Design, Synthesis and Structure-Activity Relationship Optimization of Lycorine Derivatives for HCV Inhibition
Chen,Duozhi; Cai,Jieyun; Cheng,Junjun; Jing,Chenxu; Yin,Junlin; Jiang,Jiandong; Peng,Zonggen; Hao,Xiaojiang
2015-10-07
Source PublicationSCIENTIFIC REPORTS
Volume5
AbstractLycorine is reported to be a multifunctional compound. We previously showed that lycorine is an HCV inhibitor with strong activity. Further research on the antivirus mechanism indicated that lycorine does not affect the enzymes that are indispensable to HCV replication but suppresses the expression of Hsc70 in the host cell to limit HCV replication. However, due to the cytotoxicity and apoptosis induction of lycorine, lycorine is unsafe to be a anti-HCV agent for clinical application. As a result of increasing interest, its structure was optimized for the first time and a novel series of lycorine derivatives was synthesized, all of which lost their cytotoxicity to different degrees. Structure-activity analysis of these compounds revealed that disubstitution on the free hydroxyl groups at C1 and C2 and/or degradation of the benzodioxole group would markedly reduce the cytotoxicity. Furthermore, an alpha, beta-unsaturated ketone would improve the HCV inhibitory activity of lycorine. The C3-C4 double bond is crucial to the anti-HCV activity because hydrogenation of this double bond clearly weakened HCV inhibition.
DOI10.1038/srep14972
Indexed BySCI
Language英语
WOS IDWOS:000362346700001
Citation statistics
Cited Times:20[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/25173
Collection植物化学与西部植物资源持续利用国家重点实验室
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GB/T 7714
Chen,Duozhi,Cai,Jieyun,Cheng,Junjun,et al. Design, Synthesis and Structure-Activity Relationship Optimization of Lycorine Derivatives for HCV Inhibition[J]. SCIENTIFIC REPORTS,2015,5.
APA Chen,Duozhi.,Cai,Jieyun.,Cheng,Junjun.,Jing,Chenxu.,Yin,Junlin.,...&Hao,Xiaojiang.(2015).Design, Synthesis and Structure-Activity Relationship Optimization of Lycorine Derivatives for HCV Inhibition.SCIENTIFIC REPORTS,5.
MLA Chen,Duozhi,et al."Design, Synthesis and Structure-Activity Relationship Optimization of Lycorine Derivatives for HCV Inhibition".SCIENTIFIC REPORTS 5(2015).
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