论文标题:Flavonoids from Pterogyne nitens Inhibit Hepatitis C Virus Entry
期刊:
作者:Jacqueline Farinha Shimizu, Caroline Sprengel Lima, Carina Machado Pereira, Cintia Bittar, Mariana Nogueira Batista, Ana Carolina Nazaré, Carlos Roberto Polaquini, Carsten Zothner, Mark Harris, Paula Rahal, Luis Octávio Regasini, Ana Carolina Gomes Jardim
发表时间:2017/11/23
数字识别码:10.1038/s41598-017-16336-y
原文链接:
丙型肝炎病毒(HCV-Hepatitis C virus)是全球肝病和肝移植的主要原因之一。现有的丙肝治疗法是基于干扰素-α,利巴韦林,以及直接作用的抗病毒药物,比如NS3蛋白酶和NS5B聚合酶抑制剂。但这些疗法药物设计价格昂贵,有强烈的副作用,而且展现出了HCV抗药性,所以开发新的疗法已是势在必行。
在《明升体育app手机版》发表的一篇名为Flavonoids from Pterogyne nitens Inhibit Hepatitis C Virus Entry的文章里,来自巴西圣保罗省大学Ana Carolina Gomes Jardim的团队研究了来自南美洲的一种树木——Pterogyne nitens——的黄酮类化合物sorbifolin (黄酮类化合物1)和 pedalitin(黄酮类化合物2)的抗丙肝病毒的性质,尤其是它们对HCV复制周期的影响。作者利用基因型2a JFH-1亚基因组复制子和感染性病毒系统研究了这两种化合物的抗HCV性质,结果显示,化合物1和2在非细胞毒性浓度下分别可以抑制45.0%和78.7%的病毒入侵。化合物2的起效机制是直接作用于病毒颗粒,并且干扰宿主细胞,而化合物1的机制仅限于病毒灭活。此外,用这些黄酮化合物处理过的细胞并未发现对HCV的复制和释放有抑制作用。此研究是首次探讨了这两种黄酮化合物在体外的抗丙型肝炎病毒的情况。
图1:sorbifolin 和pedalitin能够阻止有效地阻止丙肝病毒进入宿主细胞
摘要:Hepatitis C virus (HCV) is one of the leading causes of liver diseases and transplantation worldwide. The current available therapy for HCV infection is based on interferon-α, ribavirin and the new direct-acting antivirals (DAAs), such as NS3 protease and NS5B polymerase inhibitors. However, the high costs of drug design, severe side effects and HCV resistance presented by the existing treatments demonstrate the need for developing more efficient anti-HCV agents. This study aimed to evaluate the antiviral effects of sorbifolin (1) and pedalitin (2), two flavonoids from Pterogyne nitens on the HCV replication cycle. These compounds were investigated for their anti-HCV activities using genotype 2a JFH-1 subgenomic replicons and infectious virus systems. Flavonoids 1 and 2 inhibited virus entry up to 45.0% and 78.7% respectively at non-cytotoxic concentrations. The mechanism of the flavonoid 2block to virus entry was demonstrated to be by both the direct action on virus particles and the interference on the host cells. Alternatively, the flavonoid 1 activity was restricted to its virucidal effect. Additionally, no inhibitory effects on HCV replication and release were observed by treating cells with these flavonoids. These data are the first description of 1 and 2 possessing in vitro anti-HCV activity.
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(来源:明升手机版(明升官网))
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