Design and Synthesis of Novel Arctigenin Analogues for the Amelioration of Metabolic Disorders
文献类型：期刊论文
| 作者 | Duan, Shudong1; Huang, Suling1 ; Gong, Jian1; Shen, Yu1; Zeng, Limin1; Feng, Ying1; Ren, Wenming1; Leng, Ying1; Hu, Youhong1,2
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| 刊名 | ACS MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2015-04 |
| 卷号 | 6期号:4页码:386-391 |
| 关键词 | Natural product arctigenin analogues 2-deoxyglucose uptake in L6 myotubes amelioration of metabolic disorders |
| ISSN号 | 1948-5875 |
| DOI | 10.1021/acsmedchemlett.5b00007 |
| 文献子类 | Article |
| 英文摘要 | Analogues of the natural product (-)-arctigenin, an activator of adenosine monophosphate activated protein kinase, were prepared in order to evaluate their effects on 2-deoxyglucose uptake in L6 myotubes and possible use in ameliorating metabolic disorders. Racemic arctigenin 2a was found to display a similar uptake enhancement as does (-)-arctigenin. As a result, the SAR study was conducted utilizing racemic compounds. The structure-activity relationship study led to the discovery of key substitution patterns on the lactone motif that govern 2-deoxyglucose uptake activities. The results show that replacement of the para-hydroxyl group of the C-2 benzyl moiety of arctigenin by Cl has a pronounced effect on uptake activity. Specifically, analogue 2p, which contains the p-Cl substituent, stimulates glucose uptake and fatty acid oxidation in L6 myotubes. |
| WOS关键词 | ACTIVATED PROTEIN-KINASE ; INSULIN-RESISTANCE ; SKELETAL-MUSCLE ; AMPK ; GLUCOSE ; MICE ; LIGNAN |
| 资助项目 | Major Projects in National Science and Technology, "Creation of major new drugs"[2102ZX09103101-062] ; National Nature Science Foundation of China[81202570] ; National Nature Science Foundation of China[81225022] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000353098300004 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276582]  |
| 专题 | 药理学第一研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物化学研究室 |
| 通讯作者 | Hu, Youhong |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Zhejiang Univ, Coll Pharmaceut Sci, ZJU ENS Joint Lab Med Chem, Zhejiang Prov Key Lab Anticanc Drug Res, Hangzhou 310058, Zhejiang, Peoples R China |
| 推荐引用方式 GB/T 7714 | Duan, Shudong,Huang, Suling,Gong, Jian,et al. Design and Synthesis of Novel Arctigenin Analogues for the Amelioration of Metabolic Disorders[J]. ACS MEDICINAL CHEMISTRY LETTERS,2015,6(4):386-391. |
| APA | Duan, Shudong.,Huang, Suling.,Gong, Jian.,Shen, Yu.,Zeng, Limin.,...&Hu, Youhong.(2015).Design and Synthesis of Novel Arctigenin Analogues for the Amelioration of Metabolic Disorders.ACS MEDICINAL CHEMISTRY LETTERS,6(4),386-391. |
| MLA | Duan, Shudong,et al."Design and Synthesis of Novel Arctigenin Analogues for the Amelioration of Metabolic Disorders".ACS MEDICINAL CHEMISTRY LETTERS 6.4(2015):386-391. |
入库方式： OAI收割
来源：上海药物研究所
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