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Anti hyperglycaemic study of natural inhibitors for Insulin receptor.

ABSTRACT: UNLABELLED:Diabetes is a metabolic disorder associated with either improper functioning of the beta-cells or wherein cells fail to use insulin properly. Insulin, the principal hormone regulates uptake of glucose from the blood into most of the cells except central nervous system. Therefore, deficiency of insulin or the insensitivity of its receptors plays a key role in all forms of diabetes. In the present work, attempt has been made to find out plant sources which show anti hyperglycaemic activity (AhG) (i.e. compounds that bring down the blood glucose level in the body). Ayurvedic plants showing AhG activity formed the basis of our study by using the platform of Computer Aided Drug Designing (CADD). Among 600 plants showing AhG activity, 500 compounds were selected and screened, out of which 243 compounds showed drug likeness property that can be used as therapeutic ligand/drug. Initial screening of such compounds was done based on their drug likeness or biochemical properties. Dynamic interaction of these molecules was captured through Protein-Ligand study. It also gave an insight of the binding pockets involved. Bench marking of all the parameters were done using the diabetic inhibitor drug, Glipizide. Pharmacokinetic studies of the compounds such as Aloins, Capparisine, Funiculosin and Rhein exhibited less toxicity on various levels of the body. As a conclusion these ligands can lay a foundation for a better anti-diabetic therapy. ABBREVIATIONS:AhG - Anti hyperglycaemic, CADD - Computer Aided Drug Designing.

SUBMITTER: Chatterjee S

PROVIDER: S-EPMC3530871 | biostudies-literature | 2012

REPOSITORIES: biostudies-literature

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Anti hyperglycaemic study of natural inhibitors for Insulin receptor.

Chatterjee Subhojyoti S Narasimhaiah Akshaya Lakshmi AL Kundu Sanjay S Anand Santosh S

Bioinformation 20121208 24

<h4>Unlabelled</h4>Diabetes is a metabolic disorder associated with either improper functioning of the beta-cells or wherein cells fail to use insulin properly. Insulin, the principal hormone regulates uptake of glucose from the blood into most of the cells except central nervous system. Therefore, deficiency of insulin or the insensitivity of its receptors plays a key role in all forms of diabetes. In the present work, attempt has been made to find out plant sources which show anti hyperglycaem ...[more]

PMID: 23275719

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Project description:Synacinn™ is a standardized polyherbal supplement formulated from Cinnamomum zeylanicum Blume, Curcuma zanthorrhiza Roxb., Syzygium polyanthum (Wight) Walp., Orthosiphon stamineus Benth. and Andrographis paniculata (Burm.f.) Nees. It is designed for the synergistic treatment of diabetes mellitus and its complications. Although the beneficial effects are yet to be verified scientifically, it is traditionally used to improve general health in patients with diabetes. This study aimed to evaluate the anti-hyperglycemic effects of Synacinn™ in a streptozotocin-induced type 1 diabetes rat model. Initially, Synacinn™ was used for in vivo acute oral toxicity tests and 14 day repeated dose toxicity tests to determine the toxicity levels. An efficacy study of Synacinn™ was carried out via the oral administration of 10, 50, 100, 250, and 250 (b.i.d.) mg kg-1 doses to streptozotocin-induced diabetic rats. After 28 days, blood serum was collected to measure the fasting blood glucose, triglyceride, cholesterol, alanine aminotransferase, alkaline phosphatase, creatinine, and uric acid levels. The liver, kidney, and pancreas structures were histopathologically analyzed. In silico binding interaction studies of five phytochemicals in Synacinn™ identified via HPLC with glucokinase were performed using molecular docking analysis. The results showed that although no mortality was observed during the acute oral toxicity tests, notable damage to the liver and kidney occurred during the 14 day repeated dose testing at Synacinn™ levels of 600 mg kg-1 and 2000 mg kg-1. Treatment with 250 mg kg-1 (b.i.d.) Synacinn™ of the streptozotocin-induced type 1 diabetic rats significantly (p < 0.05) improved the fasting blood glucose (59%), triglyceride (58%), cholesterol (47%), alanine aminotransferase (60%), alkaline phosphatase (90%), and creatinine (32%) levels. Synacinn™ also improved the relative weights of liver (35%), kidney (36%), and pancreatic (36%) tissue. Histological analysis showed improvements in the conditions of the central vein of the liver, the kidney Bowman's capsule and glomerulus, and the pancreatic islets of Langerhans. HPLC analysis of a standardized extract identified five active phytochemicals: andrographolide (17.36 mg g-1), gallic acid (11.5 mg g-1), curcumin (2.75 mg g-1), catechin (3.9 mg g-1), and rosmarinic acid (5.54 mg g-1). Molecular docking studies with glucokinase showed that andrographolide yields the highest binding energy (-12.1 kcal mol-1), followed by catechin (-10.2 kcal mol-1), rosmarinic acid (-8.6 kcal mol-1), curcumin (-7.8 kcal mol-1), and gallic acid (-5.6 kcal mol-1). These current findings suggest that Synacinn™ at a dose of 250 mg kg-1 was non-toxic to rats. A twice-daily 250 mg kg-1 dose of Synacinn™ is an effective anti-hyperglycemic agent, lowering blood glucose, triglyceride, and cholesterol levels, and assisting the recovery of organ impairment caused by streptozotocin in type 1 diabetic rats.

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Anti hyperglycaemic study of natural inhibitors for Insulin receptor.

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Anti hyperglycaemic study of natural inhibitors for Insulin receptor.

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