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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。
Cycloheximide can inhibit most of the eukaryotic protein synthesis, often as a biochemical research reagent is widely used. In this paper, the antiviral activity of a more systematic study showed that cycloheximide in vitro on human immunodeficiency virus, influenza virus, Coxsackie virus, enterovirus, herpes simplex virus and human cytomegalovirus and other RNA viruses and DNA viruses show strong inhibitory effects. Especially, the strong inhibitory effect on Coxsackievirus B and enterovirus EV71 which are currently lack of effective therapeutic drugs in clinic is a cause of concern. In this paper, the structural modification of cycloheximide and its structure-activity relationship were discussed. The C-2 ’hydroxyl and C-2’ carbonyl in the cycloheximide structure were essential for antiviral activity. Both the modification of -2 ’hydroxyl and C-2’ carbonyl lead to a decrease or loss of their antiviral activity.