抗病毒类黄酮和多酚驱动的新型抗乙肝病毒疗效 。（原文句子不完整，翻译可能会存在一定局限性）
Antiviral flavonoids- and polyphenols-driven novel anti-HBV efficacy of .
作者信息
Niyazi Sakina, Parvez Mohammad K, Ahmed Tanzeel, Basudan Omar A, Rehman Md Tabish, Al-Dosari Mohammed S, Herqash Rashed N, Alqasoumi Saleh I
机构信息
School of Biotechnology, IFTM University, Moradabad, India.
Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
出版信息
Arch Med Sci. 2024 Jun 6;21(3):919-929. doi: 10.5114/aoms/188809. eCollection 2025.
INTRODUCTION
Antiviral natural products have shown great promise as alternatives to conventional therapies to address drug resistance in hepatitis B virus (HBV). The abundance of bioactive flavonoids and polyphenolic contents in leaves of (yerba mate) warrants assessment of its anti-HBV activity.
MATERIAL AND METHODS
The total ethanol extract of leaves (IP-Ext), including its -hexane (IP-Hex), chloroform (IP-Chl), ethyl acetate (IP-EtAc) and ethanol (IP-EtOH) fractions, was tested for non-hepatocytotoxicity on HepG2 cells (MTT assay) and anti-HBV efficacy on HepG2.2.15 cells (ELISA). Further, quantitative high-performance liquid chromatography (HPLC) was employed to identify the antiviral compounds in the extract. In addition, molecular docking was performed to delineate the possible mechanism of anti-HBV activity of the identified compounds.
RESULTS
All samples showed non-cytotoxicity except IP-EtAc, with mild toxicity at 200 μg/ml. Their anti-HBV assessment showed dose-dependent inhibitions of HBV antigens (HBsAg and HBeAg). At the selected optimal dose (50 μg/ml), while IP-Ext showed mild (HBsAg: 24.2% and HBeAg: 20.6%) and IP-Chl showed moderate (HBsAg: 42.3% and 40.1%) activity, IP-Hex (HBsAg: 55.6% and HBeAg: 52.4%) and IP-EtOH (HBsAg: 53.2% and HBeAg: 50.2%) exhibited high activity. HPLC revealed known anti-HBV flavonoids (rutin: 18.98, quercetin: 6.52 and kaempferol: 9.10 μg/g) and polyphenols (caffeic acid: 11.43 and chlorogenic acid: 3.22 μg/g) in the extract. Their (10 μg/ml, each) anti-HBV activities were: quercetin (HBsAg: 67.8% and HBeAg: 64.4%), kaempferol (HBsAg: 63.5% and HBeAg: 61.6%), chlorogenic acid (HBsAg: 55.2% and HBeAg: 53.8%), rutin (HBsAg: 51.2% and HBeAg: 48.4%) and caffeic acid (HBsAg: 42.2% and HBeAg: 39.5%). Notably, while our previous molecular docking had shown strong interactions of these flavonoids with HBV polymerase, here, we observed good binding affinity of the polyphenols with both drug-sensitive (wild-type) and drug-resistant (mutant) polymerases.
CONCLUSIONS
This is the first study suggesting the anti-HBV therapeutic efficacy of attributed to its antiviral flavonoids and polyphenols.
引言
抗病毒天然产物作为传统疗法的替代方案，在应对乙型肝炎病毒（HBV）耐药性方面展现出巨大潜力。巴拉圭茶树叶中丰富的生物活性黄酮类化合物和多酚类成分值得对其抗HBV活性进行评估。
材料与方法
测试了巴拉圭茶树叶的总乙醇提取物（IP-Ext）及其正己烷（IP-Hex）、氯仿（IP-Chl）、乙酸乙酯（IP-EtAc）和乙醇（IP-EtOH）馏分对HepG2细胞的非肝细胞毒性（MTT法）以及对HepG2.2.15细胞的抗HBV功效（ELISA法）。此外，采用定量高效液相色谱（HPLC）鉴定提取物中的抗病毒化合物。另外，进行了分子对接以阐明所鉴定化合物抗HBV活性的可能机制。
结果
除IP-EtAc外，所有样品均显示无细胞毒性，IP-EtAc在200μg/ml时具有轻度毒性。它们的抗HBV评估显示对HBV抗原（HBsAg和HBeAg）有剂量依赖性抑制作用。在选定的最佳剂量（50μg/ml）下，IP-Ext显示出轻度活性（HBsAg：24.2%，HBeAg：20.6%），IP-Chl显示出中度活性（HBsAg：42.3%，HBeAg：40.1%），而IP-Hex（HBsAg：55.6%，HBeAg：52.4%）和IP-EtOH（HBsAg：53.2%，HBeAg：50.2%）表现出高活性。HPLC显示提取物中含有已知的抗HBV黄酮类化合物（芦丁：18.98、槲皮素：6.52、山奈酚：9.10μg/g）和多酚类化合物（咖啡酸：11.43、绿原酸：3.22μg/g）。它们（各10μg/ml）的抗HBV活性分别为：槲皮素（HBsAg：67.8%，HBeAg：64.4%）、山奈酚（HBsAg：63.5%，HBeAg：61.6%）、绿原酸（HBsAg：55.2%，HBeAg：53.8%）、芦丁（HBsAg：51.2%，HBeAg：48.4%）和咖啡酸（HBsAg：42.2%，HBeAg：39.5%）。值得注意的是，虽然我们之前的分子对接显示这些黄酮类化合物与HBV聚合酶有强烈相互作用，但在此我们观察到多酚类化合物与药物敏感（野生型）和耐药（突变型）聚合酶均具有良好的结合亲和力。
结论
这是第一项表明巴拉圭茶因其抗病毒黄酮类化合物和多酚类化合物而具有抗HBV治疗功效的研究。
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