title: Yeast α-glucosidase inhibition by isoflavones from plants of Leguminosae as an in vitro alternative to acarbose.
abstract: In the course of searching for new classes of α-glucosidase inhibitors originated from natural resources, 11 kinds of isoflavones, i.e., medicarpin (1), formononetin (2), mucronulatol (3), (3R)-calussequinone (5), (3R)-5'-methoxyvestitol (6), tectorigenin (7), biochanin A (8), tuberosin (9), calycosin (10), daidzein (11), and genistein (12), as well as a flavone, liquritigenin (4), were isolated as active principles responsible for the yeast α-glucosidase inhibitory activity from two leguminous plant extracts, i.e., the heartwood extract of Dalbergia odorifera and the roots extract of Pueraria thunbergiana. Each components (1-12) demonstrated a significantly potent inhibition on yeast α-glucosidase in a dose dependent manner when the p-nitrophenyl-α-D-glucopyranoside was used as a substrate in vitro. The concentration required for 50% enzyme inhibition (IC50) were calculated as 2.93 mM (1), 0.51 mM (2), 3.52 mM (7) 0.35 mM (8), 3.52 mM (9), 0.85 mM (11), and 0.15 mM (12) when that of reference drug acarbose was evaluated as 9.11 mM, in vitro. However, isoflavone glycosides, i.e., puerarin (13), daidzin (14), formononetin-7-O-β-glucopyranoside (15), and genistin (16), exhibited a relatively poor inhibitory activity on yeast α-glucosidase as compared with the corresponding isoflavone (2, 11, 12), respectively.
authors.affiliation: Korea Research Institute of Chemical Technology, Daejeon 305-600, Korea.
authors.forename: Chun Whan
authors.initials: CW
authors.lastname: Choi
authors.forename: Yeon Hee
authors.initials: YH
authors.lastname: Choi
authors.forename: Mi-Ran
authors.initials: MR
authors.lastname: Cha
authors.forename: Dae Seok
authors.initials: DS
authors.lastname: Yoo
authors.forename: Young Sup
authors.initials: YS
authors.lastname: Kim
authors.forename: Gyu Hwan
authors.initials: GH
authors.lastname: Yon
authors.forename: Kyung Sik
authors.initials: KS
authors.lastname: Hong
authors.forename: Young Ho
authors.initials: YH
authors.lastname: Kim
authors.forename: Shi Yong
authors.initials: SY
authors.lastname: Ryu
mesh_terms: D020909:Acarbose / Q000737:chemistry; D055808:Drug Discovery; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000302:isolation & purification; D007887:Fabaceae / Q000737:chemistry*; D065089:Glycoside Hydrolase Inhibitors; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000302:isolation & purification; D007529:Isoflavones / Q000737:chemistry* / Q000302:isolation & purification; D007700:Kinetics; D010936:Plant Extracts / Q000737:chemistry; D012441:Saccharomyces cerevisiae / Q000201:enzymology*; D029701:Saccharomyces cerevisiae Proteins / Q000037:antagonists & inhibitors*
chemical_list: D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D007004:Hypoglycemic Agents; D007529:Isoflavones; D010936:Plant Extracts; D029701:Saccharomyces cerevisiae Proteins; D020909:Acarbose