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
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
2015-04-01
卷号25期号:7页码:1509-1514
关键词Artemisia capillaris p-Hydroxyacetophenone derivatives Anti-HBV activity Structure-activity relationships
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
英文摘要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.
学科主题Chemistry, Medicinal; Chemistry, Organic
类目[WOS]Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]Pharmacology & Pharmacy ; Chemistry
关键词[WOS]ANTIVIRAL ACTIVITY ; CONSTITUENTS ; INHIBITORS ; ANALOGS ; THUNB ; ACID
收录类别SCI
语种英语
WOS记录号WOS:000351688700029
内容类型期刊论文
源URL[http://ir.kib.ac.cn/handle/151853/20626]  
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.,...&Chen, Ji-Jun.(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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