Cucurbitane-Type Triterpenoids from the Blood Glucose-Lowering Extracts of Coccinia indica and Momordica balsamina Fruits.

CONTEXT: Few vegetables that are commonly consumed in India as part of diet have been claimed for their antidiabetic potential. OBJECTIVE: The present study was aimed at evaluating preventive effects of cucurbit vegetables namely, Coccinia indica and Momordica balsamina belonging to family Cucurbitaceae in diabetic hyperglycemia. MATERIALS AND METHODS: The fruits of M. balsamina and C. indica were extracted with chloroform and fractionated with hexane to prepare an extract rich in moderately polar components. These extracts were used for evaluating the effect of these cucurbits in nicotinamide/streptozotocin-induced type 2 diabetes. Streptozotocin-nicotinamide-induced diabetic animals were orally treated with chloroform extract of fruits (250 mg/kg BW) given daily for a week separately. RESULTS: Both the extracts reduced fasting blood glucose significantly (P < 0.05 versus diabetic control) when estimated on seventh day of treatments. Pretreatment with fruit extracts for 7 days also blunted the OGTT (oral glucose tolerance test) curve. Results indicated that C. indica and M. balsamina fruits possess beneficial effects in diabetes by lowering elevated blood glucose level. Six cucurbitane-type triterpenoids were isolated from bioactive extracts of C. indica ((1-3) and M. balsamina (4-6). The structures of these compounds were elucidated on the basis of spectroscopic data analysis. CONCLUSION: The study concludes that the inclusion of C. indica and M. balsamina fruits in food can be useful for newly diagnosed diabetic patients or highrisk group of population for glycemic control. SUMMARY: "Cucurbitane-type triterpenoids from the blood glucose-lowering extracts of Coccinia indica and M. balsamina fruit" The beneficial effects of chloroform extracts of vegetal cucurbits namely C. indica (Ivy gourd) and M. balsamina (Balsam apple) in streptozotocin-nicotinamide (STZ-NA)-induced diabetic rats has been evaluated.The isolation and characterization of six cucurbitacins from bioactive extracts of C. indica (Coccinoside A, B, and C) and M. balsamina (cucurbit-5, 7-dien-3ß-ol, cucurbita-5-en-3ß-ol-3-O-ß-d-glucopyranoside, and cucurbit-5-en-3ß-ol-3-O-ß-d-glucopyranosyl-(4'→1")-O-ß-d-glucopyranoside) have been reported for the first time.The study concludes that the inclusion of C. indica and M. balsamina fruits in food can be useful for newly diagnosed diabetic patients or high risk group of population for glycemic control. Abbreviation used: C: indica (Coccinia indica), M: balsamina (Momordica balsamina), Kbr: Potassium bromide, FTIR: Fourier transform infrared spectroscopy, COSY: Corelated Spectroscopy, DEPT: Distortionless Enhancement by Polarization Transfer, DMSO: Dimethyl sulfoxide, TMS: tetramethylsilane, ESI-MS: Electrospray Ionization mass spectrometry, TLC: thin layer chromatography, STZ-NA: Streptozotocin-nicotinamide, CMC: carboxy methyl cellulose, BW: body weight, ANOVA: analysis of variance, AUC: area under curve.

Cucurbitacins - An insight into medicinal leads from nature.

Cucurbitacins which are structurally diverse triterpenes found in the members of Cucurbitaceae and several other plant families possess immense pharmacological potential. This diverse group of compounds may prove to be important lead molecules for future research. Research focused on these unattended medicinal leads from the nature can prove to be of immense significance in generating scientifically validated data with regard to their efficacy and possible role in various diseases. This review is aimed to provide an insight into the chemical nature and medicinal potential of these compounds exploring their proposed mode of action, probable molecular targets and to have an outlook on future directions of their use as medicinal agents.

Perceptive solutions to anti-filarial chemotherapy of lymphatic filariasis from the plethora of nanomedical sciences.

INTRODUCTION: Growing interest in the application of nanotechnology to treat lymphatic filariasis (LF) implies that the imminent medical arsenal of this interesting technology is attractive for health authorities. Currently, they are completely dependent on friendly oral mass drug (anti-filarials) administration to eliminate this morbid disease and are now looking for new alternatives to bring about further improvements. AREAS COVERED: A plethora of issues affecting the oral bioavailability of the mainstay human lymphatic filarial drugs, leading to meager pharmacokinetics and pharmacodynamics issues in anti-filarial chemotherapy are identified. Various important nanomedical drug delivery systems are highlighted and their solutions provided. A conceptual resolution to strictly arrest the transmission of LF in endemic areas is also presented. FUTURE PERSPECTIVES: Unless the solutions for pharmacokinetic tribulations and the measurement of factual pharmacodynamic endpoints for the existing anti-filarial drugs are evaluated using relevant approaches, health authorities will not be able to devise optimal treatment regimens for affected patients. Contemporary therapeutic paradigms need to be shifted toward the upcoming schemes of nanopharmaceutical sciences, which have enormous potential to advance the community-directed management of this tropical disease by improving the pharmacokinetic and pharmacodynamic properties of the filaricidal agents.

Formulation and evaluation of floating tablets of liquorice extract.

BACKGROUND: Floating tablets prolong the gastric residence time of drugs, improve bioavailability, and facilitate local drug delivery to the stomach. With this objective, floating tablets containing aqueous extract of liquorice as drug was prepared for the treatment of Helicobacter pylori and gastric ulcers. METHODS: The aqueous extract of liquorice was standardized by HPTLC. Tablets containing HPMC K100M (hydrophilic polymer), liquorice extract, sodium bicarbonate (gas generating agent), talc, and magnesium stearate were prepared using direct compression method. The formulations were evaluated for physical parameters like diameter, thickness, hardness, friability, uniformity of weight, drug content, buoyancy time, dissolution, and drug release mechanism. The formulations were optimized on the basis of buoyancy time and in vitro drug release. RESULTS: The diameter of all formulations was in the range 11.166-11.933 mm; thickness was in the range 4.02-4.086 mm. The hardness ranged from 3.1 to 3.5 kg/cm(2). All formulations passed the USP requirements for friability and uniformity of weight. The buoyancy time of all tablet formulations was less than 5 min and tablet remained in floating condition throughout the study. All the tablet formulations followed zero-order kinetics and Korsemeyer-Peppas model in drug release. CONCLUSION: The optimized formulation was found to be F6 which released 98.3% of drug in 8 h in vitro, while the buoyancy time was 3.5 min. Formulations containing psyllium husk, sodium bicarbonate and HPMC K100M in combination can be a promising for gastroretentive drug delivery systems.