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Anti-hepatitis B virus effects of the traditional Chinese herb Arteinisia capillaris and its active enynes
Geng, Chang-An1; Yang, Tong-Hua1; Huang, Xiao-Yan1; Yang, Jing1; Ma, Yun-Bao1; Li, Tian-Ze1; Zhang, Xue-Mei1; Chen, Ji-Jun1,2
2018-10-05
发表期刊JOURNAL OF ETHNOPHARMACOLOGY
ISSN0378-8741
卷号224页码:283-289
摘要Ethnopharmacological relevance: Artemisia capillaris (Yin-Chen) is a famous traditional Chinese medicine (TCM) for treating acute and chronic hepatitis in China. Enynes are one type of characteristic constituents in this herb, while their anti-hepatitis B virus (anti-HBV) properties have not been systemically investigated. Aim of the study: This study is to reveal the active part of A. capillaris, and systemically investigate the enynes and their anti-HBV activity. Materials and methods: The total extract and each fraction of A. capillaris were assayed for the anti-HBV activity to reveal the active part. Bioassay-guided fractionation using various chromatographic techniques yielded the enynes, whose structures were elucidated by spectroscopic analyses and ECD calculations. The anti-HBV properties inhibiting HBsAg and HBeAg secretions and HBV DNA replication were evaluated on HepG 2.2.15 cell line in vitro. Results: ACT-2 and ACT-3 was revealed to be the respective active and toxic part of A. capillaris. Twelve enynes (1-12) involving four new ones (1-4) and two unusual enyne analogs (13-14) were isolated from the active part (ACT-2). All the isolates were assayed for their anti-HBV activity, and the preliminary structure-activity relationships were summarized based on the structural features. In particular, compound 4 could significantly inhibit the secretions of HBsAg and HBeAg, and HBV DNA replication with IC50 values of 197.2 (SI > 5.1), 48.7 (SI > 20.5) and 9.8 (SI > 102) mu M. Conclusions: Enynes are responsible for the anti-HBV effects of A. capillaris. Hydroxyl and glycosyl groups are preferable for maintaining activity. This is the first time to systematically investigate the anti-HBV activity of enynes in A. capillaris, which provides valuable information for understanding the ethnopharmacological application of Yin-Chen.
关键词Artemisia capillaris Enynes Anti-HBV activity Structure-activity relationships
资助信息CAS "Light of West China" Program (Western Youth Scholars "A"); Youth Innovation Promotion Association CAS; National Natural Science Foundation of China; Program of Yunling Scholarship; Applied Basic Research Programs of Yunnan Province
语种英语
资助项目CAS "Light of West China" Program (Western Youth Scholars "A") ; Youth Innovation Promotion Association CAS ; National Natural Science Foundation of China[81202436] ; Program of Yunling Scholarship ; Applied Basic Research Programs of Yunnan Province[2017FB137]
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文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/62140
专题中国科学院昆明植物研究所
植物化学与西部植物资源持续利用国家重点实验室
通讯作者Chen, Ji-Jun
作者单位1.Chinese Acad Sci, Kunming Inst Bot, Yunnan Key Lab Nat Med Chem, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
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Geng, Chang-An,Yang, Tong-Hua,Huang, Xiao-Yan,et al. Anti-hepatitis B virus effects of the traditional Chinese herb Arteinisia capillaris and its active enynes[J]. JOURNAL OF ETHNOPHARMACOLOGY,2018,224:283-289.
APA Geng, Chang-An.,Yang, Tong-Hua.,Huang, Xiao-Yan.,Yang, Jing.,Ma, Yun-Bao.,...&Chen, Ji-Jun.(2018).Anti-hepatitis B virus effects of the traditional Chinese herb Arteinisia capillaris and its active enynes.JOURNAL OF ETHNOPHARMACOLOGY,224,283-289.
MLA Geng, Chang-An,et al."Anti-hepatitis B virus effects of the traditional Chinese herb Arteinisia capillaris and its active enynes".JOURNAL OF ETHNOPHARMACOLOGY 224(2018):283-289.
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