Xanthones from Swertia mussotii as Multitarget-Directed Antidiabetic Agents
文献类型：期刊论文
| 作者 | Zheng, Huan-Huan1; Luo, Cui-Ting1; Chen, Heru1,2,3; Lin, Juan-Na4; Ye, Chun-Ling4; Mao, Shuang-Shuang1; Li, Yu-Lin5 |
| 刊名 | chemmedchem
 |
| 出版日期 | 2014-07-01 |
| 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 |
| 中文摘要 | 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. |
| 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. |
| WOS标题词 | science & technology ; life sciences & biomedicine |
| 类目[WOS] | chemistry, medicinal ; pharmacology & pharmacy |
| 研究领域[WOS] | pharmacology & pharmacy |
| 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记录号 | WOS:000338991100005 |
| 公开日期 | 2014-12-19 |
| 源URL | [http://ir.nwipb.ac.cn/handle/363003/4215]  |
| 专题 | 西北高原生物研究所_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. |
入库方式： OAI收割
来源：西北高原生物研究所
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