swertiamarin and Diabetes-Mellitus--Type-2

The herbal plant extract of Enicostemma littorale is widely used to medicate and treat type II Diabetes. This extract in medicine has shown its value in reducing blood glucose & lipid levels, and improving the kidney functioning, lipid profile, controlling blood pressure and heart rate. The well characterized chemical components such as iridoid and secoiridoid glycosides are present in aqueous and ethanolic extracts of the plant. Swertiamarin, a secoiridoid glycoside, is identified as the lead compound that confers anti-hyperglycemic & anti-hyperlipidemic effects. The swertiamarin binds with one or more molecular targets to alter their expression and/or activity. The in silico, in vivo and in vitro studies have been carried out to uncover the underlying molecular mechanism of action of swertiamarin and its derivatives for showing the better anti-diabetic & anti-hyperlipidemic activities. In brief, the present review focuses on unraveling the information about molecular targets of swertiamarin. Our review will open new avenues to develop therapeutic approaches and drugs to treat diabetes and other inflammatory diseases.

Topics: Animals; Computer Simulation; Diabetes Mellitus, Type 2; Disease Models, Animal; Gentianaceae; Glucose; Humans; Hypoglycemic Agents; Hypolipidemic Agents; Insulin; Iridoid Glucosides; Lipid Metabolism; Metabolic Networks and Pathways; Metabolic Syndrome; Molecular Targeted Therapy; Pyrones; Signal Transduction; Structure-Activity Relationship

Swertiamarin is a lead, biologically active compound obtained from

Topics: Diabetes Mellitus, Type 2; Dipeptidyl-Peptidase IV Inhibitors; Humans; Hypoglycemic Agents; Iridoid Glucosides; Molecular Docking Simulation; Pyrones

Swertiamarin (Sw) and quercetin (Qu) have been isolated from different plants and are reported for their antidiabetic activities. The plants from which swertiamarin and quercetin were isolated are also traditionally used in the treatment of diabetes mellitus.. The present study is aimed to evaluate the synergistic effect of a combination of swertiamarin and quercetin (CSQ) on α-amylase in vitro and on streptozotocin (STZ) induced diabetes mellitus in vivo.. Swertiamarin was isolated from the plant Enicostemma axillare and quercetin was procured in its pure form. Sw, Qu and CSQ were evaluated for in vitro α-amylase inhibitory activity. Based on the in vitro study results, CSQ was assessed for in vivo streptozotocin induced diabetes mellitus in Wistar rats. The effect of CSQ on blood glucose levels, body weight, serum biochemical parameters and antioxidant enzymes such as glutathione (GSH), superoxide dismutase (SOD), catalase, glutathione peroxidase (GPx) and lipid peroxide levels were estimated. The histopathological observations of pancreatic tissues were also made.. The purity of swertiamarin was confirmed by HPLC. The results showed that CSQ was found to possess high percentage of inhibition in an in vitro α-amylase inhibitory study. In a STZ-induced type 2 diabetes mellitus (T2DM), body weight of rats in CSQ treated and control groups were unaltered. A marked reduction in the blood glucose levels was observed in the CSQ treated groups on 14th and 28th day. Decrease in the levels of low-density lipoprotein (LDL), triglycerides, total cholesterol and an increase in high-density lipoprotein (HDL) cholesterol level was observed in a dose dependant in CSQ treated groups. However, CSQ treated groups could significantly improve antioxidant protection by increasing the levels of serum GSH, SOD, Catalase and GPx and decreasing the levels of lipid peroxide (p < 0.05). In the histopathological study, the pancreatic islets of Langerhans and vacuolization have shown significant increase in both the treated groups.. The combination of swertiamarin and quercetin (CSQ) has proven a preventive and therapeutic effect against T2DM and suggests that this is a potential combination of phytoconstituents for excellent hypoglycemic activity in T2DM.

Topics: alpha-Amylases; Animals; Blood Glucose; Body Weight; Diabetes Mellitus, Experimental; Diabetes Mellitus, Type 2; Ethnopharmacology; Hyperglycemia; Hyperlipidemias; Hypoglycemic Agents; Iridoid Glucosides; Lipids; Male; Oxidative Stress; Pyrones; Quercetin; Rats; Rats, Wistar

Dyslipidaemia is one of the major risk factors for cardiovascular disease in diabetes mellitus. Lipid changes associated with diabetes mellitus are attributed to increases in free fatty acid flux, secondary to insulin resistance. In the present study, we have investigated the beneficial effects of swertiamarin on dyslipidaemic conditions associated with type 2 diabetes in streptozotocin-induced type 2 diabetic rats. Swertiamarin (50 mg/kg, i.p.) administered once a day for 6 weeks resulted in significant (p < 0.001) reductions in serum triglycerides, cholesterol and low-density lipoprotein levels in diabetic animals as compared with diabetic control animals. Serum fasting glucose was significantly (p < 0.05) decreased, moreover, the insulin sensitivity index was significantly (p < 0.05) increased in swertiamarin treated animals. Overall the data suggest that swertiamarin has beneficial effects on diabetic associated complications such as dyslipidaemia.

Topics: Animals; Blood Glucose; Diabetes Mellitus, Experimental; Diabetes Mellitus, Type 2; Dyslipidemias; Gentianaceae; Hypoglycemic Agents; Insulin Resistance; Iridoid Glucosides; Lipase; Lipoproteins, LDL; Male; Phytotherapy; Pyrones; Rats; Streptozocin