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
发表期刊EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN0223-5234
卷号41期号:11页码:1247-1252
摘要Cathepsin 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.
关键词Biflavones Inhibitors Cathepsin b Cathepsin k Docking
学科领域Chemistry ; Medicinal
DOI10.1016/j.ejmech.2006.06.002
收录类别SCI
语种英语
WOS研究方向Pharmacology & Pharmacy
WOS类目Chemistry, Medicinal
WOS记录号WOS:000242454100003
引用统计
被引频次:20[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/2149
专题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, 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
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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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