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Xanthones from Swertia mussotii as Multitarget‐Directed Antidiabetic Agents
Author(s) -
Zheng HuanHuan,
Luo CuiTing,
Chen Heru,
Lin JuanNa,
Ye ChunLing,
Mao ShuangShuang,
Li YuLin
Publication year - 2014
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201300507
Subject(s) - xanthone , aldose reductase , chemistry , antioxidant , pharmacology , diabetes mellitus , glucoside , aldose reductase inhibitor , oxidative stress , traditional medicine , biochemistry , medicine , stereochemistry , enzyme , endocrinology , pathology , alternative medicine
Oxidative stress has been suggested to play a causative role in the development of obesity‐induced insulin resistance and type 2 diabetes. Given the antioxidant potency of previously reported xanthones isolated from Swertia mussotii . These natural products were further evaluated against other targets in diabetes, aldose reductase and α‐glucosidase, in order to identify novel multitarget‐directed antidiabetic agents. Among the 14 xanthones screened, 1,3,7,8‐tetrahydroxyxanthone ( 6 ), 1,3,5,8‐tetrahydroxyxanthone ( 7 ), and 2,3,6,8‐tetrahydroxyxanthone‐7C‐(β‐ D ‐glucoside) ( 12 ) were confirmed as good antioxidants and α‐glucosidase inhibitors. Xanthone 7 was also confirmed as a potent inhibitor of aldose reductase (ALR2). Xanthone 7 was the most active α‐glucosidase and ALR2 inhibitor, with IC 50 values of 5.2±0.3 μ M and 88.6±1.6 n M , respectively, while compound 12 was shown to be the most active antioxidant. Given the overall profile, xanthone 7 is considered to be the most promising multitarget antidiabetic agent, and may have potential for the treatment of both diabetes and diabetic complications.