title: Structure-activity relationships of bergenin derivatives effect on α-glucosidase inhibition.
abstract: The α-glucosidase inhibitory activities of bergenin derivatives were evaluated. Bergenin derivatives were synthesized from bergenin which is a characteristic compound of B. ligulata. A new bergenin derivative, 11-O-(3',4'-dimethoxybenzoyl)-bergenin showed the highest potent inhibitory activity among those of bergenin derivatives. The presence of substituents at 3',4'-position in bergenin derivatives altered the α-glucosidase inhibitory activity. 11-O-(3',4'-dimethoxybenzoyl)-bergenin was noncompetitive inhibitor for α-glucosidase. The present study reveals that bergenin derivatives could be classified as a new group of α-glucosidase inhibitors.
authors.affiliation: Department of Applied Chemistry, Faculty of Science and Engineering, Kinki University , Kowakae, Higashiosaka-shi, Osaka , Japan.
authors.forename: Yusei
authors.initials: Y
authors.lastname: Kashima
authors.forename: Hidehiko
authors.initials: H
authors.lastname: Yamaki
authors.forename: Takuya
authors.initials: T
authors.lastname: Suzuki
authors.forename: Mitsuo
authors.initials: M
authors.lastname: Miyazawa
mesh_terms: D001578:Benzopyrans / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D065089:Glycoside Hydrolase Inhibitors; D015394:Molecular Structure; D012441:Saccharomyces cerevisiae / Q000201:enzymology; D031995:Saxifragaceae / Q000737:chemistry*; D013329:Structure-Activity Relationship; D000520:alpha-Glucosidases / Q000378:metabolism
chemical_list: D001578:Benzopyrans; D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D000520:alpha-Glucosidases; C006741:bergenin