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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.
Phytomedicine. 2014 Sep 25; 21(11):1237-48.P

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 3h of the treatment. The administration of 1 and 2 (50 mg/kgb.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.

Authors+Show Affiliations

Plant Tissue Culture Laboratory, Department of Botany, School of Life Sciences, Bharathiar University, Coimbatore 641 046, Tamil Nadu, India. Electronic address: mahendran0007@gmail.com.Department of Chemistry, School of Chemical Sciences, Bharathiar University, Coimbatore 641 046, Tamil Nadu, India.Computational Biology Lab, Bioinformatics Department, Bharathiar University, Coimbatore 641 046, Tamil Nadu, India.Computational Biology Lab, Bioinformatics Department, Bharathiar University, Coimbatore 641 046, Tamil Nadu, India.Computational Biology Lab, Bioinformatics Department, Bharathiar University, Coimbatore 641 046, Tamil Nadu, India.Department of Chemistry, School of Chemical Sciences, Bharathiar University, Coimbatore 641 046, Tamil Nadu, India.Plant Tissue Culture Laboratory, Department of Botany, School of Life Sciences, Bharathiar University, Coimbatore 641 046, Tamil Nadu, India.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

25172785

Citation

Mahendran, G, et al. "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." Phytomedicine : International Journal of Phytotherapy and Phytopharmacology, vol. 21, no. 11, 2014, pp. 1237-48.
Mahendran G, Manoj M, Murugesh E, et al. 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. Phytomedicine. 2014;21(11):1237-48.
Mahendran, G., Manoj, M., Murugesh, E., Sathish Kumar, R., Shanmughavel, P., Rajendra Prasad, K. J., & Narmatha Bai, V. (2014). 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. Phytomedicine : International Journal of Phytotherapy and Phytopharmacology, 21(11), 1237-48. https://doi.org/10.1016/j.phymed.2014.06.011
Mahendran G, et al. 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. Phytomedicine. 2014 Sep 25;21(11):1237-48. PubMed PMID: 25172785.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - 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. AU - Mahendran,G, AU - Manoj,M, AU - Murugesh,E, AU - Sathish Kumar,R, AU - Shanmughavel,P, AU - Rajendra Prasad,K J, AU - Narmatha Bai,V, Y1 - 2014/07/22/ PY - 2014/01/03/received PY - 2014/04/30/revised PY - 2014/06/19/accepted PY - 2014/8/31/entrez PY - 2014/8/31/pubmed PY - 2015/3/31/medline KW - 2BEL KW - Antidiabetic activity KW - Antioxidant KW - SUR1 KW - Swertia corymbosa KW - Xanthones SP - 1237 EP - 48 JF - Phytomedicine : international journal of phytotherapy and phytopharmacology JO - Phytomedicine VL - 21 IS - 11 N2 - 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 3h of the treatment. The administration of 1 and 2 (50 mg/kgb.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. SN - 1618-095X UR - https://www.unboundmedicine.com/medline/citation/25172785/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_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0944-7113(14)00260-8 DB - PRIME DP - Unbound Medicine ER -