| 16-nor Limonoids from Harrisonia perforata as promising selective 11 beta-HSD1 inhibitors | |
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; Hao, Xiao-Jiang1
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| 2016-11-11 | |
| Source Publication | SCIENTIFIC REPORTS
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| Volume | 6Pages:1 |
| Abstract | 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. |
| DOI | 10.1038/srep36927 |
| Indexed By | SCI |
| Language | 英语 |
| WOS ID | WOS:000387474000001 |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://ir.kib.ac.cn/handle/151853/33667 |
| Collection | 植物化学与西部植物资源持续利用国家重点实验室 |
| Affiliation | 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 |
| Recommended Citation 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,2016,6:1. |
| 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,6,1. |
| MLA | Xiao-HuiYan,et al."16-nor Limonoids from Harrisonia perforata as promising selective 11 beta-HSD1 inhibitors".SCIENTIFIC REPORTS 6(2016):1. |
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| 20.pdf（1151KB） | 期刊论文 | 作者接受稿 | 开放获取 | CC BY-NC-SA | View Download | |
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