虫草素(cordycepin)是一种具有广泛生物活性和药理作用的脱氧核苷类似物,对多种疾病都有潜在的治疗作用。但从50年代被发现以来有关其体内实验的报道甚少,主要是由于它在体内腺苷脱氨酶(ADA)的作用下快速脱氨基后会变为生物活性极小的3’-脱氧次黄嘌呤核苷。近几年的研究表明,ADA抑制剂能有效延缓虫草素在体内的代谢。本文介绍了虫草素体内代谢和药理作用的特点及其与ADA抑制剂联合应用的研究进展。 Cordycepin is a deoxynucleoside analogue with a wide range of biological activities and pharmacological effects and has a potential therapeutic effect on various diseases. However, there have been very few reports about its in vivo experiments since its discovery in the 1950s, mainly due to its rapid deamination under the action of adenosine deaminase (ADA) in the body, which turns into a biologically minimal 3’-deoxygenation sequence. Xanthosine. Studies in recent years have shown that ADA inhibitors can effectively delay the metabolism of cordycepin in the body. This article describes the characteristics of cordycepin in vivo metabolism and pharmacological effects and its application in combination with ADA inhibitors.