Xanthones from Swertia mussotii as Multitarget-Directed Antidiabetic Agents

doi:10.1002/cmdc.201300507

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	Xanthones from Swertia mussotii as Multitarget-Directed Antidiabetic Agents
	Zheng, Huan-Huan 1; Luo, Cui-Ting 1; Chen, Heru 1,2,3; Lin, Juan-Na 4; Ye, Chun-Ling 4; Mao, Shuang-Shuang 1; Li, Yu-Lin 5
刊名	CHEMMEDCHEM
	2014-07
卷号	9 期号:7 页码:1374-1377
关键词	aldose reductases antioxidants diabetes alpha-glucosidases multitarget inhibitors xanthones
ISSN号	1860-7179
DOI	10.1002/cmdc.201300507
文献子类	Article
英文摘要	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.
资助项目	National Natural Science Foundation of China[81172982] ; Guangdong Provincial Project of Science and Technology[2010A030100006] ; Chinese State Key Laboratory of Drug Research[SIMM1302KF-12]
WOS关键词	DESIGNED MULTIPLE LIGANDS ; DIABETIC-RATS ; HYPOGLYCEMIC ACTIVITY ; ALDOSE REDUCTASE ; MANGIFERIN ; INHIBITORS ; CELLS
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	WILEY-V C H VERLAG GMBH
WOS记录号	WOS:000338991100005
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/277000]
专题	新药研究国家重点实验室中科院受体结构与功能重点实验室
通讯作者	Chen, Heru
作者单位	1.Jinan Univ, Coll Pharm, Inst Tradit Chinese Med & Nat Prod, Guangzhou 510632, Guangdong, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.Guangdong Prov Key Lab Pharmacodynam Constituents, Guangzhou 510632, Guangdong, Peoples R China; 4.Jinan Univ, Coll Pharm, Dept Pharmacol, Guangzhou 510632, Guangdong, Peoples R China; 5.Chinese Acad Sci, Northwest Inst Plateau Biol, Xining 810001, Peoples R China
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,2014,9(7):1374-1377.
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,9(7),1374-1377.
MLA	Zheng, Huan-Huan,et al."Xanthones from Swertia mussotii as Multitarget-Directed Antidiabetic Agents".CHEMMEDCHEM 9.7(2014):1374-1377.