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; Peng, Zong-Gen5; Hao, Xiao-Jiang1
2013-05-01
发表期刊BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
卷号23期号:9页码:2679-2682
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.
关键词(+)-lycoricidine Heat-stress Cognate 70 (Hsc70) Down-regulators Structure-activity Relationship (Sar) Anti-hcv Activity
资助信息National Natural Science Foundation of China [30830114, 31270404]; Ministry of Science and Technology [2009CB522300]
收录类别SCI ; IC
语种英语
引用统计
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/16417
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 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
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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.
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