In vivo anti-diabetic,antioxidant and molecular docking studies of 1, 2, 8-trihydroxy-6-methoxy xanthone and 1, 2-dihydroxy-6-methoxyxanthone-8-O-β-d-xylopyranosyl isolated from Swertia corymbosa |
| |
| Institution: | 1. Plant Tissue Culture Laboratory, Department of Botany, School of Life Sciences, Bharathiar University, Coimbatore 641 046, Tamil Nadu, India;2. Department of Chemistry, School of Chemical Sciences, Bharathiar University, Coimbatore 641 046, Tamil Nadu, India;3. Computational Biology Lab, Bioinformatics Department, Bharathiar University, Coimbatore 641 046, Tamil Nadu, India;1. Laboratorio de Biofísica y Biocatálisis, Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Díaz Mirón, Ciudad de México 11340, Mexico;2. Laboratorio de Investigación en Bioquímica, Sección de Estudios de Posgrado e Investigación y Departamento de Formación Básica Disciplinaria, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Díaz Mirón, Ciudad de México 11340, Mexico;3. Laboratorio de Modelado Molecular, Diseño de Fármacos y Bioinformática, Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Díaz Mirón, Ciudad de México 11340, Mexico;1. Natural Product Chemistry, CSIR-Central Institute of Medicinal and Aromatic Plants-Research Centre, Boduppal, Hyderabad 500092, India;2. Toxicology Unit, Biology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India;3. Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India;4. Metabolic and Structural Biology Department, CSIR-CIMAP, Lucknow 226015, UP, India;1. Institute of Pharmaceutical Science, King’s College London, 150 Stamford Street, London SE1 9NH, UK;2. Department of Chemistry, King’s College London, 150 Stamford Street, London SE1 9NH, UK;1. Department of Pharmacy, Faculty of Biological Sciences, University of Malakand, Chakdara 18000 Dir (L), KP, Pakistan;2. Department of Pharmacy, University of Swabi, KP, Pakistan;3. Department of Chemistry, COMSATS University Islamabad, Abbottabad Campus, 22060 Abbottabad, Pakistan;1. Jan Nayak Ch. Devi Lal Memorial College of Pharmacy, Sirsa, 125055, Haryana, India;2. Chitkara College of Pharmacy, Chitkara University, Rajpura, Patiala, 140401, Punjab, India |
| |
| Abstract: | 1, 2, 8-trihydroxy-6-methoxy xanthone (1) and 1, 2- dihydroxy-6-methoxyxanthone-8-O-β-d-xylopyranosyl (2) are the main constituents of petroleum ether and ethyl acetate extracts from Swertia corymbosa (Gentinaceae), a medicinal plant used in Indian traditional system for the treatment of diabetes. The present study was designed to examine the antihypoglycemic, antihyperlipidemic and antioxidant effect of compounds 1 and 2 in streptozotocin (STZ) induced diabetic rats. Diabetes was induced in male Wistar rats by a single intraperitoneal injection of STZ (60 mg/kg b.w.). The isolated compounds 1 and 2 at a dose of 50 mg/kg b.w., produced the maximum fall of 83% in the blood glucose level in the diabetic rats after 3 h of the treatment. The administration of 1 and 2 (50 mg/kg b.w.) daily for 28 days in STZ induced diabetic rats, resulted in a significant decrease in blood glucose, glycosylated hemoglobin, SGOT, SGPT, ALP serum urea and creatinine with significant rise in plasma insulin level. Test compounds 1 and 2 showed antihyperlipidemic activities as evidenced by significant decrease in serum TC, TG, LDL-C, VLDL-C levels coupled together with elevation of HDL-C level in diabetic treated rats when compared to diabetic untreated rats, indicate the protective role against liver and kidney damage. The results of histopathology also showed 1 and 2 protected tissues (pancreas, liver and kidney) against peroxidation damage and maintained tissue integrity. Further, the molecular interaction study of the ligands 1, 2 and glibenclamide with various diabetes mellitus related protein targets like glucokinase (PDB ID: 1V4S), fructose-1, 6-bisphosphatase 1 (PDB ID: 2JJK) 11-β-hydroxysteroid dehydrogenase (PDB ID: 2BEL) and modeled protein sulfonylurea receptor 1 (SUR1) showed that ligand 1 and 2 possess binding affinity with all protein targets except for 2BEL target protein for which ligand 1 has no interaction. The ligand pose with 2BEL and SUR1 protein target of ligand 2 gave the best binding conformation. Hence 1 and 2 can be considered for developing into a potent antidiabetic drug. |
| |
| Keywords: | Xanthones Antidiabetic activity Antioxidant 2BEL SUR1 |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
