环己酰亚胺及其衍生物的抗病毒活性研究

环己酰亚胺能抑制大多真核细胞的蛋白合成, 常作为生化研究试剂被广泛使用。本文对其抗病毒活性进行了较系统研究, 结果显示, 环己酰亚胺体外对人类免疫缺陷病毒、流感病毒、柯萨奇病毒、肠道病毒、单纯疱疹病毒及人巨细胞病毒等多种RNA病毒和DNA病毒显示出很强的抑制作用。尤其是对目前临床上尚缺乏有效治疗药物的柯萨奇病毒B及肠道病毒EV71的强抑制作用令人关注。本文对环己酰亚胺的结构修饰及其构效关系进行了初步探讨, 环己酰亚胺分子结构中的C-2' 羟基和C-2' 羰基为抗病毒活性必需基团, 对C-2' 羟基和C-2' 羰基的修饰均导致其抗病毒活性的降低或消失。

Antiviral activities of cycloheximide and its derivatives

Cycloheximide (CHX) inhibits protein synthesis in most eukaryotic cells and it is a well-known tool commonly used in biochemical research.  In this paper, the antiviral spectrum of CHX against several DNA and RNA viruses have been evaluated.  CHX showed strong inhibitory activities against several RNA viruses such as HIV-1, influenza viruses, coxsackie B virus, enterovirus (EV71) and several DNA viruses such as HSV and HCMV.  Especially the strong inhibitory activities of CHX against coxsackie B virus and enterovirus caught our attention, since effective drugs available in clinic are limited.  The SAR of CHX derivatives also has been discussed in the paper.  The hydroxyl group at C-2' and carbonyl group at C-2' of CHX are essential for its  antiviral activity.  And modification to these groups results its derivatives’ antiviral activities reduced or lost.