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学科主题: 药学
题名:
Synthesis and Anti- HCV Entry Activity Studies of bCyclodextrin- Pentacyclic Triterpene Conjugates
作者: Xiao, Sulong1; Wang, Qi1,3; Si, Longlong1; Shi, Yongying1; Wang, Han1; Yu, Fei1; Zhang, Yongmin2; Li, Yingbo1; Zheng, Yongxiang1; Zhang, Chuanling1; Wang, Chunguang1; Zhang, Lihe1; Zhou, Demin1
关键词: antiviral agents ; click chemistry ; echinocystic acid ; HCV entry inhibitors ; pentacyclic triterpenes ; cyclodextrins
刊名: CHEMMEDCHEM
发表日期: 2014-05-01
DOI: 10.1002/cmdc.201300545
卷: 9, 期:5, 页:1060-1070
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal ; Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: BETULINIC ACID ; HIV ACTIVITY ; CRATAEGUS-SINAICA ; OLEANOLIC ACID ; MORONIC ACID ; AIDS AGENTS ; CYCLODEXTRINS ; DERIVATIVES ; VIRUS ; INHIBITORS
英文摘要:

In our previous studies, oleanolic acid (OA) and echinocystic acid (EA), isolated from Dipsacus asperoides, were found to have anti-HCV entry properties. The major issue for members of this type of triterpene is their low water solubility. In this study, a series of new water-soluble triazole-bridged -cyclodextrin (CD)-pentacyclic triterpene conjugates were synthesized via click chemistry. Thanks to the attached -CD moiety, all synthesized conjugates showed lower hydrophobicity (AlogP) than their parent compounds. Several conjugates exhibited moderate anti-HCV entry activity. With the exception of per-O-methylated -CD-pentacyclic triterpene conjugates, all other conjugates showed no cytotoxicity based on an alamarBlue assay carried out with HeLa, HepG2, MDCK, and 293T cells. More interestingly, the hemolytic activity of these conjugates disappeared upon the introduction of -CDs. Easy access to such conjugates that combine the properties of -CD and pentacyclic triterpenes may provide a way to obtain a new class of anti-HCV entry inhibitors.

语种: 英语
所属项目编号: 2010CB12304 ; 81101239 ; 20932001 ; 81361168002 ; 81373271
项目资助者: National Basic Research Program of China (973 Program) ; National Natural Science Foundation of China
WOS记录号: WOS:000335001700021
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/54410
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Univ Paris 06, Univ Sorbonne, CNRS, LabEx Michem,UMR 8232,IPCM, F-75005 Paris, France
3.Peking Univ, Sch Pharmaceut Sci, Dept Mol & Cellular Pharmacol, Beijing 100191, Peoples R China

Recommended Citation:
Xiao, Sulong,Wang, Qi,Si, Longlong,et al. Synthesis and Anti- HCV Entry Activity Studies of bCyclodextrin- Pentacyclic Triterpene Conjugates[J]. CHEMMEDCHEM,2014,9(5):1060-1070.
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