植物黃酮可用來抵禦丙型肝炎病毒入侵

論文標題：Flavonoids from Pterogyne nitens Inhibit Hepatitis C Virus Entry

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

數字識別碼：10.1038/s41598-017-16336-y

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。現有的丙肝治療法是基於干擾素-α，利巴韋林，以及直接作用的抗病毒藥物，比如NS3蛋白酶和NS5B聚合酶抑製劑。但這些療法藥物設計價格昂貴，有強烈的副作用，而且展現出了HCV抗藥性，所以開發新的療法已是勢在必行。

在《科學報告》發表的一篇名為Flavonoids from Pterogyne nitens Inhibit Hepatitis C Virus Entry的文章里，來自巴西聖保羅省大學Ana Carolina Gomes Jardim的團隊研究了來自南美洲的一種樹木——Pterogyne nitens——的黃酮類化合物sorbifolin （黃酮類化合物1）和 pedalitin（黃酮類化合物2）的抗丙肝病毒的性質，尤其是它們對HCV複製周期的影響。作者利用基因型2a JFH-1亞基因組複製子和感染性病毒系統研究了這兩種化合物的抗HCV性質，結果顯示，化合物1和2在非細胞毒性濃度下分別可以抑制45.0%和78.7%的病毒入侵。化合物2的起效機制是直接作用於病毒顆粒，並且干擾宿主細胞，而化合物1的機制僅限於病毒滅活。此外，用這些黃酮化合物處理過的細胞並未發現對HCV的複製和釋放有抑制作用。此研究是首次探討了這兩種黃酮化合物在體外的抗丙型肝炎病毒的情況。

圖1：sorbifolin 和pedalitin能夠阻止有效地阻止丙肝病毒進入宿主細胞

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.

期刊介紹：Scientific Reports(https://www.nature.com/srep/) is an online, open access journal from the publishers of Nature. We publish scientifically valid primary research from all areas of the natural and clinical sciences.

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