Three new anti-HBV active constituents from the traditional Chinese herb of Yin-Chen (Artemisia scoparia)
Three new anti-HBV active constituents from the traditional Chinese herb of Yin-Chen (Artemisia scoparia)
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传统中药茵陈中的三种新的抗乙型肝炎活性成分
DOI：
10.1016/j.jep.2015.10.032
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发表时间：
2015-12-24
影响因子：
5.4
通讯作者：
Chen, Ji-Jun
中科院分区：
文献类型：
--
作者：
Geng, Chang-An;Huang, Xiao-Yan;Chen, Ji-Jun
民族药理学相关性：茵陈是中国治疗急慢性肝炎的著名中药。中国药典收载茵陈的道地药材有滨蒿和茵陈蒿。前期研究证明，绿原酸类似物和酚酸类是黄芪抗乙型肝炎病毒活性成分的两种主要类型。毛细血管。然而，目前还没有关于A.研究目的：本研究的目的是识别A. scoparia的新的抗HBV成分。材料和方法：LCMS和生物测定指导的分离，对A. Scoparia导致分离出三种新化合物。通过详细的光谱分析确定了它们的结构。采用体外抗HBV实验方法，对HepG 2.2.15细胞株进行HBsAg、HBeAg分泌抑制和HBV DNA复制抑制实验。首次发现Scoparia具有抗HBV活性，并通过柱层析将其进一步分离成多个组分。其中D-4抗HBV活性最高，经LCMS分析鉴定，从中分离得到3个新化合物，包括1个4-吡啶酮糖苷（1）和2个聚乙炔糖苷（2-3）。化合物1-3显示出抗HBsAg和HBeAg分泌和HBV DNA复制的活性。特别地，化合物2和3抑制HBV DNA复制，IC 50值分别为0.07 +/- 0.04和0.012 +/- 0.05 mM，SI值分别为23.6和17.1。在MS/MS实验的基础上，提出了化合物1在正负离子模式下的裂解途径，以及化合物2和3在负离子模式下的裂解途径。离子对388-208（阳性）和432-206（阴性）代表1，离子对503-341（阴性）代表2，离子对503-203（阴性）代表3，可以被认为是各自的诊断离子。结论：首次对A.从茵陈中分离得到3个新的活性成分，为进一步了解茵陈的民族药理学作用以及茵陈与黄芪的化学差异提供了有价值的信息。毛细血管。(c)2015爱思唯尔爱尔兰有限公司版权所有。
Ethnopharmacological relevance: Yin-Chen is a famous traditional Chinese medicine (TCM) in China for the treatment of acute and chronic hepatitis. Two species, namely Artemisia scoparia and Artemisia capillaris, are documented in Chinese Pharmacopoeia as the authentic resources for Yin-Chen. Previous investigation has proved that chlorogenic acid analogs and phenolic acids are two main types of the anti-HBV active constituents of A. capillaris. However, there is no investigation concerned with the anti-HBV components of A. scoparia.Aim of the study: The aim of the present study is to recognize the new anti-HBV constituents of A. scoparia by detailed LCMS analyses.Materials and methods: LCMS and bioassay-guided fractionation on the active part of A. scoparia led to the isolation of three new compounds. Their structures were determined by detailed spectroscopic analyses. Anti-HBV assay involving inhibition on HBsAg and HBeAg secretions and HBV DNA replication were performed in virto on HepG 2.2.15 cell line.Results: The 90% ethanol extract of A. scoparia was revealed with anti-HBV activity for the first time, which was further separated into several fractions by column chromatography. Fr. D-4 was revealed with the highest anti-HBV activity, from which three new compounds including one unusual 4-pyridone glucoside (1) and two polyacetylene glucosides (2-3) were isolated under the guidance of LCMS analyses. Compounds 1-3 exhibited activity against the secretions of HBsAg and HBeAg, and HBV DNA replication. In particular, compounds 2 and 3 inhibited HBV DNA replication with IC50 values of 0.07 +/- 0.04 and 0.012 +/- 0.05 mM, with SI values of 23.6 and 17.1, respectively. Based on the MS/MS experiment, the fragmentation pathways of 1 in both positive and negative modes, and 2 and 3 in negative mode were proposed. The ion pairs of 388-208 (positive) and 432-206 (negative) for 1, 503-341 (negative) for 2, and 503-203 (negative) for 3, could be recognized as their respective diagnostic ions.Conclusions: The first time investigation on the anti-HBV constituents of A. scoparia yielded three new active compounds, which will provide valuable information for understanding the ethnopharmacological usage of Yin-Chen, as well as the chemical difference with A. capillaris. (c) 2015 Elsevier Ireland Ltd. All rights reserved.