瓜蒌提取物的植物化学特征及其对丙型肝炎病毒的活性

T. Wahyuni, Lydia Tumewu, A. A. Permanasari, C. Utsubo, A. Widyawaruyanti, A. Hafid
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摘要

丙型肝炎病毒(HCV)是一种 RNA 病毒,容易发生变异,抗药性风险很高。丙型肝炎病毒的疫苗尚未问世,目前的治疗费用也非常昂贵。为了提供植物抗病毒的替代性和互补性,本研究评估了瓜蒌(P. betle)对 HCV 的活性及其与现有抗病毒药物利巴韦林(Ribavirin)和西美普韦(Simeprevir)的组合。通过使用 Huh7it-1 细胞和 JFH1a HCV 进行体外培养,确定了其抗病毒抑制作用。此外,还通过薄层色谱法(TLC)和高效液相色谱法(HPLC)测定了植物化学成分。结果表明,槟榔的乙醇提取物具有很强的活性,其 IC50 值为 0.08 ± 0.028 µg/mL。作用机制显示,槟榔乙醇提取物主要抑制后进入步骤。此外,槟榔提取物与西美瑞韦(simeprevir)合用可提高其抗 HCV 活性,但与利巴韦林合用则没有效果。Western 印迹分析表明,槟榔提取物对 NS3 蛋白水平的抑制呈剂量依赖性。植物化学评估显示,提取物中含有黄酮类、多酚类和生物碱。这些结果表明,槟榔的乙醇提取物可能是开发抗HCV药物或替代药物的良好候选物。关键词:丙型肝炎病毒丙型肝炎病毒 瓜蒌 药用植物 西美瑞韦 利巴韦林 药物
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The Phytochemistry profile of Piper betle extract and its Activity Against Hepatitis C Virus
Hepatitis C virus (HCV) is an RNA virus that is easy to mutate and high risk of resistance. The vaccine for HCV has not been provided yet, and the current treatment is very expensive. To provide alternative and complementary antiviral from plants, this study evaluated the activities of Piper betle (P. betle) against HCV and its combination with existing antiviral drugs, Ribavirin and Simeprevir. The antiviral inhibition was identified by in vitro culture using Huh7it-1 cells and JFH1a HCV. Moreover, the phytochemistry profile was also determined by Thin Layer Chromatography (TLC) and High-Performance Liquid Chromatography (HPLC). The result showed that the ethanol extract of P. betle was possess strong activity with an IC50 value of 0.08 ± 0.028 µg/mL. The mechanism of action revealed the extract dominantly inhibit in the post-entry steps. Furthermore, the combination of P. betle extract with simeprevir increased its anti-HCV activity, however, no effect was observed in the combination with ribavirin. The Western blotting analysis was shown inhibition of NS3 protein levels in a dose-dependent manner. Phytochemistry evaluation was shown for the extract containing flavonoids, polyphenols, and alkaloids. These results suggested that the ethanolic extract of P. betle could be a good candidate for the development or an alternative to anti-HCV drugs. Keywords: Hepatitis C Virus, Piper betle, Medicinal plants, Simeprevir, Ribavirin, Medicine.
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