16-nor Limonoids from Harrisonia perforata as promising selective 11 beta-HSD1 inhibitors
文献类型：期刊论文
| 作者 | Xiao-HuiYan1,2; Yi, Ping3,4; Cao, Pei1; Yang, Shi-Ying5,6; Fang, Xin1; Zhang, Yu1 ; Wu, Bin1; Leng, Ying7; Di, Ying-Tong1; Lv, Yang5,6
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| 刊名 | SCIENTIFIC REPORTS
 |
| 出版日期 | 2016-11-11 |
| 卷号 | 6 |
| 英文摘要 | Two new 16-nor limonoids, harperspinoids A and B (1 and 2), with a unique 7/5/5/6/5 ring system, have been isolated from the plant Harrisonia perforate together with a known one, Harperforin G (3). Their structures were elucidated by NMR spectroscopy, X-ray diffraction analysis and computational modelling. Compound 1 exists as polymorphic crystals. Conformations of 1 in solution were further discussed based on the computational results. These compounds exhibited notable inhibitory activity against the 11 beta-HSD1 enzyme. Compound 3 had potencies for the inhibition of human 11 beta-HSD1 with high selectivity against 11 beta-HSD2 (IC50 0.58 mu M, SI > 174). Molecular docking and quantitative structure-activity relationship studies revealed a mixed regulatory mechanism. |
| 类目[WOS] | Multidisciplinary Sciences |
| 研究领域[WOS] | Science & Technology - Other Topics |
| 关键词[WOS] | DEHYDROGENASE TYPE-I ; REARRANGED LIMONOIDS ; CRYSTAL-STRUCTURES ; DISCOVERY ; CHEMISTRY ; CHROMONES ; SKELETON ; TYPE-1 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000387474000001 |
| 源URL | [http://ir.kib.ac.cn/handle/151853/33667]  |
| 专题 | 昆明植物研究所_植物化学与西部植物资源持续利用国家重点实验室 |
| 作者单位 | 1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Peoples R China 2.Southwest Forestry Univ, Coll Forestry, Key Lab Forest Disaster Warning & Control Yunnan, Kunming 650224, Peoples R China 3.Key Lab Chem Nat Prod Guizhou Prov, Guiyang 550002, Peoples R China 4.Chinese Acad Sci, Guiyang 550002, Peoples R China 5.Chinese Acad Med Sci, Inst Mat Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R China 6.Peking Union Med Coll, Beijing 100050, Peoples R China 7.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 200031, Peoples R China |
| 推荐引用方式 GB/T 7714 | Xiao-HuiYan,Yi, Ping,Cao, Pei,et al. 16-nor Limonoids from Harrisonia perforata as promising selective 11 beta-HSD1 inhibitors[J]. SCIENTIFIC REPORTS,2016,6. |
| APA | Xiao-HuiYan.,Yi, Ping.,Cao, Pei.,Yang, Shi-Ying.,Fang, Xin.,...&Hao, Xiao-Jiang.(2016).16-nor Limonoids from Harrisonia perforata as promising selective 11 beta-HSD1 inhibitors.SCIENTIFIC REPORTS,6. |
| MLA | Xiao-HuiYan,et al."16-nor Limonoids from Harrisonia perforata as promising selective 11 beta-HSD1 inhibitors".SCIENTIFIC REPORTS 6(2016). |
入库方式： OAI收割
来源：昆明植物研究所
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