Ide Kazuke, Kawasaki Yohei, Kawakami Koji, Yamada Hiroshi
Department of Pharmacoepidemiology, Graduate School of Medicine and Public Health, Kyoto University, Yoshida Konoe-cho, Sakyo-ku, Kyoto 606-8501, Japan.
Curr Med Chem. 2016;23(42):4773-4783. doi: 10.2174/0929867324666161123091010.
Influenza infection and associated epidemics represent a serious public health problem. Several preventive and curative measures exist against its spread including vaccination and therapeutic agents such as neuraminidase inhibitors (e.g., oseltamivir, zanamivir, as well as peramivir and laninamivir, which are licensed in several countries) and adamantanes (e.g., amantadine and rimantadine). However, neuraminidase inhibitor- and adamantane- resistant viruses have been detected, whereas vaccines exhibit strain-specific effects and are limited in supply. Thus, new approaches are needed to prevent and treat influenza infections. Catechins, a class of polyphenolic flavonoids present in tea leaves, have been reported as potential anti-influenza virus agents based on experimental and clinical studies. (-)-epigallocatechin gallate (EGCG), a major and highly bioactive catechin, is known to inhibit influenza A and B virus infections in Madin-Darby canine kidney cells. Additionally, EGCG and other catechin compounds such as epicatechin gallate and catechin-5-gallate also show neuraminidase inhibitory activities as demonstrated via molecular docking. These catechins can bind differently to neuraminidase and might overcome known drug resistancerelated virus mutations. Furthermore, the antiviral effects of chemically modified catechin derivatives have also been investigated, and future structure-based drug design studies of catechin derivatives might contribute to improvements in influenza prevention and treatment. This review briefly summarizes probable mechanisms underlying the inhibitory effects of tea catechins against influenza infection and their clinical benefits on influenza prevention and treatment. Additionally, the great potential of tea catechins and their chemical derivatives as effective antiviral agents is described.
流感感染及相关疫情是一个严重的公共卫生问题。针对其传播存在多种预防和治疗措施，包括接种疫苗以及使用治疗药物，如神经氨酸酶抑制剂（如奥司他韦、扎那米韦，还有在多个国家获批的帕拉米韦和拉尼米韦）和金刚烷类药物（如金刚烷胺和金刚乙胺）。然而，已检测到对神经氨酸酶抑制剂和金刚烷类药物耐药的病毒，而疫苗具有毒株特异性效应且供应有限。因此，需要新的方法来预防和治疗流感感染。基于实验和临床研究，儿茶素（茶叶中存在的一类多酚类黄酮）已被报道为潜在的抗流感病毒药物。（-）-表没食子儿茶素没食子酸酯（EGCG）是一种主要且具有高生物活性的儿茶素，已知其能抑制甲型和乙型流感病毒在马-达二氏犬肾细胞中的感染。此外，EGCG和其他儿茶素化合物，如表儿茶素没食子酸酯和儿茶素-5-没食子酸酯，通过分子对接也显示出神经氨酸酶抑制活性。这些儿茶素与神经氨酸酶的结合方式不同，可能克服已知的与耐药相关的病毒突变。此外，还研究了化学修饰的儿茶素衍生物的抗病毒作用，未来基于结构的儿茶素衍生物药物设计研究可能有助于改进流感的预防和治疗。这篇综述简要总结了茶儿茶素对流感感染抑制作用的潜在机制及其在流感预防和治疗方面的临床益处。此外，还描述了茶儿茶素及其化学衍生物作为有效抗病毒药物的巨大潜力。
