Isolation, synthesis and anti-hepatitis B virus evaluation of p-hydroxyacetophenone derivatives from Artemisia capillaris
Zhao, Yong; Geng, Chang-An; Chen, Hao; Ma, Yun-Bao; Huang, Xiao-Yan; Cao, Tuan-Wu; He, Kang; Wang, Hao; Zhang, Xue-Mei; Chen, Ji-Jun; Chen,JJ (reprint author),Chinese Acad Sci,Kunming Inst Bot,State Key Lab Phytochem & Plant Resources West Ch,Kunming 650201,Peoples R China.; chenjj@mail.kib.ac.cn
2015-04-01
发表期刊BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷号25期号:7页码:1509-1514
摘要p-Hydroxyacetophenone (p-HAP), as a main hepatoprotective and choleretic constituent of Artemisia capillaris, was revealed with anti-hepatitis B virus (HBV) effects in recent investigation. In addition to p-HAP, four derivatives of p-HAP were also isolated from Artemisia capillaris by various chromatographic methods. Subsequent structural modification on p-HAP and its glycoside led to the synthesis of 28 additional derivatives, of which 13 compounds showed activity inhibiting hepatitis B surface antigen (HBsAg) secretion; and 18 compounds possessed inhibition on HBV DNA replication. The primary structure-activity relationships (SARs) suggested that the conjugated derivatives of p-HAP glycoside and substituted cinnamic acids (2a-2i) obviously enhanced the activity against HBV DNA replication with IC50 values ranged from 5.8 to 74.4 mu M. (C) 2015 Elsevier Ltd. All rights reserved.
关键词Artemisia Capillaris P-hydroxyacetophenone Derivatives Anti-hbv Activity Structure-activity Relationships
资助信息National Natural Science Foundation of China [81202436]; National Science Foundation of China for Distinguished Young Scholars [81025023]; Youth Innovation Promotion Association, CAS
学科领域Chemistry, Medicinal ; Chemistry, Organic
DOI10.1016/j.bmcl.2015.02.024
收录类别SCI
语种英语
WOS研究方向Pharmacology & Pharmacy ; Chemistry
WOS类目Chemistry, Medicinal ; Chemistry, Organic
WOS记录号WOS:000351688700029
引用统计
被引频次:7[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/20626
专题植物化学与西部植物资源持续利用国家重点实验室
通讯作者Chen,JJ (reprint author),Chinese Acad Sci,Kunming Inst Bot,State Key Lab Phytochem & Plant Resources West Ch,Kunming 650201,Peoples R China.; chenjj@mail.kib.ac.cn
作者单位Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Peoples R China
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Zhao, Yong,Geng, Chang-An,Chen, Hao,et al. Isolation, synthesis and anti-hepatitis B virus evaluation of p-hydroxyacetophenone derivatives from Artemisia capillaris[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2015,25(7):1509-1514.
APA Zhao, Yong.,Geng, Chang-An.,Chen, Hao.,Ma, Yun-Bao.,Huang, Xiao-Yan.,...&chenjj@mail.kib.ac.cn.(2015).Isolation, synthesis and anti-hepatitis B virus evaluation of p-hydroxyacetophenone derivatives from Artemisia capillaris.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,25(7),1509-1514.
MLA Zhao, Yong,et al."Isolation, synthesis and anti-hepatitis B virus evaluation of p-hydroxyacetophenone derivatives from Artemisia capillaris".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 25.7(2015):1509-1514.
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