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Hyperglycemia is a pathological condition associated with prediabetes and diabetes. The incidence of prediabetes and diabetes is increasing and imposes great burden on healthcare worldwide. Patients with prediabetes and diabetes have significantly increased risk for cardiovascular diseases and other complications. Currently, management of hyperglycemia includes pharmacological interventions, physical exercise, and change of life style and diet. Food supplements have increasingly become attractive alternatives to prevent or treat hyperglycemia, especially for subjects with mild hyperglycemia. This review summarized current patents and patent applications with relevant literature on five commonly used food supplements with claims of hypoglycemic effects, including emblica officinalis (gooseberry), fenugreek, green tea, momordica charantia (bitter melon) and cinnamon. The data from human clinical studies did not support a recommendation for all five supplements to manage hyperglycemia. Fenugreek and composite supplements containing emblica officinalis showed the most consistency in lowering fasting blood sugar (FBS) or glycated hemoglobin (HbA1c) levels in diabetic patients. The hypoglycemic effects of cinnamon and momordica charantia were demonstrated in most of the trials with some exceptions. However, green tea exhibited limited benefits in reducing FBS or HbA1c levels and should not be recommended for managing hyperglycemia. Certain limitations are noticed in a considerable number of clinical studies including small sample size, poor experimental design and considerable variations in participant population, preparation format, daily dose, and treatment duration. Future studies with more defined participants, standardized preparation and dose, and improved trial design and size are warranted.
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The Indian traditional system of medicine prescribed traditional plant therapies. Two such plants, i.e. Momordica charantia (MC) and Mucuna pruriens (MP), earlier shown to reduce hyperglycaemia, were assessed for their anti hyperglycaemic effect on varying degrees of hyperglycaemia and diabetic complications. Alcohol and aqueous extracts of MC (50, 100 and 200 mg/kg/day) and only an alcohol extract of MP (100, 200 and 400 mg/kg/day) were evaluated in a pilot study (plasma glucose >180 mg/dL, 21 days), a chronic study in alloxanized rats (plasma glucose >280mg/dL, 120 days) and streptozotocin (STZ) mice (plasma glucose >400 mg/dL, 60 days). In the pilot study, the maximum antihyperglycaemic effect occurred with an aqueous extract of MC at week 3 and an alcohol extract of MP at week 6 at a dose of 200 mg/kg/day. In chronic alloxanized rats, the selected dose of MC led to a significant fall of 64.33%, 66.96%, 69.7% and 70.53% in plasma glucose levels at 1, 2, 3 and 4 months, respectively. MP showed a decrease of 40.71%, 45.63%, 50.33% and 51.01% at the same time period. In chronic STZ diabetic mice, MC led to a mean reduction of 15.37%, 18.68% and 22.86% in plasma glucose levels on days 40, 50 and 60 of sampling while MP had no significant effect. The alteration in hepatic and skeletal muscle glycogen content and hepatic glucokinase, hexokinase, glucose-6-phosphate and phosphofructokinase levels in diabetic mice were partially restored by MC but not by MP. The mechanism of action of MC and MP is discussed.
A new inhibitor of human immunodeficiency virus (HIV) has been isolated and purified to homogeneity from the seeds and fruits of the Momordica charantia. This compound, MAP 30 (Momordica Anti-HIV Protein), is a basic protein of about 30 kDa. It exhibits dose-dependent inhibition of cell-free HIV-1 infection and replication as measured by: (i) quantitative focal syncytium formation on CEM-ss monolayers; (ii) viral core protein p24 expression; and (iii) viral-associated reverse transcriptase (RT) activity in HIV-1 infected H9 cells. The doses required for 50% inhibition (ID50) in these assays were 0.83, 0.22 and 0.33 nM, respectively. No cytotoxic or cytostatic effects were found under the assay conditions. These data suggest that MAP 30 may be a useful therapeutic agent in the treatment of HIV-1 infections. The sequence of the N-terminal 44 amino acids of MAP 30 has been determined.
The healing of acetic acid induced gastric ulcer was increased by both doses of the extract. In pylorus-ligated rats, the extract showed significant decrease in ulcer index, total acidity, free acidity and pepsin content and an increase in gastric mucosal content. The extract also reduced the ulcer index in stress induced, ethanol induced and indomethacin induced gastric ulcers and cysteamine induced duodenal ulcer.
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β-Glucan purified from oats (OG) and bitter melon, Momordica charantia Linn (MC), water extracts have shown favorable effects on diabetes and its complications. We investigated to find out the optimal composition showing hypoglycemic and antidiabetic complication effects in variable compositions (OG:MC = 1:1, 1:2, 1:4, 1:6, 1:8, 1:10, 2:1, 4:1, 6:1, 8:1, 10:1). Extracts were administered orally once a day for 28 days following 7 days post streptozotocin (STZ) dosing. Five rats per group (total 15 groups; Intact, STZ, OG, MC, and the variable composition groups) were selected according to the blood glucose and body weight at 6 days after STZ dosing. After 28 days of extracts dosing, the changes on the body weight, liver and kidney weight, blood glucose, blood urea nitrogen (BUN), creatinine, aspartate aminotransferase (AST) and alanine aminotransferase (ALT), low-density lipoprotein (LDL), and total-cholesterol levels were observed. As the result of STZ-induced diabetes, decreases of body weight, increases of the liver and kidney weights, blood glucose, BUN, creatinine, AST, ALT, LDL, and total-cholesterol levels in STZ control were detected compared with intact control. However, these changes of hyperglycemia, diabetic nephropathy, hepatopathy, and hyperlipemia were dramatically decreased in the OG and MC single-dosing group, and all composition groups. In addition, there were more favorable effects in all composition groups compared with the OG and MC single-dosing groups. Among variable compositions, the OG:MC 1:2 mixed group showed the most synergic effects in this study.
Twenty adult male Sprague-Dawley rats, weighing 176 +/- 70 g, were used for this study. The animals, divided randomly into 4 groups (A-D) received daily graded oral doses of 15, 25 and 50 mg/100 g body weight of methanolic seed extract of MC, respectively, while Group D rats had distilled water for 56 days. The weights of the animals in each group were recorded weekly throughout the duration of the experiment. Serum cholesterol levels were assayed from blood obtained from a left ventricular puncture.
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This study sought to investigate the effects of Purendan superfine powder comprised of Momordica charantia, Radix Ginseng, and Radix Salviae Miltiorrhiae on neuronal apoptosis and expression of bcl-2, bax, and caspase-3, which are retinal apoptosis-associated factors in rats with diabetes mellitus induced by continuous intraperitoneal injection of streptozotocin. The results showed that Purendan superfine powder could upregulate the expression of bcl-2 protein and mRNA, and downregulate the expression of bax and caspase-3 in the retina of diabetes mellitus rats. In addition, Purendan superfine powder was shown to reduce the number of apoptotic neurons. Our experimental findings indicate that Purendan superfine powder can inhibit neuronal apoptosis in the retina of diabetes mellitus rats and has protective effects on diabetic retinopathy.
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Forty-six different species collected in the Mosetene ethnia, dwelling in the Andean Piedmont of Bolivia, were screened for antimalarial properties. Thirty-three extracts were screened for antimalarial activity in vitro on Plasmodium falciparum chloroquine resistant strain (Indo), and forty-seven extracts were evaluated in vivo on the rodent malaria P. vinckei petteri 279BY. Only two plants are specifically used in combination by the Mosetene against malaria attack (Hymenachne donacifolia and Tesseria integrifolia), but they did not display any activity in vivo at 1000 mg/kg. The in vivo most active extracts were Swietenia macrophylla bark, Trema micrantha bark and Triplaris americana bark, not all of them were used for antimalarial purposes by the Mosetene. The following extracts were moderately active: Jacaratia digitata inner bark and Momordica charantia aerial part (both traditionally used as febrifuge), Kalanchoe pinnate aerial part (used in inflammatory processes), Lunania parviflora twigs and leaves, Phyllanthus acuminatus (used as piscicide), Tynanthus schumannianus fruit (used against diarrhoea), Triumfetta semitrilobata (used as febrifuge, to alleviate kidney and gynecological pain) and finally Solanum mammosum fruit (used against scabies). We present here the results of this screening, emphazing on the in vivo antimalarial activity of the selected plants. The antimalarial in vivo activity of the selected species, in relation with their traditional Mosetene use is then discussed.
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The fruit fly, Bactrocera tau (Walker) (Diptera: Tephritidae), is an important pest of fruit and vegetable crops. In this study, host preference of B. tau females and the effects of host species and larval density on larval survival, pupal weight, adult emergence, and developmental duration were investigated on cucumber (Cucumis sativus L.), sponge gourd (Luffa cylindrical L. (Roem)), bitter gourd [Momordica charantia (Cucurbitaceae) L.], guava [Psidium guajava (Myrtaceae) L.], and tangerine [Citrus reticulata (Rutaceae) (Blanco)]. The results showed that females preferred to cucumber over other host species. Larval feeding experience affected subsequent host oviposition preference of adult females. Host species and initial larval density affected certain aspects of the biology of B. tau. Larval density negatively affected insect performance. Survival rates at low densities were significantly higher than that at high densities. Total developmental duration reduced at high larval densities. Cucumber was more suitable to larval growth. Larvae on cucumber grew faster and the puparia were heavier than that on other host species. Larval survival, pupation rate and adult emergence were higher on cucumber compared with those in other host species. Oviposition preference of adult females was correlated with performance of their offspring.
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the hypoglycemic effect of the ethanolic extract of Momordica charantia (cucurbitaceae) was investigated in both normal and streptozotocin - induced diabetic mice. The ethanolic extract of Unriped fruits of M. charantia (800mg/kg) reduced the blood glucose of normal mice from 172 ±3 to 136 ± 5 mg/100ml 4 hours after intrapertitoneal administration (P<0.001), and also significantly lowered the blood glucose of streptoxotocin induced diabetic mice from 686± 60 to 407± 35 mg/100ml under similar conditions (p<0.01). The possible mechanism of hypoglycemic action of M.Charantia is due to the increased glucose uptake in liver cells because it markedly lowers the blood glucose levels in streptozotocin induced diabetic mice.
First, rats were divided randomly into two groups: the control group was fed with control diet, whereas the experimental group was fed with a 60% high-fructose diet for 8 weeks. After the first 6 weeks, the fructose-treated rats were further subdivided into six groups and were orally fed with or without Momordica charantia L. or rosiglitazone (ROS) for 2 weeks while rats were still on fructose diet.
Chromium reduced glycosylated hemoglobin (HbA(1c)) and fasting blood glucose (FBG) levels in a large meta-analysis. Gymnema sylvestre reduced HbA(1c) levels in 2 small open-label trials. Cinnamon improved FBG but its effects on HbA(1c) are unknown. Bitter melon had no effect in 2 small trials. Fibre had no consistent effect on HbA(1c) or FBG in 12 small trials. Green tea reduced FBG levels in 1 of 3 small trials. Fenugreek reduced FBG in 1 of 3 small trials. Vanadium reduced FBG in small, uncontrolled trials. There were no trials evaluating microvascular or macrovascular complications or other clinical end points.
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Bitter melon (Momordica charantia L.) is rich in a variety of biologically active ingredients, and has been widely used in traditional Chinese medicine (TCM) to treat various diseases, including type 2 diabetes and obesity.
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Twenty-one species of anti-diabetic plants were recorded, Momordica charantia (score: 0.71), Azadirachta indica (score: 0.64), Trigonella foenum-graecum (score: 0.63), Capparis decidua (score: 0.60), Withania coagulans (score: 0.54), Gymnema sylvestre (score: 0.52) and Syzygium cumini (score: 0.51) were the most significant anti-diabetic plants of the area of study, having DCI more than 0.5.
During diabetes, structural and functional changes in the alimentary tract are known to take place resulting in increased absorption of intestinal glucose and alterations in the activities of brush border disaccharidases. Similar observations are also reported in the renal cortex. In the present investigation, we examined the effect of feeding bitter gourd fruit devoid of seeds on activities of intestinal and renal disaccharidases, viz., maltase, sucrase, and lactase in streptozotocin-induced diabetic rats. Normal and diabetic rats were fed either with basal diet or a diet containing 10% bitter gourd powder. Specific activities of intestinal disaccharidases were significantly increased during diabetes, and supplementing bitter gourd in the diet clearly indicated amelioration in the activities of maltase and lactase during diabetes. However, a significant change was not observed with sucrase activity by feeding of bitter gourd. During diabetes, renal disaccharidase activities were significantly lower than those in the control rats. Bitter gourd supplementation was beneficial in alleviating the reduction in maltase activity during diabetes. However, not much change in the activities of sucrase and lactase was observed upon feeding. This positive influence of feeding bitter gourd on intestinal and renal disaccharidases clearly indicates their beneficial role in the management of diabetes, thus making diabetic animals more tolerant to hyperglycemia.
We report that PHF pretreatment downregulated the expression of intestinal Pgp and this downregulated intestinal Pgp would result in decreased functional activity. In addition, this downregulated Pgp expression might affect the bioavailability of antidiabetic Pgp substrate drugs.
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Natural products isolated from plants used in traditional medicine, which have potent anti-plasmodial action in vitro, represent potential sources of new anti-malarial drugs.
The weightof transdermal patches of M. charantia (2 cm(2); 10 mg/patch) and was found to be 0.03 gm.Thickness of patches of M. charantia (2 cm(2); 10 mg/patch) was found to be satisfactory. The percentage release of active constituents from transdermal patches of M.charantia (2 cm(2); 10 mg/patch) was found to be 47.59% in 10% hydroalcoholic phosphate buffer pH 7.4 at the end of 6 h.The transdermal route exhibited negligible skin irritation and in vivo results revealed that the patches successfully decrease the blood glucose level.
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The study was conducted to analyze the effect of plant growth regulators on callogenesis and direct and indirect organogenesis of Memordica charantia. Callus cultures were induced from leaf, stem and cotyledonary explants of Momordica charantia, at different auxin and cytokinin concentrations either in single or in combination in MS medium. The best callogenic response was observed from all three explants (leaf, stem and cotyledon) on MS medium supplemented with 1.0 and 1.5 mg L(-1) BAP with 1.5 mg L(-1) NAA and 1.0 mg L(-1) 2,4-D, respectively. The callus produced was hard, green and compact. These totipotent cells were failed to give rise shooting response when transferred to same or different growth regulator containing medium as second subculture. Indirect organogenesis response was very low or absent due to hardening of callus and habitutation. Best shooting was observed at 1.0 mg L(-1) BAP + 0.1 TDZ and 1.5 mg L(-1) BAP + 0.2 mg L(-1) NAA from shoot tip and cotyledonary node explants. While root formation was achieved when generated shoots were transferred to MS medium both full and half strength supplemented with different auxin concentrations.
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Plants are an invaluable source of potential new anti-cancer drugs. Momordica charantia is one of these plants with both edible and medical value and reported to exhibit anticancer activity. To explore the potential effectiveness of Momordica charantia, methanol extract of Momordica charantia (MCME) 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, in this study. MCME showed cytotoxic activity towards all cancer cells tested, with the approximate IC(50) ranging from 0.25 to 0.35 mg/mL at 24 h. MCME 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. MCME 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 MCME-induced cell death. These findings indicate that MCME has cytotoxic effects on human cancer cells and exhibits promising anti-cancer activity by triggering apoptosis through the regulation of caspases and mitochondria.
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The in vivo effect of the administration of extracts of Momordica charantia on certain biochemical parameters of Sprague-Dawley rats was investigated. It was observed that there was an increase in muscle and liver protein levels, while there was a reduction in the levels of brain protein, muscle and liver glycogen. The activities of plasma L-alanine transaminase and alkaline phosphatase were reduced. The L-aspartate transaminase and adenosine triphosphatase activities were slightly elevated in whole plant extract treated rats while the L-aspartate transaminase was unaffected by the ethanol extract but reduced the adenosine triphosphatase activity.
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Peroxisome proliferator-activated receptor alpha (PPARalpha) is a ligand-dependent transcription factor that regulates the expression of genes involved in lipid metabolism and transport. Ligands/activators of PPARalpha, like fibrate-type drugs, may have hypolipidemic effects. To identify food that contains activators of PPARalpha, a transactivation assay employing a clone of CHO-K1 cells stably transfected with a (UAS)(4)-tk-alkaline phosphatase reporter and a chimeric receptor of Gal4-rPPARalpha LBD was used to screen ethyl acetate (EA) extracts of a large variety of food materials. It was found that the EA extract of bitter gourd (Momordica charantia), a common oriental vegetable, activated PPARalpha to an extent that was equivalent to or even higher than 10 microM Wy-14643, a known ligand of PPARalpha. This extract also activated PPARgamma to a significant extent which was comparable to 0.5 microM BRL-49653. The activity toward PPARalpha was mainly in the soluble fraction of the organic solvent. The EA extract prepared from the whole fruit showed significantly higher activity than that from seeds or flesh alone. The bitter gourd EA extract was then incorporated into the medium for treatment of a peroxisome proliferator-responsive murine hepatoma cell line, H4IIEC3, for 72 h. Treated cells showed significantly higher activity of acyl CoA oxidase and higher expressions of mRNA of this enzyme and fatty acid-binding protein, indicating that the bitter gourd EA extract was able to act on a natural PPARalpha signaling pathway in this cell line. It is thus worth further investigating the PPAR-associated health benefits of bitter gourd.
Liriomyza sativae Blanchard (Diptera: Agromyzidae) is one of the important pests harming a wide variety of vegetables and ornamental plants throughout the world. The leaf ethanol extract of Momordica charantia at the concentration of 2000-4000 microg x ml(-1) displayed significant antifeedant and antioviposition activities against L. sativae adults. For further purifying the extract, four solvents, i. e., cyclohexane, ethyl acetate, n-butanol and water, were used to extract the ethanol extract, and the antifeedant and antioviposition activities of the extracts against L. sativae adults were tested. The results showed that after treated with the extracts at the concentration of 1000 microg x ml(-1) for 2 days, the antifeedant index (AFI) of cyclohexane-, ethyl acetate-, n-butanol- and water extracts against L. sativae adults was 11.08%, 34.89%, 22.99% and 0, and the antioviposition index (AOI) was 0, 30.91%, 6.45% and 0, respectively. Ethyl acetate extract had the highest bioactivity. At the concentration of 4000 microg x ml(-1), the AFI and AOI of ethyl acetate extract were 70.95% and 69.49%, respectively. The ethyl acetate extract was then isolated by silica gel column chromatography, and three compounds, i.e., (19S, 23E)-5beta,19-epoxy-19-methoxy-cucurbita-6,23-dien-3beta and 25-diol (compound 1), (19R, 23E)-5beta,19-epoxy-19-methoxy-cucurbita-6,23-dien-3beta and 25-diol (compound 2), and 3beta, 7beta,25-trihydroxycucurbita-5,23-dien-19-al-3-O-beta-D-glucopyranoside (compound 3), were obtained. These three compounds at concentration of 100-400 microg x ml(-1) all had inhibitory effects on the feeding and oviposition of L. sativae. At the concentration of 400 microg x ml(-1), the AFI and AOI were 66.89% , 53.53% and 78.02% , and 76.32%, 58.36% and 78.36% for compound 1, 2 and 3, respectively.
It has been reported that the water extract of the whole unripe fruit of Momordica charantia can significantly reduce blood glucose levels. However the safety of its use during pregnancy has not been fully investigated. The aim of this investigation is to determine the safety of this extract during pregnancy. The water extract of the unripe fruit was given to pregnant Sprague Dawley rats on days 7, 8, 9, 10, 11, 12, 13 and 14 of gestation. The litter size was determined for each group and the litters were examined for gross malformations. The gross and histological examinations of various organs of the litters were also carried out. Results show that 8.65% of the litters from experimental animals were malformed as against 1.62% of control. It also showed that 31.2% of all the malformed litters had multiple congenital malformations. It also showed that the experimental rats had nine resorption sites while control had none. This demonstrates that the water extract of Momordica charantia is teratogenic in Sprague Dawley rats and should be used with caution in man.
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Native and exotic Brazilian plants collected in the State of Minas Gerais were evaluated for their anticancer potential. Methanol extracts from leaves of 51 plant species were tested for cytotoxicity against four tumor cell lines: B16 (murine skin), HL-60 (human leukemia), MCF-7 (human breast), and HCT-8 (human colon). Plant extracts that exhibited IC(50) values less than 30 microg/ml against any tumor cell line were tested on sea urchin egg development and mouse erythrocytes. In addition, all extracts were evaluated for their general toxicity using the brine shrimp lethality assay. The most active extracts against the tumor cells were those obtained from Lantana fucata, Copaifera langsdorffii, and Momordica charantia. These three extracts inhibited sea urchin development from the first cleavage, but those from C. langsdorffii and M. charantia were very active against mouse erythrocytes. Only the L. fucata extract presented no hemolytic activity. Consequently, although the extracts of L. fucata, M. charantia, and C. langsdorffii could be useful in the development of new anticancer products, the first of these extracts is the most promising since it did not present unspecific toxicity, as suggested by negative results obtained with brine shrimp lethality and mouse erythrocytes assays.