Genomics Study Laboratory, São Paulo State University, IBILCE, S. José do Rio Preto, SP, Brazil.
Laboratory of Virology, Institute of Biomedical Science, ICBIM, Federal University of Uberlândia, Uberlândia, MG, Brazil.
Sci Rep. 2017 Nov 23;7(1):16127. doi: 10.1038/s41598-017-16336-y.
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 2 block 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.
丙型肝炎病毒(HCV)是全球导致肝脏疾病和移植的主要原因之一。目前 HCV 感染的治疗方法基于干扰素-α、利巴韦林和新的直接作用抗病毒药物(DAAs),如 NS3 蛋白酶和 NS5B 聚合酶抑制剂。然而,现有治疗方法存在药物设计成本高、严重副作用和 HCV 耐药性等问题,这表明需要开发更有效的抗 HCV 药物。本研究旨在评估从 Pterogyne nitens 中分离得到的两种黄酮类化合物(1)和(2)对 HCV 复制周期的抗病毒作用。使用基因型 2a JFH-1 亚基因组复制子和感染性病毒系统研究了这些化合物的抗 HCV 活性。在非细胞毒性浓度下,黄酮类化合物 1 和 2 分别抑制病毒进入达 45.0%和 78.7%。黄酮类化合物 2 抑制病毒进入的机制被证明是通过直接作用于病毒颗粒和干扰宿主细胞两种方式。相反,黄酮类化合物 1 的活性仅限于其杀病毒作用。此外,用这些黄酮类化合物处理细胞时,未观察到对 HCV 复制和释放的抑制作用。这些数据首次描述了 1 和 2 具有体外抗 HCV 活性。