Bitter melon (BM) is known for its hypoglycemic effect but its effect on rats fed a hyperinsulinemic high fat diet has not been examined. In a dose-response (0.375, 0.75 and 1.5%) study, oral glucose tolerance was improved in rats fed a high fat (HF; 30%) diet supplemented with freeze-dried BM juice at a dose of 0.75% or higher (P < 0.05). At the highest dose, BM-supplemented rats had lower energy efficiency (P < 0.05) and tended (P = 0.10) to have less visceral fat mass. In a subsequent experiment, rats habitually fed a HF diet either continued to consume the diet or were switched to a HF+BM, low fat (LF; 7%) or LF+BM diet for 7 wk. BM was added at 0.75%. Final body weight and visceral fat mass of the two last-mentioned groups were similar to those of rats fed a LF diet for the entire duration. Rats switched to the HF+BM diet gained less weight and had less visceral fat than those fed the HF diet (P < 0.05). The addition of BM did not change apparent fat absorption. BM supplementation to the HF diet improved insulin resistance, lowered serum insulin and leptin but raised serum free fatty acid concentration (P < 0.05). This study reveals for the first time that BM reduces adiposity in rats fed a HF diet. BM appears to have multiple influences on glucose and lipid metabolism that strongly counteract the untoward effects of a high fat diet.
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Momordica charantia L., also known as bitter melon, has been shown to ameliorate obesity and insulin resistance. However, metabolic changes regulated by M. charantia in obesity are not clearly understood. In this study, serums obtained from obese and M. charantia-treated mice were analyzed by using gas and liquid chromatography-mass spectrometry, and multivariate statistical analysis was performed by Orthogonal partial least squares discriminant analysis. The results from this study indicated that body weight fat and insulin levels of obese mice are dramatically suppressed by 8 weeks of dietary supplementation of M. charantia. Metabolomic data revealed that overproductions of energy and nutrient metabolism in obese mice were restored by M. charantia treatment. The antiinflammatory and inhibition of insulin resistance effect of M. charantia in obesity was illustrated with the restoration of free fatty acids and eicosanoids. The findings achieved in this study further strengthen the therapeutic value of using M. charantia to treat obesity. Copyright © 2016 John Wiley & Sons, Ltd.
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In this study, we evaluated the extract of M. charantia for its antiepimastigote, antifungal, and cytotoxic activities.
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Momordica charantia Linn. (Cucurbitaceae) fruit is commonly known as bitter melon. C57BL/6J mice were firstly divided randomly into two groups: the control (CON) group was fed with a low-fat diet, whereas the experimental group was fed a 45% high-fat (HF) diet for 8 weeks. Afterwards, the CON group was treated with vehicle, whereas the HF group was subdivided into five groups and still on HF diet and was given orally M. charantia extract (MCE) or rosiglitazone (Rosi) or not for 4 weeks. M. charantia decreased the weights of visceral fat and caused glucose lowering. AMP-activated protein kinase (AMPK) is a major cellular regulator of lipid and glucose metabolism. MCE significantly increases the hepatic protein contents of AMPK phosphorylation by 126.2-297.3% and reduces expression of phosphenolpyruvate carboxykinase (PEPCK) and glucose production. Most importantly, MCE decreased expression of hepatic 11beta hydroxysteroid dehydroxygenase (11beta-HSD1) gene, which contributed in attenuating diabetic state. Furthermore, MCE lowered serum triglycerides (TGs) by inhibition of hepatic fatty acid synthesis by dampening sterol response element binding protein 1c and fatty acid synthase mRNA leading to reduction in TGs synthesis. This study demonstrates M. charantia ameliorates diabetic and hyperlipidemic state in HF-fed mice occurred by regulation of hepatic PEPCK, 11beta-HSD1 and AMPK phosphorylation.
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Sensitivity of 100 Plasmodium falciparum isolates to chloroquine, quinine, amodiaquine, mefloquine, sulphadoxine/pyrimethamine, artemisinin, Momordica charantia ('Ejirin') Diospyros monbuttensis ('Egun eja') and Morinda lucida ('Oruwo') was determined using the in vitro microtest (Mark III) technique to determine the IC50 of the drugs. All the isolates tested were sensitive to quinine, mefloquine and artesunate. Fifty-one percent of the isolates were resistant to chloroquine, 13% to amodiaquine and 5% to sulphadoxine/pyrimethamine. Highest resistance to chloroquine (68.9%) was recorded among isolates from Yewa zone while highest resistance to amodiaquine (30%) was observed in Ijebu zone. Highest resistance to sulphadoxine/pyrimethamine was recorded in Yewa and Egba zones, respectively. A positive correlation was observed between the responses to artemisinin and mefloquine (P<0.05), artemisinin and quinine (P<0.05) and quinine and mefloquine (P<0.05). A negative correlation was observed between the responses to chloroquine and mefloquine (P>0.05). Highest anti-plasmodial activity was obtained with the ethanolic extract of D. monbuttensis (IC50 = 3.2 nM) while the lowest was obtained from M. lucida (IC50 = 25 nM).
Deep sequencing using 454 technology with non-normalized and normalized cDNA libraries prepared from bitter melon seeds at 18 DAP resulted in the identification of transcripts for the vast majority of known genes involved in fatty acid and triacylglycerol biosynthesis. The non-normalized library provided a transcriptome profile of the early stage in seed development that highlighted the abundance of transcripts for genes encoding seed storage proteins as well as for a number of genes for lipid metabolism-associated polypeptides, including Δ12 oleic acid desaturases and fatty acid conjugases, class 3 lipases, acyl-carrier protein, and acyl-CoA binding protein. Normalization of cDNA by use of a duplex-specific nuclease method not only increased the overall discovery of genes from developing bitter melon seeds, but also resulted in the identification of 345 contigs with homology to 189 known lipid genes in Arabidopsis. These included candidate genes for eleostearic acid metabolism such as diacylglycerol acyltransferase 1 and 2, and a phospholipid:diacylglycerol acyltransferase 1-related enzyme. Transcripts were also identified for a novel FAD2 gene encoding a functional Δ12 oleic acid desaturase with potential implications for eleostearic acid biosynthesis.
Momordica charantia (MC; bitter gourd) is a traditional herb commonly used for its antidiabetic, antioxidant, contraceptive and antibacterial properties. It is also used for the rapid healing of wounds.
Diabetes was induced in Wistar rats by a s.c., subcutaneous injection of alloxan monohydrate (100 mg/kg) in acetate buffer (pH 4.5). MCE and glibenclamide were administered orally to alloxan diabetic rats at doses of 150 mg/kg, 300 mg/kg & 600 mg/kg, and 4 mg/kg respectively for 30 days, blood was withdrawn for glucose determination on 0, 7, 14, 21 and 30th days. On the 31st day, overnight fasted rats were sacrificed and blood was collected for various biochemical estimations including glycosylated haemoglobin, mean blood glucose, serum insulin, cholesterol, triglcerides, protein and glycogen content of liver. The hemidiaphragms and livers were also isolated, carefully excised and placed immediately in ice cooled perfusion solution and processed to study the glucose uptake/transfer processes. Hypolipidemic activity in old obese rats was evaluated by treating two groups with MCE (150 mg/kg & 300 mg/kg) orally for 30 days and determining total cholesterol, triglyceride and HDL-CH, LDL-CH and VLDL-CH levels from serum samples.
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The anti-ulcerogenic effect of the oily extract of Momordica charantia fruits was investigated in male Sprague-Dawley rats. Animals were separated into six groups. Distilled water (control group), famotidine (40 mg/kg), oily extracts (5 and 10 ml/kg), and vehicles (olive oil -5 and 10 ml/kg) were given orally (gavage). Thirty minutes later indomethacin (25 mg/kg) was administrated to all the groups. Six hours later, animals were killed with decapitation. For each stomach, ulcerated and total areas were measured (mm2). The ulcer indexes for each stomach and the ulcer inhibition rates for each group were calculated, after which the stomachs were evaluated pathologically (polymorphonuclear leukocytes infiltration).
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The ribonuclease MC1 (RNase MC1) from seeds of bitter gourd (Momordica charantia) consists of 190 amino acid residues with four disulfide bridges and belongs to the RNase T(2) family, including fungal RNases typified by RNase Rh from Rhizopus niveus and RNase T(2) from Aspergillus oryzae. The crystal structure of RNase MC1 has been determined at 1.75 A resolution with an R-factor of 19.7% using the single isomorphous replacement method. RNase MC1 structurally belongs to the (alpha+beta) class of proteins, having ten helices (six alpha-helices and four 3(10)-helices) and eight beta-strands. When the structures of RNase MC1 and RNase Rh are superposed, the close agreement between the alpha-carbon positions for the total structure is obvious: the root mean square deviations calculated only for structurally related 151 alpha-carbon atoms of RNase MC1 and RNase Rh molecules was 1.76 A. Furthermore, the conformation of the catalytic residues His-46, Glu-105, and His-109 in RNase Rh can be easily superposed with that of the possible catalytic residues His-34, Glu-84, and His-88 in RNase MC1. This observation strongly indicates that RNase MC1 from a plant origin catalyzes RNA degradation in a similar manner as fungal RNases.
Momordica charantia (MC) is a common oriental vegetable with known antidiabetic, laxative and antimicrobial properties. This study investigates the effects of aqueous fruit extract of MC on the transport of d-glucose, l-tyrosine and fluid across rat-everted intestine in vitro. Everted intestinal sacs from rats were mounted in an organ bath containing Krebs-Henseleit bicarbonate buffer. Graded concentrations (1.5-12mg/ml) of MC fruit extract were incubated in the mucosal solution with and without exogenous ATP in the mucosal bathing fluid. The serosal appearance and mucosal disappearance of d-glucose, l-tyrosine and the fluid absorptive capacity of the intestine were significantly inhibited (p<0.05) with increasing graded concentrations of MC. The concentration of d-glucose accumulated or metabolized by the enterocytes in the intestinal tissues were significantly higher (p<0.05) when incubated with MC. Increasing graded concentrations of exogenous ATP (25-200 microM) were incubated with 3.0mg/ml MC to confirm inhibition of the ATP-dependent active transport of d-glucose, l-tyrosine and fluid across rat enterocytes. It was found that increasing concentrations of mucosal ATP from 25 to 100 microM significantly (p<0.05) reverses the MC-depression of the d-glucose, l-tyrosine and fluid uptake across rat everted intestinal sacs. It is hypothesized that bioactive phytochemicals such as saponins in MC fruit extract inhibits the active transport of d-glucose, l-tyrosine and fluid across rat intestine by inhibiting the production of ATP responsible for the active transport of these molecules. It is likely that MC can be a potential alternative drug therapy of postprandial hyperglycaemia via inhibition of glucose uptake across the small intestine.
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This paper is based on ethnobotanical interviews conducted from 1996-2000 in Trinidad and Tobago with thirty male and female respondents.
This review describes the nature and applications of ribosome inactivating proteins (RIPs) from Momordica charantia (bitter melon). RIPs from the plant kingdom have received much attention in biomedical research because they target conserved host protein synthesis machinery and show specificity towards human and animal cell targets. Recent studies aimed at unravelling the enzymatic activities of the M charantia RIPs provide a structural basis for their activities. It has been reported that RIPs are member of the single chain ribosome inactivating protein (SCRIP) family which act irreversibly on ribosome by removing adenine residue from eukaryotic ribosomal RNA. Various activities of RIPs include anti-tumor, broad anti-viral, ribonuclease and deoxyribonuclease. MAP30 (Momordica Anti-HIV Protein), alpha- and beta-momorcharins inhibit HIV replication in acutely and chronically infected cells and thus are considered potential therapeutic agent in HIV infection and AIDS. Further, MAP30 improved the efficacy of anti-HIV therapy when used in combination with other anti-viral drugs. MAP30 holds therapeutic promise over other RIPs because not only it is active against infection and replication of both HSV and HIV but is non toxic to normal cells. Here we review the nature, action, structure function relationship and applications of RIPs from Momordica charantia and evaluate their potential for anti-cancer and anti-viral therapy.
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Hypoglycemic effects of the extracts of two Siamese plants, Momordica charantia (M.c.) and Phyllanthus urinaria (P.u.), were examined in streptozotocin-induced diabetic rats. Oral administration of a 50% methanol extract (30 mg/kg) of M.c. and P.u. decreased the blood glucose levels (BGL) by 25% and 24%, respectively, at 3 hr after administration. Among other fractions such as the ethyl ether or water soluble fractions, the 10 and 30 mg/kg n-butanol soluble fraction from M.c. extract was most effective in lowering BGL by 26% and 34%, respectively. Similarly with M.c., the n-butanol fraction from P.u. extract decreased BGL by 23% and 39% at the doses of 10 and 30 mg/kg, respectively. In the oral glucose tolerance test, n-butanol fractions from M.c. and P.u. (30 mg/kg, p.o.) both inhibited the initial increase in BGL to the same degree. In the intraperitoneal glucose tolerance test the n-butanol fraction of M.c. inhibited the increase of BGL prominently, but the n-butanol fraction of P.u. did not. These plants generally contain moderately non-polar hypoglycemic compound(s) soluble in n-butanol; and specifically, with regards to the hypoglycemic mechanism, the M.c. extract seems to act like insulin or via insulin secretion from the pancreas, like the action of sulfonyl ureas, and the P.u. extract may act via facilitation of glucose metabolism and/or the inhibition of glucose absorption in the gut like the action of biguanides.
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Anti-LDL glycative agents were investigated using aqueous extracts of Psidium guajava L. (PE), Toona sinensis Roem. (TE), Momordica charantia L. (ME) and Graptopetalum paragugayene E. Walther (GE). Concentrations of extracts 0.01-0.625 mg/mL, low density lipoprotein (LDL; 100 microg protein/mL) and inducers glucose (400 mM) and glyoxal (2.5 mM) were incubated at 37 degrees C. Evaluation parameters involved the thiobarbituric acid reactive substances (TBARS), conjugated dienes (CD), relative electrophoretic mobility (REM), 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging capability and total polyphenolic content. Results for anti-TBARS efficiency (in%) were PE (75.77), TE (75.10), ME (68.81) and GE (19.81) at 0.5 mg/mL, respectively, when induced by glucose; 36.68, 35.60, 32.62 and inactive, respectively, by glyoxal. The lag times for CD formation (in min) were: 289 and 125 by PE and TE, respectively, comparing to the control (45). REM was 1.6 with respect to PE (0.1 mg/mL) compared to the control (4.2). PE at 0.01 mg/mL effectively inhibited with 63.45% efficiency on AGEs induced by glucose. We conclude that PE virtually is a potent antiglycative agent, which can be of great value in the preventive glycation-associated cardiovascular and neurodegenerative diseases.
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The aim of the present study is to investigate the antioxidant activities of the aqueous extract of seeds of two varieties, namely a country and hybrid variety of Momordica charantia (MCSEt1 and MCSEt2) respectively in streptozotocin induced diabetic rats. Oral administration of both the seed extracts at a concentration of 150 mg/kg b.w for 30 days showed a significant decrease in fasting blood glucose, hepatic and renal thiobarbituric acid reactive substances and hydroperoxides. The treatment also resulted in a significant increase in reduced glutathione, superoxide dismutase, catalase, glutathione peroxidase and glutathione-s-transferase in the liver and kidney of diabetic rats. The results clearly suggest that seeds of Momordica charantia treated group may effectively normalize the impaired antioxidant status in streptozotocin induced-diabetes than the glibenclamide treated groups. The extract exerted rapid protective effects against lipid peroxidation by scavenging of free radicals there by reducing the risk of diabetic complications. The effect was more pronounced in MCSEt1 compared to MCSEt2.
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The effective concentration capable of killing 50% of parasites (IC(50)) was 46.06 µg/mL. The minimum inhibitory concentration (MIC) was ≤ 1024 µg/mL. Metronidazole showed a potentiation of its antifungal effect when combined with an extract of M. charantia.
The M. charantia L. showed strong antimicrobial potential, with bactericidal and fungicidal profile, there is the prospect to constitute a new therapeutic strategy for the control of infections, particularly in multiresistant strains.
Many species belonging to Cucurbitaceae family have long been regarded as food, medicinal plants, or both. Preliminary phytochemical screening of Citrullus colocynthis L., Cucumis sativus L. and Momordica charantia L. herbs showed the presence of phenolic compounds. Quantitative analysis of total phenolic compounds using Folin-Ciocalteu reagent revealed the presence of 50.87 mg GAE g(-1), 56.58 mg GAE g(-1) and 42.36 mg GAE g(-1) in C. colocynthis L., C. sativus L. and M. charantia L. herbs, respectively. HPLC analysis of phenolic content showed the presence of chlorogenic acid (16.3 mg per 100g dry sample and 27.7 mg per 100 g(-1) dry samples in C. colocynthis L. and C. sativus L., respectively) and gallic acid (26.7 mg per 100 g dry sample) as a major phenolic acids in M. charantia L. herb. The antioxidant activity of the herb of plants under investigation was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay and total antioxidant capacity was determined in terms of GAE. This study showed that C. sativus L. is the most active antioxidant, followed by C. colocynthis L., while M. charantia L. has the least antioxidant activity.
Momordica charantia (M. charantia) seed has been supposed to have an antifertility property but mechanisms underlying the infertility effect have not been investigated.
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The unfolding of alpha-momorcharin was systematically investigated using steady-state and time-resolved tryptophan fluorescence, circular dichroism and 8-anilino-1-naphthalenesulfonic acid (ANS) binding. These spectroscopic studies demonstrated that alpha-momorcharin unfolded through a compact folded intermediate state. The content of alpha-helix was increased, Trp192 approached closer to the side of active site and its rotational motion was restricted by being equilibrated with 2-3 M of guanidine hydrochloride. Furthermore, the binding of ANS with alpha-momorcharin was more suppressed to show that the hydrophobic parts would not be accessed to the protein surface but rather be sealed off in this specific conformation state. These results suggest that the structure of alpha-momorcharin holds the more compact conformation as an incipient state for unfolding, which is the sharp contrast to beta-momorcharin that gives the characteristics of the generally known molten globule state.
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The activities of hepatic and intestinal Phase-II enzyme levels increased along with mRNA levels except CYP3A mRNA level. PHF administration increases the activity of hepatic and intestinal UDP-glucuronyltransferase and glutathione S-transferase in response to dose and time; however, the activity of hepatic sulfotransferase increased at higher doses.
Momordica charantia (MC) or bitter gourd is widely known for its antidiabetic properties. The aim of the present study was to observe the protective effect of MC extract on the kidneys of streptozotocin-induced diabetic rats. Eighteen male Sprague-Dawley rats (n=18) weighing 200+/-50 g were taken for the study. The study comprised of three groups i.e. a non-diabetic, diabetic untreated and diabetic treated with MC extract, with each group comprising of six (n=6) rats. Diabetes was induced in the overnight fasted rats by intramuscular injection of streptozotocin (50 mg/kg body weight). The MC extract (50 mg/kg body weight) was administered via oral gavage. Both the kidneys were collected on the tenth day following treatment. Histological study using Verhoeff's van Gieson (VvG) and Periodic Acid-Schiff (PAS) stains were performed. The kidneys of the diabetic rats showed thickening of the basement membrane of the Bowman's capsule, edema and hypercellurarity of the proximal tubules, necrosis and hyaline deposits. These features were found to be reversed when the MC extract was administered to the experimental animals. The MC extract acted as an antioxidant thereby preventing the oxidative damage involved in the diabetic kidney. The administration of MC extract prevents oxidative damage in diabetic nephropathy.
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This explorative survey emphasizes the need to preserve and document the traditional healing practices for managing DSD inviting for more imminent scientific research on the plants to determine their efficacy as well as safety. With the help of statistical analysis (DCI), we propose 10 priority plants for DSD in present work. Systematic pharmacological study with these plants may contribute significant result.
These results suggest that from an acute standpoint, a freeze dried MC extraction in its present dose form does not affect plasma glucose/insulin levels, energy expenditure, substrate mixture and appetite scores following an oral glucose load in non-diabetic overweight men.
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The antidiabetic activities of bitter melon powders produced with lyophilization/superfine grinding and hot air drying/normal grinding were investigated in vivo for selecting a suitable bitter melon processing procedure. After a five-week treatment, bitter melon lyophilized superfine grinding powder (BLSP) had a higher antidiabetic activity with reducing fasting blood glucose levels from 21.40 to 12.54 mmol/L, the serum insulin levels from 40.93 to 30.74 mIU/L, and restoring activities of SOD compared with those in the bitter melon hot air drying powder (BAP) treated group. Furthermore, BLSP protected pancreatic tissues including islet beta cells and reduced the loss of islet cells. Combined with the difference of compositions in BLSP and BAP, it could be concluded that superfine grinding and lyophilization processes were beneficial for presenting the antidiabetic activity, which will provide a reference for direct utilization of bitter melon as a suitable functional food to relieve symptoms of diabetes.
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An anti-CD5 monoclonal antibody (mAb) was linked to the plant toxin momordin, a type-1 ribosome-inactivating protein purified from Momordica charantia. The in vitro cytotoxicity of the immunotoxin was evaluated as the inhibition of protein and/or DNA synthesis on isolated peripheral blood mononuclear cells (PBMC) and on human T cell leukemia Jurkat. The potency of the immunotoxin on PBMC was very high (IC50 = 1 - 10 pM) and was not affected by blood components. The conjugate was also very efficient in the inhibition of the proliferative response in a mixed lymphocyte reaction (IC50 = 10 pM). Moreover, the in vitro performance of the immunotoxin compared favorably with those reported for other anti-CD5-based immunoconjugates containing ricin A chain. The in vivo activity of the immunotoxin was assessed in the model of nu/nu mice bearing Jurkat leukemia. A significant inhibition of the tumour development (80%, P < 0.01) in the animals treated with immunotoxin was observed. Taken together, the in vitro and in vivo results suggest that the anti-CD5-momordin conjugate may be useful for graft-versus-host disease therapy and potentially in the treatment of CD5-positive leukemias and lymphomas.