Pharmacological evaluation of hyperin for antihyperglycemic activity and effect on lipid profile in diabetic rats.

Antihyperglycemic potential of hyperin at 25 and 50 mg/kg doses for 30 days to streptozotocin induced diabetic rats has been reported. In oral glucose tolerance test, hyperin treated rats showed a significant reduction in blood glucose level after 120 min. It was found that hyperin exhibited dose dependent and significant antihyperglycemic activity in streptozotocin induced diabetic rats which were nearly similar with standard drug glybenclamide. Activities of glucose-6-phosphatase, fructose-1,6-bisphosphatase, glycogen phosphorylase, glycosylated haemoglobin and level of serum urea and creatinine were significantly decreased in hyperin supplemented diabetic rats, dose dependently. Activities of hexokinase and glycogen synthase were increased with augmentation in liver glycogen, insulin and haemoglobin content in hyperin treated diabetic rats. General hematological parameters did not show any significant change in hyperin treated diabetic rats hence it is safe at these doses. Histopathological studies showed significant morphological changes in pancreatic beta-cells of streptozotocin induced diabetic rats. A decreased number of secretory granules of beta-cells were observed in diabetic rats and these pathological abnormalities were normalized after treatment with hyperin and standard drug glybenclamide. Further, hyperin decreases significant in serum total cholesterol, triglyceride, low density lipoprotein, very low density lipoprotein levels coupled with elevation of high density lipoprotein in diabetic rats. These results suggest that hyperin has a pivotal role in blood glucose level in streptozotocin induced hyperglycemia by improving the function of pancreatic islets and increasing glycolysis and decreasing gluconeogenesis.

Wound healing potential of flowers extracts of Woodfordia fruticosa Kurz.

Wound healing or repair is the body's natural process of regenerating dermal and epidermal tissue. Woodfordia fruticosa Kurz (Family: Lythraceae) is used traditionally in wound healing by the tribals of Chhattisgarh district. However, there is a paucity of scientific data in support. In this study, we evaluated antimicrobial activity of petroleum ether, chloroform, ethanolic and aqueous extracts against a diverse range of gram +ve and gram -ve bacteria along with pathogenic fungi. The wound healing activity of ethanolic extract was also evaluated at dose levels of 250 and 500 mg/kg body wt in rats by excision, incision and dead space wound healing models along with histopathology of wound area of skin. The ethanolic extract showed potent wound healing activity, as evident from the increase in the wound contraction and breaking strength in dose-dependent manner. Treatment with ethanolic extract (250 and 500 mg/kg body wt) showed significant dose-dependently decrease in epithelization period and scar area. Hydroxyproline, hexuronic acid and hexosamine contents, the important constituents of extracellular matrix of healing were also correlated with the observed healing pattern. During early wound healing phase, pro-inflammatory cytokines TNF-alpha, IL-6 and anti-inflammatory cytokine IL-10 levels were found to be upregulated by the ethanolic extract treatment. The ethanolic extract exhibited a strong and broad spectrum antimicrobial activity, as compared to other extracts. It showed very low Minimum inhibitory concentration (MIC) values and inhibited the growth of E. coli, Staphylococcus aureus and Candida albicans in concentration of 2.5 microg/disc. Thus, the results of the present study demonstrated the strong wound healing potential and antimicrobial activities of W. fruticosa, flowers, supporting the folklore use of the plant by the tribal people of Chhattisgarh district.

Antihyperglycemic activity of Woodfordia fruticosa (Kurz) flowers extracts in glucose metabolism and lipid peroxidation in streptozotocin-induced diabetic rats.

The ethanolic extract of W. fruticosa flowers (250 and 500 mg/kg) significantly reduced fasting blood glucose level and increased insulin level after 21 days treatment in streptozotocin diabetic rats. The extract also increased catalase, superoxide dismutase, glutathione reductase, glutathione peroxidase activities significantly and reduced lipid peroxidation. Glycolytic enzymes showed a significant increase in their levels while a significant decrease was observed in the levels of the gluconeogenic enzymes in ethanolic extract treated diabetic rats. The extract has a favourable effect on the histopathological changes of the pancreatic beta-cells in streptozotocin induced diabetic rats. The results suggest that W. fruticosa possess potential antihyperglycemic effect by regulating glucose homeostasis and antioxidant efficacy in streptozotocin-induced diabetic rats.

Protective effect of Amaranthus spinosus against D-galactosamine/lipopolysaccharide-induced hepatic failure.

The current study is an effort to identify the hepatoprotective activity of the 50% ethanol extract of the whole plant of Amaranthus spinosus Linn. (Amaranthaceae) against d-galactosamine/lipopolysaccharide (d-GalN/LPS)-induced liver injury in rats. d-GalN/LPS (300 mg/kg body weight/30 µg/kg body weight)-induced hepatic damage was manifested by a significant (p <0.05) increase in the activities of marker enzymes (aspartate transaminase, alanine transaminase, alkaline phosphatase, lactate dehydrogenase and gamma glutamyl transferase) and bilirubin level in serum while phospholipids significantly decreased. All other parameters, i.e. cholesterol, triglycerides and free fatty acids were increased significantly in both serum and liver compared to the control group. Pretreatment of rats with A. spinosus extract (400 mg/kg) significantly (p <0.05) reversed these altered parameters to normal compared to the intoxicated group. The biochemical observations were supplemented by histopathological examination of liver sections. There were no significant changes in the activities of marker enzymes, bilirubin level and lipids in the rats treated with A. spinosus extract alone. Results of this study revealed that A. spinosus extract could afford a significant protection against d-GalN/LPS-induced hepatocellular injury.

Hepatoprotective activity of Amaranthus spinosus in experimental animals.

The hepatoprotective and antioxidant activity of 50% ethanolic extract of whole plant of Amaranthus spinosus (ASE) was evaluated against carbon tetrachloride (CCl4) induced hepatic damage in rats. The ASE at dose of 100, 200 and 400 mg/kg were administered orally once daily for fourteen days. The substantially elevated serum enzymatic levels of serum glutamate oxaloacetate transaminase (AST), serum glutamate pyruvate transaminase (ALT), serum alkaline phosphatase (SALP) and total bilirubin were restored towards normalization significantly by the ASE in a dose dependent manner. Higher dose exhibited significant hepatoprotective activity against carbon tetrachloride induced hepatotoxicity in rats. The biochemical observations were supplemented with histopathological examination of rat liver sections. Meanwhile, in vivo antioxidant activities as malondialdehyde (MDA), hydroperoxides, reduced glutathione (GSH), superoxide dismutase (SOD) and catalase (CAT) were also screened which were also found significantly positive in a dose dependent manner. The results of this study strongly indicate that whole plants of A. spinosus have potent hepatoprotective activity against carbon tetrachloride induced hepatic damage in experimental animals. This study suggests that possible mechanism of this activity may be due to the presence of flavonoids and phenolics compound in the ASE which may be responsible to hepatoprotective activity.

Toxicological screening of traditional medicine Laghupatha (Cissampelos pareira) in experimental animals.

Laghupatha (Cissampelos pareira) a important medicinal plant in Indian traditional system of medicine and is widely used in many countries by different tribal. Despite the wide use of Cissampelos pareira in folk medicine, no study has been published in the scientific literature about its toxicological profile. In present study 50% aqueous ethanolic extract of Cissampelos pareira (Menispermaceae) was evaluated for the acute and subacute toxicity. In the acute toxicity test, oral administration of 2g/kg of Cissampelos pareira produced neither mortality nor changes in behavior or any other physiological activities in mice. In subacute toxicity studies, no mortality was observed when the two doses of 1 or 2g/kg day of 50% aqueous ethanolic extract of Cissampelos pareira were administered p.o. for a period of 28 days in rats. There were no significant changes occurred in the blood chemistry analysis including glucose, sodium, potassium, calcium, phosphorus, chloride, total cholesterol, high density lipoprotein, triglycerides, total protein, blood urea nitrogen, creatinine, conjugated billirrubin, aspartate transaminase, alanine transaminase, total billirrubin, albumin, prothrombin time and thromboplastin partial time in both sexes of animals. Hematological analysis showed no marked differences in any of the parameters examined (WBC count, platelet and hemoglobin estimation) in either the control or treated group of both sexes. The urinalysis was negative for glucose, ketonic bodies, casts, red blood cells, and albumin in the control and treatment groups. There were no significant differences in the body and organ weights between controls and treated animals of both sexes. Pathologically, neither gross abnormalities nor histopathological changes were observed. Cissampelos pareira was found safe in acute and subacute toxicities while chronic toxicity studies are further required for the support of the safe and sound use of this traditional plant.

Antinociceptive and antiarthritic activity of Cissampelos pareira roots.

In the present study, 50% aqueous ethanolic extract of Cissampelos pareira (Menispermaceae) roots (C. pareira) at the dose levels of 100-400 mg/kg, once daily for 3 days exhibited significant (P < 0.001) resistance against mechanical pain after 30 min in analgesymeter induced pain in mice. In acetic acid (0.6%; i.p.) inducing writhing, Cissampelos pareira significantly (P < 0.05) decreased the writhing episodes; the degree of percent protection at 200 and 400 mg/kg was 22.73 and 51.63. The hot plate reaction time was increased by 2.07 (P < 0.05) and 2.70 (P < 0.001) folds. respectively. Further Cissampelos pareira showed the dose dependent significant protective effect against complete Freund's adjuvant induced arthritis. The percentage protection on the 18th day was 40.54 (P < 0.01) and 71.52 (P < 0.001) at 200 and 400 mg/kg respectively. Lysosomal enzymes (acid phosphatase and N-acetyl glucosaminidase) were decreased by 50% (P < 0.01) and 26.26% (P < 0.05) by using Cissampelos pareira, dextramethasone decreased them 56.56% (P < 0.01) and 31.82% (P < 0.01) and the glycoprotein contents (total hexose and sialic acid) were increased by 1.55-folds (P < 0.01) and 1.51-folds (P < 0.05) by using Cissampelos pareira while dextramethasone increases them by 1.51-folds (P < 0.001) and 1.60-folds (P < 0.01) respectively in stomach homogenate with respect to arthritic group. The increased pain threshold and protective effect against CFE by Cissampelos pareira vindicated its medicinal value in treatment of pain and arthritis.

Evaluation of anti-inflammatory activity of Cissampelos pareira root in rats.

In the present study, 50% ethanolic extract of Cissampelos pareira roots (CPE) in acute, subacute and chronic models of inflammation was assessed in rats. Per os (p.o.) administration of CPE (200, 400 mg/kg) exhibited significant anti-inflammatory activity. In acute inflammation as produced by carrageenin 59.55% and 64.04%, by histamine 15.38% and 30.77%, by 5-hydroxytryptamine 17.78% and 31.11% and by prostaglandin E(2)-induced hind paw edema 19.23% and 30.77% protection was observed. While in subacute anti-inflammatory models using formaldehyde-induced hind paw edema (after 1.5 h) 38.36% and 47.95% and in chronic anti-inflammatory model using cotton pellet granuloma 15.02% and 19.19% protection from inflammation was observed. CPE did not show any sign of toxicity and mortality up to a dose level of 1000 mg/kg, p.o. in rats. Both acute as well as chronic administration of CPE (100, 200 and 400 mg/kg, p.o.) did not produce any gastric lesion in rats. These data indicate that CPE possesses significant anti-inflammatory activity without ulcerogenic activity suggesting its potential as an anti-inflammatory agent for use in the treatment of various inflammatory diseases.

Antihyperglycemic and antihyperlipidemic activity of ethyl acetate fraction of Rhododendron arboreum Smith flowers in streptozotocin induced diabetic rats and its role in regulating carbohydrate metabolism.

OBJECTIVE: To explore and identify the most potent antihyperglycemic fraction from the ethanol extract of Rhododendron arboreum (R. arboreum) flowers. METHODS: Normal and streptozotocin induced diabetic rats were treated with all four fractions of R. arboreum flowers for short term and with fraction 3 for long term study. On completion of the treatment, a range of indicators were tested including fasting blood glucose, plasma protein, haemoglobin A1C, insulin secretion, body weight, blood lipid profile and carbohydrate metabolism regulating enzymes of liver. RESULTS: In short term study, the fraction 3 (Active fraction) produced a significant (P<0.000 1) reduction (73.6%) in blood glucose level at a dose of 200 mg/kg after the treatment in the diabetic rats. Administration of active fraction (200 and 400 mg/kg) once daily for 30 d in streptozotocin diabetic rats resulted in a significant (P<0.001 to P<0.000 1) fall in blood glucose level, hemoglobin A1C, serum urea and creatinine with significant but a increase in insulin level similar to standard drug glybenclamide. Further, the active fraction showed antihyperlipidemic activity as evidenced by significant (P<0.001 to P<0.000 1) decreases in serum serum total cholesterol, triglycerides, low density lipoprotein cholesterol and very low density cholesterol levels coupled together with elevation of high density lipoprotein cholesterol in the diabetic rats. CONCLUSIONS: The active fraction of R. arboreum flowers decreases streptozotocin induced hyperglycemia by promoting insulin secretion and glycolysis and by decreasing gluconeogenesis.

Antihyperglycemic activity, antihyperlipedemic activity, haematological effects and histopathological analysis of Sapindus mukorossi Gaerten fruits in streptozotocin induced diabetic rats.

OBJECTIVE: To investigate the antihyperglycemic and antihyperlipidemic properties of hydroalcoholic extract of fruits of Sapindus mukorossi Gaerten and its beneficial effect on haematological parameters with histopathological analysis in streptozotocin induced diabetic rats. METHODS: Sapindus mukorossi fruits extract (250 and 500 mg/kg body weight) and standard drug glybenclamide (0.5 mg/kg body weight) were administered to diabetic rats. Effect of extract on hyperglycemia, hyperlipidemia and hematological parameters was studied in diabetic rats. Histopathological changes in diabetic rat pancreas were also observed after extract and glybenclamide treatment. RESULTS: Daily oral administration of Sapindus mukorossi fruits extract (250 and 500 mg/kg body weight) and glybenclamide for 20 days showed beneficial effects on blood glucose level (P<0.01) and lipid level. The extract has a favorable effect on the histopathological changes of the pancreas in streptozotocin induced diabetes. CONCLUSION: These findings reveal that the hydroalcoholic extract of Sapindus mukorossi fruits extract possesses antihyperglycemic and antihyperlipidemic properties. In addition, the extract can prevent various complications of diabetes and improve some haematological parameters.

Protective effect of ethyl acetate fraction of Rhododendron arboreum flowers against carbon tetrachloride-induced hepatotoxicity in experimental models.

OBJECTIVE: To evaluate the hepatoprotective potential of ethyl acetate fraction of Rhododendron arboreum (Family: Ericaceae) in Wistar rats against carbon tetrachloride (CCl(4))-induced liver damage in preventive and curative models. MATERIALS AND METHODS: Fraction at a dose of 100, 200, and 400 mg/kg was administered orally once daily for 14 days in CCl(4)-treated groups (II, III, IV, V and VI). The serum levels of glutamic oxaloacetic transaminase (SGOT), glutamate pyruvate transaminase (SGPT), alkaline phosphatase (SALP), γ-glutamyltransferase (γ -GT), and bilirubin were estimated along with activities of glutathione S-transferase (GST), glutathione reductase, hepatic malondialdehyde formation, and glutathione content. RESULT AND DISCUSSION: The substantially elevated serum enzymatic activities of SGOT, SGPT, SALP, γ-GT, and bilirubin due to CCl(4) treatment were restored toward normal in a dose-dependent manner. Meanwhile, the decreased activities of GST and glutathione reductase were also restored toward normal. In addition, ethyl acetate fraction also significantly prevented the elevation of hepatic malondialdehyde formation and depletion of reduced glutathione content in the liver of CCl(4)-intoxicated rats in a dose-dependent manner. Silymarin used as standard reference also exhibited significant hepatoprotective activity on post-treatment against CCl(4)-induced hepatotoxicity in rats. The biochemical observations were supplemented with histopathological examination of rat liver sections. The results of this study strongly indicate that ethyl acetate fraction has a potent hepatoprotective action against CCl(4)-induced hepatic damage in rats.

Hepatoprotective and antioxidant activity of Amaranthus spinosus against CCl4 induced toxicity.

AIM: 50% ethanolic extract (ASE) of Amaranthus spinosus (whole plant) was evaluated for in vitro antioxidant and hepatoprotective activity. METHODS: The total phenolics and reducing capacity of ASE was determined using standard curve of gallic acid (0-1.0mg/ml) and butylated hydroxy anisole. In vitro antioxidant activity was determined by DPPH, superoxide, hydroxyl radicals, hydrogen peroxide and nitric oxide scavenging methods. The hepatoprotective activity of ASE was evaluated at 6, 7, 8, 9 and 10 microg/ml concentration against CCl(4) (1%) induced toxicity in freshly isolated rat hepatocytes and HepG2 cells. RESULTS: ASE was found to contain 336+/-14.3mg/g total polyphenolics expressed as gallic acid equivalent while the reducing capacity was 2.26 times of BHA. ASE showed significant antioxidant activity in DPPH assay (IC(50) 29 microg/ml), scavenges superoxide (IC(50) approximately 66-70 microg/ml), hydrogen peroxide (IC(50) approximately 120-125 microg/ml), hydroxyl radicals (IC(50) approximately 140-145 microg/ml) and nitric oxide (IC(50) approximately 135-140 microg/ml). ASE (6, 7, 8, 9 and 10 microg/ml) was able to normalise the levels of biochemical parameters in isolated rat hepatocytes intoxicated with CCl(4). A dose dependent increase in percentage viability was observed in CCl(4) intoxicated HepG2 cells. CONCLUSIONS: ASE possesses significant hepatoprotective activity which might be due to antioxidant defence factors and phenolics might be the main constituents responsible for activity.

Antinociceptive activity of Amaranthus spinosus in experimental animals.

AIM OF THE STUDY: 50% ethanol extract (ASE) of Amaranthus spinosus (whole plant) has been evaluated for antinociceptive and antiinflammatory activities. MATERIALS AND METHODS: Analgesic and antiinflammatory activities were studied by measuring nociception by formalin, acetic acid, hot plate, tail immersion method while inflammation was induced by carrageenan. RESULTS: ASE had significant dose dependent percentage protection against acetic acid (0.6% of 10 ml) induced pain and the effects were also compared to aspirin, morphine and naloxone while formalin induced pain (0.05 ml of 2.5%) was significantly blocked only at higher dose (400mg/kg) in first phase. ASE significantly blocked pain emanating from inflammation at all the doses in second phase. The reaction time in hot plate was increased significantly and dose dependently where as pretreatment with naloxone rigorously reduced the analgesic potentials of ASE. Further in tail immersion test the same dose dependent and significant activity was observed. Aspirin had no effect on thermal induced pain i.e. hot plate and tail immersion tests but showed an effect on writhing test. CONCLUSIONS: Our investigation show that Amaranthus spinosus possess significant and dose dependant antiinflammatory activity, it has also central and peripheral analgesic activity.