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Byline: Neeraj. Verma, Anil. Singh, G. Amresh, P. Sahu, Ch. Rao Objective: To evaluate the hepatoprotective potential of ethyl acetate fraction of Rhododendron arboreum (Family: Ericaceae) in Wistar rats against [...]

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 galactosamine/lipopolysaccharide (GalN/LPS)-induced liver injury in rats. 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 GalN/LPS-induced hepatocellular injury. [ABSTRACT FROM AUTHOR]

The ethanol extract (50%) of the whole plant of Amaranthus spinosus Linn. (Amaranthaceae) (ASE) significantly inhibited travel of a charcoal meal at three different doses of ASE, but when 400 mg/kg of ASE was repeated in the presence of yohimbine, intestinal propulsive inhibition decreased, while morphine reversed the activity. The percentages related to controls for the onset of diarrhea were 16.58, 83.42, and 116.18% at doses of 100, 200, and 400 mg/kg of ASE, while with morphine this value was 123.93% compared to controls. The percentage purging frequency related to controls was 41.09, 64.38, 71.23, and 86.30% at three different doses of ASE and with morphine, respectively. The inhibitions in intestinal accumulation were 8.9, 48.16, and 68.06% at doses of 100, 200, and 400 mg/kg of ASE, respectively, compared to control, while inhibition with yohimbine was 50.78%. Antidiarraheal indices of ASE were 23.55, 49.16, and 76.53 at the three different doses of ASE, while morphine had a maximum index of 88.45. Protection in ethanol- induced ulcer was 51.07, 55.91, 77.95, and 60.75%, but in aspirin-induced ulcer it was 41.33, 61.77, 80.88, and 74.66% at doses of 100, 200, and 400 mg/kg of ASE and with cimetidine, respectively. Lipid peroxidation was also associated with a concomitant decrease in ulcer index, while protection was 56.96, 63.29, 81.01, and 52.32% at three different doses of ASE and with cimetidine in cold restraint-induced ulcer. [ABSTRACT FROM AUTHOR]

The current study is an effort to identify the effect of a hydroalcohol (50% ethanol) extract of roots of Cissampelos pareira (L.) Hirsuta (Menispermaceae) (CPE) in forestomach cancer and on carcinogen metabolizing phase I and phase II enzymes along with antioxidant enzymes. In forestomach, the activities of glutathione S-transferase (GST), DT-diaphorase (DTD), and superoxide dismutase (SOD) increased significantly and dose-dependently. The protective effect of CPE was studied against benzo(a)pyrene [B(a)P]-induced gastric cancer in mice, and the tumor incidence was reduced and the mean number of tumors and the tumor multiplicity were reduced significantly and dose-dependently. The modulatory effect of CPE was also examined on carcinogen metabolizing phase I and phase II enzymes, antioxidant enzymes, glutathione content, lactate dehydrogenase, and lipid peroxidation in liver. Significant increases in the levels of acid-soluble sulfhydryl (-SH) and cytochrome P450 contents and in enzyme activities of cytochrome P450 reductase, cytochrome b5 reductase, GST, DTD, SOD, catalase, glutathione (GSH) peroxidase, and GSH reductase but decreased malondialdehyde (MDA) were observed. Butylated hydroxyanisole (BHA) showed an increase in hepatic levels of GSH content, cytochrome b5, DTD, GST, glutathione reductase (GR), and catalase, whereas MDA formation was inhibited significantly. BHA also showed increased levels of DTD, GST, and SOD significantly in forestomach. The enhanced GSH level and enzyme activities involved in xenobiotic metabolism and maintaining antioxidant status of cells are suggestive of a chemopreventive efficacy of Cissampelos pareira against chemotoxicity, including carcinogenicity. [ABSTRACT FROM AUTHOR]

Abstract: 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 10μg/ml concentration against CCl4 (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 (IC50 29μg/ml), scavenges superoxide (IC50 ∼66–70μg/ml), hydrogen peroxide (IC50 ∼120–125μg/ml), hydroxyl radicals (IC50 ∼140–145μg/ml) and nitric oxide (IC50 ∼135–140μg/ml). ASE (6, 7, 8, 9 and 10μg/ml) was able to normalise the levels of biochemical parameters in isolated rat hepatocytes intoxicated with CCl4. A dose dependent increase in percentage viability was observed in CCl4 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. [Copyright &y& Elsevier]

Background: Lagerstroemia speciosa (SEL) leaves are a popular folk medicine for diabetes treatment due to presence of corosolic acid. It has low water solubility resulting poor absorption after oral administration. Self micro-emulsified drug delivery system is the way by which we can improve the oral absorption of drug., Objective: The objective of this study was to develop the self micro-emulsifying formulation of standardized extract of SEL leaves and evaluate its pharmacodynamic performance for antidiabetic activity., Materials and Methods: The SME formulation was prepared by using sefsol-218 as oil, cremophor-EL as surfactant and transcutol-P as co-surfactant. The ratio of surfactant and co-surfactant was determined by pseudoternary phase diagram. SME formulations were characterized for dilution at different pH, self emulsification, optical clarity, globule size and thermodynamic stability. Pharmacodynamic evaluation of formulations was assessed in Wistar rats by using parameters viz. blood glucose level and serum lipid profile., Results: SEL loaded SME formulation was successfully developed by using sefsol-218, cremophor-EL and transcutol-P with a droplet size 23.53 nm. Pharmacodynamic results showed a higher reduction in blood glucose by SME formulation than SEL without SMES respectively at 50 mg/kg dose while reduction produced at dose of 100 mg/kg was found significant and better on 15th day of study. The percentage reduction produced by SME formulation on serum lipid profile was also significant and was more prominent than SEL., Conclusion: This study confirms that the formulation elevates the pharmacodynamic performance of SEL approximately two fold., (Copyright © 2017 Transdisciplinary University, Bangalore and World Ayurveda Foundation. Published by Elsevier B.V. All rights reserved.)

Self microemulsifying formulation is an approach used for enhancing the bioavailability of poorly soluble molecules due to their lipidic nature and small particle size. The objective of the present study was to evaluate the hepatoprotective activity of poorly soluble hydroxy- and polyhydroxy-organic phytomolecules rich Lagerstroemia speciosa leaves extract in modern formulation i.e. "Self microemulsifying System". Different doses of SME (Self microemulsifying) formulation of L.   speciosa leaves extract were evaluated for the hepatoprotective activity against carbon tetrachloride induced liver toxicity in rats. The parameters evaluated were (a) biochemical parameters like serum enzymes: aspartate aminotransferase (AST), serum glutamate pyruvate transaminase (ALT), serum alkaline phosphatase (ALP) and total bilirubin (b) liver antioxidant parameters as estimation of Lipid peroxidation (LPO), catalase (CAT), Superoxide dismutase (SOD) activity and concentration of reduced glutathione (GSH). Oral administration of SME formulation provided the significant protection in marker enzyme of treated group at 100 mg/kg, p.o. as AST (P < 0.001), ALT (P < 0.001), ALP (P < 0.001) and total bilirubin (P < 0.001) comparable to the group treated with silymarin. Treatment with SME formulation at the doses of 100 mg/kg, p.o. significantly prevented the rise in levels of LPO significantly (P < 0.001). The GSH, SOD and CAT contents had significantly (P < 0.001) increased in SME formulation treated groups whereas carbon tetrachloride intoxicated group had shown significant decrease in these parameters compared to control group. Formulation at the dose 100 mg/kg, p.o. has shown maximum protection which was almost comparable to those of the normal control and standard. The histological observations further uphold the results for hepatoprotective activity.

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 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.

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.