Natural biflavones as novel inhibitors of cathepsin B and K
Zeng, G. -Z.; Pan, X. -L.; Tan, N. -H.; Xiong, J.; Zhang, Y. M.
2006-11-01
Source PublicationEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN0223-5234
Volume41Issue:11Pages:1247-1252
AbstractCathepsin B and K, two important members in lysosomal proteases, involve in many serious human diseases, such as tumor and osteoporosis. In order to find their novel inhibitors, we performed the inhibition assays of cathepsin B and cathepsin K in vitro, randomly screened compounds from plants, and found six biflavones, named AMF1-5 and HIF, can potently inhibit cathepsin B and cathepsin K, especially AMF4 and HIF with IC50 of 0.62 and 0.58 W against cathepsin B. They are novel inhibitors for cathepsin B and K. Inhibition and flexible docking studies indicated that these biflavones are reversible inhibitors of cathepsin B, and their binding patterns and interaction modes with cathepsin B made them more specific to cathepsin B endopeptidase. (c) 2006 Elsevier Masson SAS. All rights reserved.
KeywordBiflavones Inhibitors Cathepsin b Cathepsin k Docking
Subject AreaChemistry ; Medicinal
DOI10.1016/j.ejmech.2006.06.002
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000242454100003
Citation statistics
Cited Times:20[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/2149
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, State Key Lab Phytochem & Plant Resources W China, Kunming Inst Bot, Kunming 650204, Peoples R China
2.Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China
Recommended Citation
GB/T 7714
Zeng, G. -Z.,Pan, X. -L.,Tan, N. -H.,et al. Natural biflavones as novel inhibitors of cathepsin B and K[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2006,41(11):1247-1252.
APA Zeng, G. -Z.,Pan, X. -L.,Tan, N. -H.,Xiong, J.,&Zhang, Y. M..(2006).Natural biflavones as novel inhibitors of cathepsin B and K.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,41(11),1247-1252.
MLA Zeng, G. -Z.,et al."Natural biflavones as novel inhibitors of cathepsin B and K".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 41.11(2006):1247-1252.
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