Isolation, synthesis and anti-hepatitis B virus evaluation of p-hydroxyacetophenone derivatives from Artemisia capillaris

doi:10.1016/j.bmcl.2015.02.024

	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
学科领域	Chemistry, Medicinal ; Chemistry, Organic
DOI	10.1016/j.bmcl.2015.02.024
收录类别	SCI
语种	英语
WOS记录号	WOS:000351688700029
引用统计
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
推荐引用方式 GB/T 7714	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.

条目包含的文件		下载所有文件
文件名称/大小	文献类型	版本类型	开放类型	使用许可
Zhao-2015-Isolation,（2494KB）			开放获取	CC BY-NC-ND	浏览下载