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首页> 外文期刊>Journal of Ethnopharmacology: An Interdisciplinary Journal Devoted to Bioscientific Research on Indigenous Drugs >UFLC/MS-IT-TOF guided isolation of anti-HBV active chlorogenic add analogues from Artemisia capillaris as a traditional Chinese herb for the treatment of hepatitis
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UFLC/MS-IT-TOF guided isolation of anti-HBV active chlorogenic add analogues from Artemisia capillaris as a traditional Chinese herb for the treatment of hepatitis

机译：UFLC / MS-IT-TOF指导从毛蒿蒿中提取抗乙肝病毒活性绿原添加类似物作为传统中草药治疗肝炎

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摘要

Ethnopharmacological relevance: Hepatitis B induced by HBV is a serious health problem. Artemisia capillaris (Yin-Chen) has long been used to treat hepatitis in traditional Chinese medicine. Coumarins, flavonoids and organic acids were revealed as its hepatoprotective and choleretic components, but its anti-HBV active components remain unknown. This current study focused on its anti-HBV active constituents by various chromatographic methods.Material and methods: LC/MS and bioassay-guided fractionation on the active extract of Artemisia capillaris led to the isolation of nine chlorogenic acid analogues. Structures of the isolates were elucidated by MS/MS and NMR techniques. Anti-HBV assay was performed on HepG 2.2.15 cell line in vitro: reduction of HBsAg and HBeAg secretions was measured by an ELISA method; inhibition of HBV DNA replication was monitored by real-time quantitative PCR and cellular toxicity was assessed by a MTT method.Results: The 90% ethanol extract of Artemisia capillaris (Fr. AC) showed significantly inhibitory activity on HBV DNA replication with an IC50 value of 76.1 + 3.9 ng/mL and low cytotoxic effects (SI > 20.1). To clarify its active constituents, the extract was further separated into 3 sub-fractions (AC-1, AC-2 and AC-3), of which Fr. AC-2 was the most active fraction against HBeAg secretion and HBV DNA replication with IC50 values of 44.2 + 2.8 and 23.2 ± 1.9 ng/mL Nine chlorogenic acid analogues were detected from the active part (Fr. AC-2) by a LC/MS technique and further separated by a HPLC method. The isolates were determined as chlorogenic acid (1), cryptochlorogenic acid (2), neochlorogenic acid (3), 3,5-dicaffeoyl-quinic acid (4), 4,5-dicaffeoylquinic acid (5), 3,4-dicaffeoylquinic acid (6), chlorogenic acid methyl ester (7), cryptochlorogenic acid methyl ester (8), neochlorogenic acid methyl ester (9). Compounds 1-6 possessed potent activity against HBV DNA replication with IC50 values in the range of 5.5 + 0.9-13.7 ± 1.3 nM. Di-caffeoyl analogues (4-6) also exhibited activity against the secretions of HBsAg and HBeAg. Esterified analogues (7-9) showed dramatically decreased anti-HBV activity, indicating that carboxyl group is closely associated to the anti-HBV activity.Conclusions: This investigation was focused on the active fractions of Artemisia capillaris and their active compositions, which showed that Fr. AC-2 was the main active section of Artemisia capillaris and chlorogenic acid analogues were the main constituents contributing to its anti-HBV activity. These results support the ethnooharmacological use of Artemisia capillaris as anti-HBV agents.
机译：人类药理学意义：HBV诱发的乙型肝炎是一个严重的健康问题。长期以来，中草药一直使用艾蒿（Yin-Chen）治疗肝炎。香豆素，类黄酮和有机酸被认为具有保肝和利胆作用，但其抗乙肝病毒活性成分仍然未知。本研究主要通过各种色谱方法研究其抗HBV活性成分。材料和方法：对毛细蒿的活性提取物进行LC / MS和生物测定指导的分馏，分离出9种绿原酸类似物。通过MS / MS和NMR技术阐明了分离物的结构。在体外对HepG 2.2.15细胞系进行抗HBV检测：通过ELISA方法检测HBsAg和HBeAg分泌的减少;通过实时定量PCR监测HBV DNA复制的抑制作用，并通过MTT方法评估细胞毒性。结果：茵陈蒿（Fr.AC）的90％乙醇提取物对HBV DNA复制具有明显的抑制活性，IC50值76.1 + 3.9 ng / mL的细胞毒性和低细胞毒性作用（SI> 20.1）。为了弄清其活性成分，将提取物进一步分为3个亚组分（AC-1，AC-2和AC-3），其中Fr。 AC-2是对抗HBeAg分泌和HBV DNA复制最活跃的组分，IC50值为44.2 + 2.8和23.2±1.9 ng / mL，通过LC / LC从活性部分（AC-2组分）中检测到9种绿原酸类似物。 MS技术，并通过HPLC方法进一步分离。分离物确定为绿原酸（1），隐绿原酸（2），新绿原酸（3），3,5-二咖啡酰奎尼酸（4），4,5-二咖啡酰奎尼酸（5），3,4-二咖啡酰奎尼酸酸（6），绿原酸甲酯（7），隐绿原酸甲酯（8），新绿原酸甲酯（9）。化合物1-6具有有效的抗HBV DNA复制的活性，IC50值为5.5 + 0.9-13.7±1.3 nM。二咖啡酰类似物（4-6）还表现出抗HBsAg和HBeAg分泌的活性。酯化的类似物（7-9）显示出明显降低的抗HBV活性，表明羧基与抗HBV活性密切相关。结论：本研究集中于艾蒿的活性级分及其活性成分，表明神父AC-2是毛蒿的主要活性部分，绿原酸类似物是有助于其抗HBV活性的主要成分。这些结果支持了艾蒿作为抗乙肝病毒药物的民族药理学应用。

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