Bavachinin analogues as agonists of pan-peroxisome proliferator-activated receptors
文献类型：期刊论文
| 作者 | Yi, Jingyu1,4; Du, Guoxin1; Zhao, Yuanyuan1; Zhang, Liuqiang1; Li, Bo2,3; Zhu, Weiliang2,3 ; Huang, Cheng1; Li, Yiming1; Guo, Fujiang1
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| 刊名 | MEDICINAL CHEMISTRY RESEARCH
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| 出版日期 | 2018-07 |
| 卷号 | 27期号:7页码:1851-1862 |
| 关键词 | Bavachinin Metabolic syndrome PPARs Reporter gene assaysThese authors contributed equally: Jingyu Yi, Guoxin Du |
| ISSN号 | 1054-2523 |
| DOI | 10.1007/s00044-018-2197-6 |
| 文献子类 | Article |
| 英文摘要 | Peroxisome proliferator-activated receptors (PPARs) agonists contribute to the regulation of glucose, lipid, and cholesterol metabolism and have emerged as key targets to treat metabolic syndrome. In our previous study, the natural compound bavachinin was found to have pan-PPAR agonist activity. In this study, five isoflavones, three isoflavanones, and five scaffold-hopping analogues of bavachinin were designed, synthesised, and evaluated through reporter gene assays for pan-PPAR agonist activity. The analogue 2-(4-hydroxyphenyl)-6-isopentenyl-7-methoxy-2,3-dihydroquinolin-4(1H)-one (21) was identified as a pan-PPAR agonist, exhibiting substantially higher PPAR alpha/beta agonist activity and equal PPAR-gamma agonist activity than does bavachinin. |
| WOS关键词 | METABOLIC SYNDROME ; NATURAL-PRODUCTS ; PPAR-GAMMA ; DERIVATIVES ; MODULATORS ; DESIGN ; POTENT ; ALPHA |
| 资助项目 | Excellent Academic Leaders Program of Shanghai[16XD1403500] ; Shanghai Science and Technology Committee funding[16401902000] ; program of Shanghai E-Research Institute of Bioactive Constituents in Traditional Chinese Medicine[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000435946100011 |
| 出版者 | SPRINGER BIRKHAUSER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279689]  |
| 专题 | 天然药物化学研究室 药物发现与设计中心 |
| 通讯作者 | Li, Yiming; Guo, Fujiang |
| 作者单位 | 1.Shanghai Univ Tradit Chinese Med, Sch Pharm, 1200 Cailun Rd, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Key Lab Receptor Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 4.Zhejiang Hosp, Dept Pharm, 12 Lingyin Rd, Hangzhou 310013, Zhejiang, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Yi, Jingyu,Du, Guoxin,Zhao, Yuanyuan,et al. Bavachinin analogues as agonists of pan-peroxisome proliferator-activated receptors[J]. MEDICINAL CHEMISTRY RESEARCH,2018,27(7):1851-1862. |
| APA | Yi, Jingyu.,Du, Guoxin.,Zhao, Yuanyuan.,Zhang, Liuqiang.,Li, Bo.,...&Guo, Fujiang.(2018).Bavachinin analogues as agonists of pan-peroxisome proliferator-activated receptors.MEDICINAL CHEMISTRY RESEARCH,27(7),1851-1862. |
| MLA | Yi, Jingyu,et al."Bavachinin analogues as agonists of pan-peroxisome proliferator-activated receptors".MEDICINAL CHEMISTRY RESEARCH 27.7(2018):1851-1862. |
入库方式： OAI收割
来源：上海药物研究所
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