title: Acylated glucosylflavones as α-glucosidase inhibitors from Tinospora crispa leaf.
abstract: The ethanolic extract of Tinospora crispa leaf had shown inhibitory activity toward α-glucosidase. Bioassay guided fractionation and separation of this extract led to the isolation of 17 flavonoids. Among them, four acylated glycosylflavonoids (6, 8, 9, 15) are new compounds. Their structures were elucidated on the basis of spectroscopic analysis. Among the isolated compounds, isovitexin 2″-(E)-p-coumarate (8) showed the best activity against α-glucosidase with an IC50 value of 4.3±1.4μM. However, isoorientin 2″-(E)-p-coumarate (7), the 3'-hydroxylated 8, is much less active (IC50 35.7μM). Such significant difference was rationalized by CAD study on α-glucosidase.
authors.affiliation: School of Pharmacy, College of Medicine, National Taiwan University, 33, Linsen S. Rd., Taipei 10050, Taiwan, ROC.
authors.forename: Chi-Chih
authors.initials: CC
authors.lastname: Chang
authors.affiliation: Department of Chemical & Materials Engineering, Chinese Culture University, 55, Hwa-Kang Road, Yang-Ming-Shan, Taipei 11114, Taiwan, ROC.
authors.forename: Sheau Ling
authors.initials: SL
authors.lastname: Ho
authors.affiliation: School of Pharmacy, College of Medicine, National Taiwan University, 33, Linsen S. Rd., Taipei 10050, Taiwan, ROC. Electronic address: shoeilee@ntu.edu.tw.
authors.forename: Shoei-Sheng
authors.initials: SS
authors.lastname: Lee
mesh_terms: D000431:Ethanol; D005419:Flavonoids / Q000737:chemistry* / Q000302:isolation & purification; D005960:Glucosides / Q000737:chemistry* / Q000302:isolation & purification; D065089:Glycoside Hydrolase Inhibitors / Q000737:chemistry* / Q000302:isolation & purification; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000302:isolation & purification; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry; D018515:Plant Leaves / Q000737:chemistry; D012997:Solvents; D013329:Structure-Activity Relationship; D031610:Tinospora / Q000737:chemistry*; D000520:alpha-Glucosidases / Q000737:chemistry*
chemical_list: D005419:Flavonoids; D005960:Glucosides; D065089:Glycoside Hydrolase Inhibitors; D007004:Hypoglycemic Agents; D010936:Plant Extracts; D012997:Solvents; D000431:Ethanol; D000520:alpha-Glucosidases
keywords: Acylated glucosylflavones; Anti-α-glucosidase; Molecular docking; Tinospora crispa