环孢素A代谢物的研究概况  

Research Process of Cyclosporin A Metabolite

作　　者：陈鑫 王晓雪[1] 唐坤[2] 李江[2] 陈文倩[1] 秦伟[1] 张丹[1] 李朋梅[1] 张相林[1] CHEN Xin;WANG Xiaoxue;TANG Kun;LI Jiang;CHEN Wenqian;QIN Wei;ZHANG Dan;LI Pengmei;ZHANG Xianglin(Dept. of Pharmacy, China-Japan Friendship Hospital, Beijing 100029, China;Dept. of Pharmacy, Affiliated Hospital of Guilin Medical College,Guangxi Guilin 541001, China)

机构地区：[1]中日友好医院药学部,北京100029 [2]桂林医学院附属医院药学部,广西桂林541001

出　　处：《中国医院用药评价与分析》2020年第3期372-376,共5页Evaluation and Analysis of Drug-use in Hospitals of China

基　　金：北京市自然科学基金(No.7192190);国家自然科学青年基金(No.81503175);中日友好医院青年基金(No.2014-3-QN-27)。

摘　　要：环孢素A是具有免疫抑制活性的环状多肽,在临床上被用于多种器官或骨髓移植患者的抗排斥反应,并可治疗自身免疫性疾病。环孢素A主要在胃肠道由肝药酶CYP3A家族代谢,得到超过30种代谢物,经胆汁排泄。初级代谢物AM1、AM9、AM4N等具有较显著的免疫抑制活性和肝肾毒性。免疫法可同时检测环孢素A及其代谢物的总浓度,而高效液相色谱法则可分别检测二者的浓度。患者的生理或病理状态也影响环孢素A及其代谢物在体内的分布。Cyclosporine A is a cyclic polypeptide with immunosuppressive activity.It is used clinically for anti-rejection in various organ or bone marrow transplant patients and can treat autoimmune diseases.Cyclosporine A is mainly metabolized in the gastrointestinal tract by the liver drug enzyme CYP3A family,and more than 30 metabolites are obtained,which are excreted through bile.The primary metabolites AM1,AM9 and AM4N have significant immunosuppressive activity and hepatorenal toxicity.The total concentration of cyclosporine A and its metabolites could be detected simultaneously by immunoassay,while high performance liquid chromatography can be used to detect the concentration.The physiological or pathological status of the patient also affects the distribution of cyclosporine A and its metabolites in vivo.

关 键 词：环孢素A CYP3A 代谢物 免疫抑制活性 肝肾毒性 血药浓度 检测技术 

分 类 号：R979.5[医药卫生—药品]