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Anti-hepatitis B virus effects of the traditional Chinese herb Arteinisia capillaris and its active enynes

Authors Geng, Chang-An; Yang, Tong-Hua; Huang, Xiao-Yan; Yang, Jing; Ma, Yun-Bao; Li, Tian-Ze; Zhang, Xue-Mei; Chen, Ji-Jun

Journal JOURNAL OF ETHNOPHARMACOLOGY , OCT 5 2018,:224

DOI 10.1016/j.jep.2018.06.005 PubMed 29890315

Abstract 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.

Species covered 茵陈蒿 Artemisia capillaris