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雷帕霉素(rapamycin,RAPA)是20世纪70年代初由加拿大Ayerst研究所从放线菌(Streptomyces hygroscopicus)培养液中分离出来的大环内酯类抗生素。研究已证明,RAPA是一种强有力的免疫抑制剂,不但对多种自身免疫性疾病有显著疗效,而且在不同种类的器官移植动物模型上显示出显著的抗排斥反应活性。RAPA在结构上与FK506相似,但它的作用主要表现为抑制T细胞和T细胞依赖性B细胞对移植物抗原的反应。由于其独特的作用机理,目前已广泛地应用于肾移植。
Rapamycin (RAPA) is a macrolide antibiotic isolated from the Streptomyces hygroscopicus culture in the early 1970s by the Ayerst Institute in Canada. Studies have shown that RAPA is a potent immunosuppressive agent that not only has a significant effect on a variety of autoimmune diseases but also shows significant anti-rejection activity in various animal models of organ transplantation. RAPA is structurally similar to FK506, but its role is mainly manifested as inhibition of T-cell and T-cell dependent B cell responses to graft antigens. Due to its unique mechanism of action, it has been widely used in kidney transplantation.