Yasui Ruka, Yoshida Chinatsu, Yamaguchi Toyofumi, Inoue Naoki
Department of Microbiology and Immunology, Gifu Pharmaceutical University, 1-25-4 Daigaku-nishi, Gifu-Shi, Gifu 501-1196, Japan.
Department of Biosciences, Teikyo University of Science, 2-2-1 Senju-Sakuragi, Adachi-ku, Tokyo 120-0045, Japan.
Microbiol Immunol. 2017 Sep;61(9):398-402. doi: 10.1111/1348-0421.12507.
An anti-varicella-zoster virus compound, a 5-chlorobenzo[b]thiophen derivative (45B5), was characterized. Its 50% effective concentration against the cell-free vaccine Oka strain and 50% cytotoxic concentration in human fibroblasts were 16.9 µM and more than 100 µM, respectively. Treatment with 45B5 decreased viral DNA synthesis and IE62 expression weakly but significantly. All 45B5-resistant viral clones isolated were found to have at least one mutation in ORF54 that encodes the portal protein. There were no effects on interaction between the portal and scaffold proteins. Thus, 45B5 may inhibit nuclear delivery of viral DNA.
一种抗水痘带状疱疹病毒化合物，即5-氯苯并[b]噻吩衍生物（45B5），得到了表征。其对无细胞疫苗Oka株的50%有效浓度和在人成纤维细胞中的50%细胞毒性浓度分别为16.9 μM和超过100 μM。用45B5处理可微弱但显著地降低病毒DNA合成和IE62表达。所有分离出的对45B5耐药的病毒克隆在编码门蛋白的ORF54中均至少有一个突变。对门蛋白和支架蛋白之间的相互作用没有影响。因此，45B5可能抑制病毒DNA的核内运输。
