Knowledge Management System of Northwest Institute of Plateau Biology, CAS
Xanthones from Swertia mussotii as Multitarget-Directed Antidiabetic Agents | |
Zheng, Huan-Huan1; Luo, Cui-Ting1; Chen, Heru1,2,3; Lin, Juan-Na4; Ye, Chun-Ling4; Mao, Shuang-Shuang1; Li, Yu-Lin5 | |
2014-07-01 | |
发表期刊 | CHEMMEDCHEM
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ISSN | 1860-7179 |
卷号 | 9期号:7页码:1374-1377 |
文章类型 | Article |
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. |
关键词 | Aldose Reductases Antioxidants Diabetes Alpha-glucosidases Multitarget Inhibitors Xanthones |
WOS标题词 | Science & Technology ; Life Sciences & Biomedicine |
关键词[WOS] | DESIGNED MULTIPLE LIGANDS ; DIABETIC-RATS ; HYPOGLYCEMIC ACTIVITY ; ALDOSE REDUCTASE ; MANGIFERIN ; INHIBITORS ; CELLS |
收录类别 | SCI |
语种 | 英语 |
WOS研究方向 | Pharmacology & Pharmacy |
WOS类目 | Chemistry, Medicinal ; Pharmacology & Pharmacy |
WOS记录号 | WOS:000338991100005 |
引用统计 | |
文献类型 | 期刊论文 |
条目标识符 | http://210.75.249.4/handle/363003/4215 |
专题 | 中国科学院西北高原生物研究所 |
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. |
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