Evaluation of anti-HCV activity and SAR study of (+)-lycoricidine through targeting of host heat-stress cognate 70 (Hsc70)
Chen, Duo-Zhi1,2,3,4; Jiang, Jian-Dong5; Zhang, Ke-Qing3,4; He, Hong-Ping1; Di, Ying-Tong1; Zhang, Yu1; Cai, Jie-Yun1,2; Wang, Lei1,2; Li, Shun-Lin1; Yi, Ping6
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
2013-05-01
卷号23期号:9页码:2679-2682
关键词(+)-Lycoricidine Heat-stress cognate 70 (Hsc70) Down-regulators Structure-activity relationship (SAR) Anti-HCV activity
ISSN号0960-894X
通讯作者Peng, ZG (reprint author), Chinese Acad Med Sci, Peking Union Med Coll, Lab Antiviral Res, Inst Med Biotechnol, Beijing 100050, Peoples R China. ; pumcpzg@126.com ; haoxj@mail.kib.ac.cn
英文摘要The anti hepatitis C virus (HCV) activity of (+)-lycoricidine (1) was evaluated for the first time in this letter, yielding an EC50 value of 0.55 nmol/mL and an selection index (SI) value of 12.72. Further studies indicated that 1 induced this effect by down-regulating host heat-stress cognate 70 (Hsc70) expression. In addition, 20 derivatives were designed and synthesised to investigate the basic structure-activity relationship (SAR) of the title compound. Several of these derivatives exhibit a good inhibition of HCV, such as compound 3 (EC50 = 0.68 nmol/mL, SI = 33.86), compound 2d (EC50 = 15 nmol/mL, SI = 12) and compound 5 (EC50 = 33 nmol/mL, SI > 10.91). Meanwhile, the experimental data suggest that the modification of certain groups of (+)-lycoricidine can reduce the cytotoxicity of the compounds. (C) 2013 Elsevier Ltd. All rights reserved.
学科主题Pharmacology & Pharmacy; Chemistry
WOS标题词Science & Technology ; Life Sciences & Biomedicine ; Physical Sciences
类目[WOS]Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]Pharmacology & Pharmacy ; Chemistry
关键词[WOS]HEPATITIS-C-VIRUS ; CHEMICAL-CONSTITUENTS ; AMARYLLIDACEAE ; RNA ; 7-DEOXY-TRANS-DIHYDRONARCICLASINE ; PROTEIN ; AGENTS
收录类别SCI ; IC
资助信息National Natural Science Foundation of China [30830114, 31270404]; Ministry of Science and Technology [2009CB522300]
语种英语
WOS记录号WOS:000317333900040
公开日期2013-06-08
内容类型期刊论文
源URL[http://ir.kib.ac.cn/handle/151853/16417]  
专题昆明植物研究所_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 West Ch, Kunming Inst Bot, Kunming 650201, Yunnan, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100039, Peoples R China
3.Yunnan Univ, Lab Conservat & Utilizat Bioresources, Minist Educ, Kunming 650091, Yunnan, Peoples R China
4.Yunnan Univ, Key Lab Microbial Div Southwest China, Minist Educ, Kunming 650091, Yunnan, Peoples R China
5.Chinese Acad Med Sci, Peking Union Med Coll, Lab Antiviral Res, Inst Med Biotechnol, Beijing 100050, Peoples R China
6.Honghe Univ, Sch Sci, Key Lab Nat Pharmaceut & Chem Biol Yunnan Prov, Mengzi 661100, Peoples R China
推荐引用方式
GB/T 7714
Chen, Duo-Zhi,Jiang, Jian-Dong,Zhang, Ke-Qing,et al. Evaluation of anti-HCV activity and SAR study of (+)-lycoricidine through targeting of host heat-stress cognate 70 (Hsc70)[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2013,23(9):2679-2682.
APA Chen, Duo-Zhi.,Jiang, Jian-Dong.,Zhang, Ke-Qing.,He, Hong-Ping.,Di, Ying-Tong.,...&Hao, Xiao-Jiang.(2013).Evaluation of anti-HCV activity and SAR study of (+)-lycoricidine through targeting of host heat-stress cognate 70 (Hsc70).BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,23(9),2679-2682.
MLA Chen, Duo-Zhi,et al."Evaluation of anti-HCV activity and SAR study of (+)-lycoricidine through targeting of host heat-stress cognate 70 (Hsc70)".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 23.9(2013):2679-2682.
个性服务
查看访问统计
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。


©版权所有 ©2017 CSpace - Powered by CSpace