Li Ruibo, Narita Ryo, Ouda Ryota, Kimura Chihiro, Nishimura Hiroshi, Yatagai Mitsuyoshi, Fujita Takashi, Watanabe Takashi
Research Institute for Sustainable Humanosphere, Kyoto University Uji Kyoto 611-0011 Japan
Institute for Frontier Life and Medical Science, Kyoto University Kyoto 606-8507 Japan.
RSC Adv. 2018 Oct 22;8(63):35888-35896. doi: 10.1039/c8ra07096b.
The pyrolysis product, wood vinegar (WV), from Japanese larch exhibited strong antiviral activity against the encephalomycarditis virus (EMCV). Catechol, 3-methyl-, 4-methyl-, 4-ethyl-, and 3-methoxycatechol, and 2-methyl-1,4-benzenediol were identified as the major antiviral compounds. The viral inhibition ability of these compounds was affected by the structure and position of the substituent group attached to the aromatic skeleton. The IC of catechol was 0.67 mg mL and those of its derivatives were <0.40 mg mL. Methyl and ethyl substitution in the para position relative to a hydroxyl group obviously increased the antiviral activities. The mode of antiviral action was investigated by adding catechol derivatives at different times of the viral life cycle. It was found that direct inactivations of EMCV by these compounds were the major pathway for the antiviral activity. The effect of catechol derivatives on the host immune system was studied by quantification of Il6 and Ifnb1 expression levels. Increased Il6 expression levels indicate NF-κB activation by reactive oxygen species from auto-oxidations of catechol derivatives, which is also a possible antiviral route. The present research provides indices for production of potent antiviral agents form lignocellulose biomass.
日本落叶松热解产物木醋液（WV）对脑心肌炎病毒（EMCV）表现出强大的抗病毒活性。邻苯二酚、3 - 甲基邻苯二酚、4 - 甲基邻苯二酚、4 - 乙基邻苯二酚、3 - 甲氧基邻苯二酚和2 - 甲基 - 1,4 - 苯二酚被鉴定为主要的抗病毒化合物。这些化合物的病毒抑制能力受连接在芳香骨架上取代基的结构和位置影响。邻苯二酚的半数抑制浓度（IC）为0.67 mg/mL，其衍生物的IC小于0.40 mg/mL。相对于羟基在对位进行甲基和乙基取代明显增强了抗病毒活性。通过在病毒生命周期的不同时间添加邻苯二酚衍生物来研究抗病毒作用模式。发现这些化合物对EMCV的直接灭活是抗病毒活性的主要途径。通过定量白细胞介素6（Il6）和干扰素β1（Ifnb1）表达水平来研究邻苯二酚衍生物对宿主免疫系统的影响。Il6表达水平升高表明邻苯二酚衍生物自氧化产生的活性氧激活了核因子κB（NF - κB），这也是一种可能的抗病毒途径。本研究为从木质纤维素生物质生产强效抗病毒剂提供了指标。
