Xanthones from Swertia mussotii as Multitarget-Directed Antidiabetic Agents

NWIPB OpenIR

	Xanthones from Swertia mussotii as Multitarget-Directed Antidiabetic Agents
	Zheng, Huan-Huan ; Luo, Cui-Ting ; Chen, Heru ; Lin, Juan-Na ; Ye, Chun-Ling ; Mao, Shuang-Shuang ; Li, Yu-Lin
	2014-07-01
发表期刊	CHEMMEDCHEM ; Zheng, HH; Luo, CT; Chen, HR; Lin, JN; Ye, CL; Mao, SS; Li, YL.Xanthones from Swertia mussotii as Multitarget-Directed Antidiabetic Agents,CHEMMEDCHEM,2014,9(7):1374
摘要	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 alpha-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-(beta-D-glucoside) (12) were confirmed as good antioxidants and alpha-glucosidase inhibitors. Xanthone 7 was also confirmed as a potent inhibitor of aldose reductase (ALR2). Xanthone 7 was the most active alpha-glucosidase and ALR2 inhibitor, with IC50 values of 5.2 +/- 0.3 mu m and 88.6 +/- 1.6 nm, 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.; 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 alpha-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-(beta-D-glucoside) (12) were confirmed as good antioxidants and alpha-glucosidase inhibitors. Xanthone 7 was also confirmed as a potent inhibitor of aldose reductase (ALR2). Xanthone 7 was the most active alpha-glucosidase and ALR2 inhibitor, with IC50 values of 5.2 +/- 0.3 mu m and 88.6 +/- 1.6 nm, 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.
文献类型	期刊论文
条目标识符	http://210.75.249.4/handle/363003/16983
专题	中国科学院西北高原生物研究所
推荐引用方式 GB/T 7714	Zheng, Huan-Huan,Luo, Cui-Ting,Chen, Heru,et al. Xanthones from Swertia mussotii as Multitarget-Directed Antidiabetic Agents[J]. CHEMMEDCHEM, Zheng, HH; Luo, CT; Chen, HR; Lin, JN; Ye, CL; Mao, SS; Li, YL.Xanthones from Swertia mussotii as Multitarget-Directed Antidiabetic Agents,CHEMMEDCHEM,2014,9(7):1374,2014.
APA	Zheng, Huan-Huan.,Luo, Cui-Ting.,Chen, Heru.,Lin, Juan-Na.,Ye, Chun-Ling.,...&Li, Yu-Lin.(2014).Xanthones from Swertia mussotii as Multitarget-Directed Antidiabetic Agents.CHEMMEDCHEM.
MLA	Zheng, Huan-Huan,et al."Xanthones from Swertia mussotii as Multitarget-Directed Antidiabetic Agents".CHEMMEDCHEM (2014).