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
2016-11-11
Source PublicationSCIENTIFIC REPORTS
Volume6Pages:1
AbstractTwo 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.
DOI10.1038/srep36927
Indexed BySCI
Language英语
WOS Research AreaScience & Technology - Other Topics
WOS SubjectMultidisciplinary Sciences
WOS IDWOS:000387474000001
Citation statistics
Cited Times:3[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://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
Affiliation1.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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