Natural biflavones as novel inhibitors of cathepsin B and K
Zeng, G. -Z.; Pan, X. -L.; Tan, N. -H.; Xiong, J.; Zhang, Y. M.
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
Indexed BySCI
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
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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