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. |
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