lung WI-38 fibroblasts cultured in the presence of tenfold dilutions of MAP30 or GAP31 were exposed to HSV and viral yield was measured at 24-48 hours by ELISA method. The effective concentrations for 50% inhibitions (EC50) were 0.1-0.2 microM for HSV-2, and 0.3-0.5 microM for HSV-1 for MAP30 and GAP31, respectively. In comparison, the EC (50) for acyclovir (ACV), a commonly used anti-HSV drug, was 0.2 and 1.7 microM for HSV-2 and HSV-1, respectively. The cytotoxicity of all three antiviral was negligible and comparable. However, the anti herpetic activity of the plant proteins against acyclovir-resistant strains was two to three logs more potent than ACV. These results suggest that MAP30 and GAP31, previously shown to be active against HIV, may be useful for the therapy of herpes virus infections

Bitter melon seed extracts shown to have male anti-fertility effects
Naseem M, Patil S, Patil S, et al. Antispermatogenic and androgenic activities of Momordica charantia (Karela) in albino rats. J Ethnopharmacology 1998; 61: 9-16

Herbal preparations have been used since antiquity to reduce female fertility. Though male anti-fertility preparations are less common, modern research has demonstrated antispermatogenic activities of extracts from at least seven plants. In this study, various extracts (ether, benzene and alcohol) of M. charantia seeds were administered orally and intraperitoneally to male rats for 35 days. All three extracts demonstrated antispermatogenic activity, with the ethanol extract being the most potent. Antispermatogenic activity was assessed using measurements of the weight of the testes and other measures. These tests showed indirect evidence of reduced availability of pituitary gonadotrophs necessary for spermatogenesis. With intraperitoneal administration, increased cholesterol and Sudanophilic lipid levels denoted inhibited steroidogenesis, further evidence of reduced availability of gonadotrophs.

Dose: Fresh juice -10-20 ml

Capsule Karela contains pure and concentrated Karela.
Dosage :one capsule twice a day, before meals.
Package size: 60 capsules.

References:

1. Dr.KM Nadkarni, The Indian Materia Medica, Vol.I, pg 805
2. Prof P.V Sharma, Dravya Guna Vigyana, Vol II, pg 684
3. The Ayurvedic Pharmacopoeia Of India, Part I, Vol.II, pg 83