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从叶下珠中分离得到的木脂素尼拉汀的抗乙型肝炎病毒的体内外活性。

In vitro and in vivo anti-hepatitis B virus activities of the lignan niranthin isolated from Phyllanthus niruri L.

机构信息

Department of Chemistry, Guangxi University, Nanning 530004, PR China.

Department of Chemistry, Guangxi University, Nanning 530004, PR China.

出版信息

J Ethnopharmacol. 2014 Sep 11;155(2):1061-7. doi: 10.1016/j.jep.2014.05.064. Epub 2014 Jul 4.

DOI:10.1016/j.jep.2014.05.064
PMID:25009077
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Niranthin is a lignan isolated from Phyllanthus niruri L. This plant has long been used in folk medicine for liver protection and antihepatitis B in many Asian countries. This study was designed to evaluate the anti-hepatitis B virus activity of niranthin using HepG2.2.15 cells and duck hepatitis B virus (DHBV) infected ducks as in vitro and in vivo models.

MATERIALS AND METHODS

Niranthin was isolated from Phyllanthus niruri L. (Euphorbiaceae) by extraction and chromatographic procedures and the anti-hepatitis B virus activity was evaluated both in vitro and in vivo. The human HBV-transfected liver cell line HepG2.2.15 was used in vitro assay. And the in vivo anti-hepatitis B virus activity was evaluated on the expression of HBV replication, HBsAg, HBeAg, ALT and AST on day 0, 7, 14, 17 after niranthin was dosed intragastricly (i.g.) once a day for 14 days at the dosages of 25, 50 and 100 mg/kg/day in the duck hepatitis B virus (DHBV) infected ducks.

RESULTS

In the human HBV-transfected liver cell line HepG2.2.15, the secretion of HBsAg and HBeAg were significantly decreased after treatment with niranthin for 144 h, with IC50 values for HBsAg of 15.6 µM, IC50 values for HBeAg of 25.1 µM. In DHBV-infected ducklings, niranthin significantly reduced the serum DHBV DNA, HBsAg, HBeAg, ALT and AST. Furthermore, analysis of the liver pathological changes confirmed the hepatoprotective effect of niranthin.

CONCLUSION

The experimental data demonstrated that niranthin exhibits anti-hepatitis B virus activity both in vitro and in vivo.

摘要

民族药理学相关性

尼兰汀是从叶下珠(Phyllanthus niruri L.)中分离得到的木脂素。这种植物在许多亚洲国家长期以来一直被民间医学用于肝脏保护和抗乙型肝炎。本研究旨在使用 HepG2.2.15 细胞和鸭乙型肝炎病毒(DHBV)感染的鸭子作为体外和体内模型来评估尼兰汀的抗乙型肝炎病毒活性。

材料和方法

尼兰汀从叶下珠(Phyllanthus niruri L.)(大戟科)中通过提取和色谱程序分离,并在体外和体内进行抗乙型肝炎病毒活性评估。人乙型肝炎病毒转染的肝细胞系 HepG2.2.15 用于体外测定。体内抗乙型肝炎病毒活性在第 0、7、14、17 天,尼兰汀每天一次经口灌胃给药 14 天后,通过 DHBV 感染鸭 HBV 复制、HBsAg、HBeAg、ALT 和 AST 的表达进行评估,剂量为 25、50 和 100mg/kg/天。

结果

在人乙型肝炎病毒转染的肝细胞系 HepG2.2.15 中,尼兰汀处理 144 小时后 HBsAg 和 HBeAg 的分泌明显减少,HBsAg 的 IC50 值为 15.6µM,HBeAg 的 IC50 值为 25.1µM。在 DHBV 感染的小鸭中,尼兰汀显著降低了血清 DHBV DNA、HBsAg、HBeAg、ALT 和 AST。此外,肝组织病理学变化分析证实了尼兰汀的保肝作用。

结论

实验数据表明,尼兰汀在体外和体内均具有抗乙型肝炎病毒活性。

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