IR@PKUHSC  > 北京大学药学院  > 药物化学系
学科主题药学
Synthesis and Anti- HCV Entry Activity Studies of bCyclodextrin- Pentacyclic Triterpene Conjugates
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
2014-05-01
DOI10.1002/cmdc.201300545
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
WOS记录号WOS:000335001700021
项目编号2010CB12304 ; 81101239 ; 20932001 ; 81361168002 ; 81373271
资助机构National Basic Research Program of China (973 Program) ; National Natural Science Foundation of China
引用统计
被引频次:18[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/54410
专题北京大学药学院_药物化学系
北京大学药学院
北京大学药学院_天然药物与仿生药物国家重点实验室
北京大学药学院_药学院
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
推荐引用方式
GB/T 7714
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.
APA Xiao, Sulong.,Wang, Qi.,Si, Longlong.,Shi, Yongying.,Wang, Han.,...&Zhou, Demin.(2014).Synthesis and Anti- HCV Entry Activity Studies of bCyclodextrin- Pentacyclic Triterpene Conjugates.CHEMMEDCHEM,9(5),1060-1070.
MLA Xiao, Sulong,et al."Synthesis and Anti- HCV Entry Activity Studies of bCyclodextrin- Pentacyclic Triterpene Conjugates".CHEMMEDCHEM 9.5(2014):1060-1070.
条目包含的文件
条目无相关文件。
个性服务
推荐该条目
保存到收藏夹
查看访问统计
导出为Endnote文件
谷歌学术
谷歌学术中相似的文章
[Xiao, Sulong]的文章
[Wang, Qi]的文章
[Si, Longlong]的文章
百度学术
百度学术中相似的文章
[Xiao, Sulong]的文章
[Wang, Qi]的文章
[Si, Longlong]的文章
必应学术
必应学术中相似的文章
[Xiao, Sulong]的文章
[Wang, Qi]的文章
[Si, Longlong]的文章
相关权益政策
暂无数据
收藏/分享
所有评论 (0)
暂无评论
 

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。