Antidiabetic and renoprotective effect of Anogeissus acuminata leaf extract on experimentally induced diabetic nephropathy.

Background Diabetic nephropathy is the leading cause of end-stage renal disease. Hyperglycemia, oxidative stress, and inflammation are some of the mechanisms involved in renal damage. Anogeissus acuminata (AA) is used in India as an antidiabetic agent and has potent antioxidant activity. However, it has never been evaluated for its effect on diabetic nephropathy. Hence, in the present study we aimed to evaluate its effect on streptozotocin-induced diabetes mellitus and its renal complications. Methods Diabetes mellitus was induced by injecting streptozotocin, 50 mg/kg, i.p. in rats fasted for 6 h. Rats with hyperglycemia were treated with extracts of AA for 8 weeks at doses of 100 and 300 mg/kg, orally. Human NPH insulin (4 IU/kg, s.c.) was used as standard treatment. Plasma glucose levels (at weeks 1, 2, 4, and 8) and oxidative stress parameters (at weeks 2 and 4) were assessed. Effect on diabetic nephropathy was evaluated by recording the urinary volume, urinary protein excretion, kidney weights, serum creatinine, and blood urea nitrogen levels at week 8. Results Methanolic extract of AA leaves produced statistically significant (p<0.05) hypoglycemic and antioxidant effect. It also resulted in improved urinary function, reflected by better urinary volume and reduced protein excretion in urine. AA treatment could prevent the elevation of serum creatinine and blood urea nitrogen level in a dose-dependent manner. Kidney hypertrophy could be attenuated remarkably, as reflected by the significantly lower kidney weight (KW) per 100 g body weight (p<0.05). Conclusions AA leaf extract attenuated the development of diabetic nephropathy and also demonstrated antidiabetic and antioxidant action.

Antiosteoporotic effect of Hemidesmus indicus Linn. on ovariectomised rats.

PHARMACOLOGICAL RELEVANCE: Root of Hemidesmus indicus (L). R. Br., an herbal drug of India is traditionally used to prevent or treat female hormonal disturbance related disorders and assuaging symptoms of menopausal conditions. AIM OF THE STUDY: Lack of scientific data for potential use in bone loss, the present study was undertaken to investigate the effects of ethanol extract of Hemidesmus indicus root for osteoporosis in ovariectomised rats. MATERIALS AND METHODS: Thirty wistar female rats were randomly divided into five groups. One group was sham operated and other four groups were undergone dorsal ovariectomy (OVX). After four weeks of post-operative recovery, three OVX groups, viz. Group1, Group2 and Group3 were treated for ninety days with standard raloxifene (RLX) 1mg/kg/day, Hemidesmus indicus root extract (HIRE) 100mg/kg/day and HIRE 200mg/kg/day respectively. Sham and OVX control groups were fed with equal 1% vehicle volume. Serum and urine biochemistry (alkaline phosphatase, tartrate resistant acid phosphatase, triglyceride, total cholesterol, calcium, phosphorous and hydroxyproline), weight of body, uterus and vagina, femur parameters, three point bending of tibia and fourth lumbar vertebra compression were examined. Furthermore, bone architecture and uterine hypertrophy were examined by histopathological studies. RESULTS: Application of HIRE has increased bone strength and restored bone turnover markers such as alkaline phosphatase, tartrate resistant acid phosphatase and hydroxyproline moreover, improved femur parameters indicated mineralized bones, similar to the results observed with raloxifene treatment. Histopathology studies showed fibrocartilaginous proliferation of trabecular bone and absence of uterine hypertrophy. CONCLUSION: The results strongly suggest that HIRE prevents bone loss in OVX induced osteoporosis without estrogen like side effects. It might be a potential remedy like raloxifene for postmenopausal or estrogen deficiency caused osteoporosis.

Characterization of natural polymers from jackfruit pulp, calendula flowers and tara seeds as mucoadhesive and controlled release components in buccal tablets.

Identification and physiochemical parameters such as solubility, loss on drying, viscosity, pH, swelling index, starch and gum constituents were determined in natural polymers and showed satisfactory results. Spectral studies established the compatibility of natural polymers. The drug release kinetics in preliminary trial batches showed that tablets containing natural mucilages and gum showed a prolonged drug release comparable to Carbopol 974P and Methocel K4M. Also, all tablets showed a satisfactory drug permeability flux. Acute toxicity studies confirmed the safety of natural polymers. Using response surface method supported by 23 factorial design, the optimized buccoadhesive tablets (C1) with drug release at 8h (R8h, %) of 53.48±0.048% showed controlled release over ≥8h and followed the Korsmeyer-Peppas model with anomalous (non-Fickian) diffusion mechanism. Mucoadhesive strength was found to be 42.71±0.49g. Comparative dissolution study between prepared and marketed formulation showed that there was no significant difference in drug release profile having similarity factor 82.97. In vivo study for optimized formulation of the buccoadhesive tablets showed the better absolute bioavailability (71.26%) against the oral solution (51.22%). Histological study confirmed non-irritant nature and stability study indicated stability of the formulation.

Glucose transporters: physiological and pathological roles.

Glucose is a primary energy source for most cells and an important substrate for many biochemical reactions. As glucose is a need of each and every cell of the body, so are the glucose transporters. Consequently, all cells express these important proteins on their surface. In recent years developments in genetics have shed new light on the types and physiology of various glucose transporters, of which there are two main types-sodium-glucose linked transporters (SGLTs) and facilitated diffusion glucose transporters (GLUT)-which can be divided into many more subclasses. Transporters differ in terms of their substrate specificity, distribution and regulatory mechanisms. Glucose transporters have also received much attention as therapeutic targets for various diseases. In this review, we attempt to present a simplified view of this complex topic which may be of interest to researchers involved in biochemical and pharmacological research.

Evaluation of anti-diabetic activity of Glucova Active Tablet on Type I and Type II diabetic model in rats.

BACKGROUND: Glucova Active Tablet is a proprietary Ayurvedic formulation with ingredients reported for anti-hyperglycemic, anti-hyperlipidemic activity and antioxidant properties. OBJECTIVE: Evaluation of anti-diabetic activity of Glucova Active Tablet on Type I and Type II diabetic model in rats. MATERIALS AND METHODS: Experimental Type I diabetes was induced in 24 albino rats with intra-peritoneal injection of streptozotocin (50 mg/kg). Type II diabetes was induced in 18 albino rats by intra-peritoneal injection of streptozotocin (35 mg/kg) along with high fat diet. The rats were divided in 5 groups for Type I model and 4 groups for Type II model. Normal control group was kept common for both experimental models. Glucova Active Tablet (108 mg/kg) treatment was provided for 28 days twice daily orally. Fasting blood glucose level, serum lipid profile and liver anti-oxidant parameters like superoxide dismutase and reduced glutathione was carried out in both experimental models. Pancreas histopathology was also done. Statistical analysis were done by 'analysis of variance' test followed by post hoc Tukey's test, with significant level of P < 0.05. RESULTS AND DISCUSSION: Glucova Active Tablet showed significant effect on fasting blood glucose level. It also showed significant alteration in lipid profile and antioxidant parameters. Histopathology study revealed restoration of beta cells in pancreas in Glucova Active Tablet treated group. CONCLUSION: Finding of this study concludes that Glucova Active Tablet has shown promising anti-diabetic activity in Type I and Type II diabetic rats. It was also found showing good anti-hyperlipidemic activity and anti-oxidant property.

Isolation and characterization of jackfruit mucilage and its comparative evaluation as a mucoadhesive and controlled release component in buccal tablets.

BACKGROUND: The purpose of the present research work was to extract jackfruit mucilage, use it as a mucoadhesive agent, and to develop extended release buccoadhesive tablets with an intention to avoid hepatic first-pass metabolism, by enhancing residence time in the buccal cavity. MATERIALS AND METHODS: The mucilage was isolated from the jackfruit pulp by the aqueous extraction method and characterized for various physiochemical parameters as well as for its adhesive properties. Three batches of tablets were prepared (wet granulation method) and evaluated containing three mucoadhesive components: Methocel K4M, Carbopol 974P, and isolated jackfruit mucilage using chlorpheniramine maleate (CPM) as a model drug and changing the proportion of the mucoadhesive component (1:2:3), resulting in nine different formulations. RESULTS: The results of the study indicate that the isolated mucilage had good physicochemical and morphological characteristics, granules and tablets conformed to the Pharmacopoeial specifications, and in vitro release studies showed the sustained action of drug with increasing concentration of the isolated natural mucoadhesive agent in the formulations. Permeability studies indicated that changing the mucoadhesive component, permeability behavior was not statistically different (P > 0.05). FTIR and UV spectroscopy studies between mucilage and CPM suggested the absence of a chemical interaction between CPM and jackfruit mucilage. CONCLUSION: The developed mucoadhesive tablets for buccal administration containing natural mucilage (MF3) have a potential for the sustained action of drug release. Thus, mucoadhesive tablets for controlled release were successfully developed using natural jackfruit mucilage.