Research Process of Cyclosporin A Metabolite

CHEN Xin; WANG Xiaoxue; TANG Kun; LI Jiang; CHEN Wenqian; QIN Wei; ZHANG Dan; LI Pengmei; ZHANG Xianglin

doi:10.14009/j.issn.1672-2124.2020.03.030

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Research Process of Cyclosporin A Metabolite

更新时间：2022-10-08

- Research Process of Cyclosporin A Metabolite
- Vol. 20, Issue 3, Pages: 372-376(2020)
- 作者机构：
  
  1. 中日友好医院药学部
  2. 桂林医学院附属医院药学部
- 作者简介：
- 基金信息：
- DOI：10.14009/j.issn.1672-2124.2020.03.030
  CLC： R979.5
- Published：2020，
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[1]陈鑫,王晓雪,唐坤,李江,陈文倩,秦伟,张丹,李朋梅,张相林.环孢素A代谢物的研究概况[J].中国医院用药评价与分析,2020,20(03):372-376.

CHEN Xin, WANG Xiaoxue, TANG Kun, et al. Research Process of Cyclosporin A Metabolite. [J]. 20(3):372-376(2020)
[1]陈鑫,王晓雪,唐坤,李江,陈文倩,秦伟,张丹,李朋梅,张相林.环孢素A代谢物的研究概况[J].中国医院用药评价与分析,2020,20(03):372-376. DOI： 10.14009/j.issn.1672-2124.2020.03.030.

CHEN Xin, WANG Xiaoxue, TANG Kun, et al. Research Process of Cyclosporin A Metabolite. [J]. 20(3):372-376(2020) DOI： 10.14009/j.issn.1672-2124.2020.03.030.

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。

Abstract

Cyclosporine A is a cyclic polypeptide with immunosuppressive activity. It is used clinically for antirejection 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 CYP3 A family

and more than 30 metabolites are obtained

which are excreted through bile. The primary metabolites AM1

AM9 and AM4 N 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ACYP3A代谢物免疫抑制活性肝肾毒性血药浓度检测技术

Keywords

Cyclosporine ACYP3AMetabolitesImmunosuppressive activityHepatorenal toxicityBlood drug concentrationDetection technology

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