Parvez Mohammad K, Al-Dosari Mohammed S, Abdelwahid Mazin A S, Alqahtani Ali S, Alanzi Abdullah R
Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Department of Organic Chemistry, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Miyagi 980-8577, Japan.
Exp Ther Med. 2022 Jun;23(6):398. doi: 10.3892/etm.2022.11325. Epub 2022 Apr 15.
Bioactive natural or phytoproducts have emerged as a potential source of antiviral agents. Of the spp., and have been reported for their antiviral activities against hepatitis B virus (HBV), while the anti-HBV efficacy of has remained elusive. In the present study, the anti-HBV activities of -derived novel catechin [3,5,13,14-flavantetrol-catechin or rhuspartin (RPT)] and epicatechin-3--rhamnoside (ECR), were assessed using the HBV-reporter cell line HepG2.2.15. RPT and ECR proved to efficiently inhibit HBV surface antigen (HBsAg) synthesis by 68.8 and 71.3%, respectively, and HBV pre-core antigen (HBeAg) production by 62.3 and 71.2%, respectively, after 5 days of treatment. Of note, RPT had a lower anti-HBV activity than ECR. In comparison, the reference drug lamivudine (LAM) inhibited HBsAg and HBeAg expression by 83.6 and 85.4%, respectively. Further molecular docking analysis revealed formations of strong complexes of RPT, ECR and LAM with HBV polymerase through interactions with binding pocket residues. Taken together, the present results demonstrated promising therapeutic potential of the novel -derived catechin and epicatechin for HBV, warranting their further molecular and pharmacological evaluation.
生物活性天然产物或植物产物已成为抗病毒药物的潜在来源。在这些物种中，[物种名称1]、[物种名称2]和[物种名称3]已被报道具有抗乙型肝炎病毒（HBV）的活性，而[物种名称4]的抗HBV疗效仍不明确。在本研究中，使用HBV报告细胞系HepG2.2.15评估了[物种名称5]衍生的新型儿茶素[3,5,13,14 - 黄烷四醇 - 儿茶素或盐肤木素（RPT）]和表儿茶素 - 3 - O - 鼠李糖苷（ECR）的抗HBV活性。经5天治疗后，RPT和ECR分别有效抑制HBV表面抗原（HBsAg）合成68.8%和71.3%，以及HBV前核心抗原（HBeAg）产生62.3%和71.2%。值得注意的是，RPT的抗HBV活性低于ECR。相比之下，参考药物拉米夫定（LAM）分别抑制HBsAg和HBeAg表达83.6%和85.4%。进一步的分子对接分析表明，RPT、ECR和LAM通过与结合口袋残基相互作用，与HBV聚合酶形成了强复合物。综上所述，本研究结果表明新型[物种名称5]衍生的儿茶素和表儿茶素对HBV具有良好的治疗潜力，值得进一步进行分子和药理学评估。
