title: Analogues of xanthones--Chalcones and bis-chalcones as α-glucosidase inhibitors and anti-diabetes candidates.
abstract: Two series of compounds (chalcones and bis-chalcones) were designed, synthesized, and evaluated as α-glucosidase inhibitors (AGIs) with 1-deoxynojirimycin as positive control in vitro. Most of the compounds with two or four hydroxyl groups showed better inhibitory activities than 1-deoxynojirimycin towards α-glucosidase with noncompetitive mechanism. Moreover, most of the hydroxy bis-chalcones exhibit good α-glucosidase inhibitory activities in enzyme test. Inspiringly, bis-chalcones 2g (at 1 μM concentration) has stronger effect than 1-deoxynojirimycin on reducing the glucose level in HepG-2 cells (human liver cancer cell line).
authors.affiliation: School of Chemistry, Sun Yat-sen University, 135 Xingang West Road, Guangzhou, 510275, PR China.
authors.forename: Chao-Yun
authors.initials: CY
authors.lastname: Cai
authors.affiliation: School of Chemistry, Sun Yat-sen University, 135 Xingang West Road, Guangzhou, 510275, PR China.
authors.forename: Li
authors.initials: L
authors.lastname: Rao
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510080, PR China.
authors.forename: Yong
authors.initials: Y
authors.lastname: Rao
authors.affiliation: School of Chemistry, Sun Yat-sen University, 135 Xingang West Road, Guangzhou, 510275, PR China.
authors.forename: Jin-Xuan
authors.initials: JX
authors.lastname: Guo
authors.affiliation: School of Chemistry, Sun Yat-sen University, 135 Xingang West Road, Guangzhou, 510275, PR China.
authors.forename: Zhi-Zun
authors.initials: ZZ
authors.lastname: Xiao
authors.affiliation: School of Chemistry, Sun Yat-sen University, 135 Xingang West Road, Guangzhou, 510275, PR China.
authors.forename: Jing-Yu
authors.initials: JY
authors.lastname: Cao
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510080, PR China.
authors.forename: Zhi-Shu
authors.initials: ZS
authors.lastname: Huang
authors.affiliation: School of Chemistry, Sun Yat-sen University, 135 Xingang West Road, Guangzhou, 510275, PR China. Electronic address: ceswb@mail.sysu.edu.cn.
authors.forename: Bo
authors.initials: B
authors.lastname: Wang
mesh_terms: D047188:Chalcones / Q000737:chemistry* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D056945:Hep G2 Cells; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D044004:Xanthones / Q000737:chemistry; D000520:alpha-Glucosidases / Q000187:drug effects*
chemical_list: D047188:Chalcones; D004791:Enzyme Inhibitors; D007004:Hypoglycemic Agents; D044004:Xanthones; D000520:alpha-Glucosidases
keywords: Bis-chalcones; Chalcones; Noncompetitive; α-glucosidase inhibitors