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1.
Pharm Biol ; 52(2): 199-207, 2014 Feb.
Article in English | MEDLINE | ID: mdl-24074272

ABSTRACT

CONTEXT: Pterospermum acerifolium (L.) Willd (Sterculiaceae) has been traditionally used in the treatment of diabetes mellitus but no scientific data has been published supporting the claimed ethnomedical use. OBJECTIVE: The present study was designed to estimate the in silico, in vitro α-amylase inhibition potential and anti-diabetic activity of Pterospermum acerifolium bark. MATERIALS AND METHODS: In silico studies were performed between human pancreatic α-amylase (HPA) and ß-sitosterol by using autodock 4.2 software. In vitro α-amylase inhibition study was carried out with 50% ethanol extract of the bark (PABEE) and its various fractions. The active ethyl acetate fraction (PABEF) was sub-fractionated into three fractions (PABE1, PABE2 and PABE3). Two doses (15 and 30 mg/kg) based on acute toxicity studies, of the above fractions were subjected to antidiabetic screening in vivo by STZ-nicotinamide induced type II diabetic rats. RESULTS: In silico studies showed the potent inhibition of ß-sitosterol on human pancreatic amylase (HPA) with an estimated inhibition constant (Ki) of 269.35 nmol and two hydrogen bond interactions. PABEF showed marked α-amylase inhibition (69.94%) compared to other fractions. Diabetic rats treated with PABE3 (30 mg/kg) reduced the levels of fasting blood glucose, HbA1c, ALT, AST, ALP, triglycerides, total cholesterol, TBARS significantly (p < 0.01) and increased the levels of HDL-C, catalase, GSH, SOD significantly (p < 0.01) as compared to that of diabetic control animals. Histological studies on PABE3 treated group showed remarkable positive changes in ß-cells. CONCLUSION: The present study confirmed the antihyperglycemic activity along with its status on hepatic biomarkers, antihyperlipidemic and antioxidant properties of Pterospermum acerifolium bark.


Subject(s)
Hypoglycemic Agents/pharmacology , Malvaceae/chemistry , Pancreatic alpha-Amylases/antagonists & inhibitors , Plant Extracts/pharmacology , Animals , Computer Simulation , Diabetes Mellitus, Experimental/drug therapy , Diabetes Mellitus, Experimental/physiopathology , Diabetes Mellitus, Type 2/drug therapy , Diabetes Mellitus, Type 2/physiopathology , Dose-Response Relationship, Drug , Humans , Hydrogen Bonding , Hypoglycemic Agents/administration & dosage , Hypoglycemic Agents/isolation & purification , Male , Niacinamide/toxicity , Plant Bark , Plant Extracts/administration & dosage , Plant Extracts/toxicity , Rats , Rats, Wistar , Sitosterols/metabolism , Sitosterols/pharmacology , Software , Streptozocin/toxicity , Toxicity Tests, Acute
2.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-672505

ABSTRACT

Objective: Barleria lupulina Lindl (Acanthaceae) (B. lupulina) has been traditionally used in the treatment of rheumatoid arthritis but, no scientific data has been published supporting the claimed ethnomedical use. This study was designed to investigate the anti-arthritic potential of B. lupulina leaves and its role in immunomodulation. Methods: Methanol extract of B. lupulina (MEBL) leaves (300 and 600 mg/kg BW) was tested for its antiarthritic activity by various models namely, formalin-induced arthritis, adjuvant induced arthritis, collagen type II-induced arthritis and monosodium iodoacetate induced osteoarthritis. Immunomodulatory activity of the same was tested by measuring WBC Count, Spleen Weight, Spleen WBC Count and Delayed Type Hypersensitivity (DTH) Reaction.Results:MEBL extracts 300 mg/kg and 600 mg/ kg showed statistically significant inhibition (P<0.05 and P<0.001) of the edema formation and Myeloperoxidase (MPO) during experimental period and activities of antioxidants were restored significantly. MEBL extracts 300 mg/kg and 600 mg/kg significantly increased the Hemoglobin (Hb) level, serum albumin, total protein, calcium and phosphorus levels and reverted back the levels of WBC count and Erythrocyte Sedimentation Rate (ESR) (P<0.05 and P<0.01). Histopathological studies of ankle joints also supported this finding. Immunomodulatory study revealed an increase in the blood leukocytes count, weight of spleen, spleenic leukocytes count and increase in paw volume on delayed type hypersensitivity footpad thickness suggesting an uplift of immune status. Conclusions: The present study concluded that, MEBL holds antiarthritic and Immunomodulatory activity. Although subsequent study is required to evaluate the active constituents responsible for the activity.

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