恩诺沙星在鲫鱼肝微粒体中的代谢及代谢关键酶

刘婉玉, Tadiyose Girma Bekele, 赵洪霞. 恩诺沙星在鲫鱼肝微粒体中的代谢及代谢关键酶[J]. 生态毒理学报, 2020, 15(3): 64-70. doi: 10.7524/AJE.1673-5897.20190903001
引用本文: 刘婉玉, Tadiyose Girma Bekele, 赵洪霞. 恩诺沙星在鲫鱼肝微粒体中的代谢及代谢关键酶[J]. 生态毒理学报, 2020, 15(3): 64-70. doi: 10.7524/AJE.1673-5897.20190903001
Liu Wanyu, Tadiyose Girma Bekele, Zhao Hongxia. Metabolism of Enrofloxacin in Liver Microsomes of Crucian Carp (Carassius auratus) and Its Key Enzymes in vitro[J]. Asian Journal of Ecotoxicology, 2020, 15(3): 64-70. doi: 10.7524/AJE.1673-5897.20190903001
Citation: Liu Wanyu, Tadiyose Girma Bekele, Zhao Hongxia. Metabolism of Enrofloxacin in Liver Microsomes of Crucian Carp (Carassius auratus) and Its Key Enzymes in vitro[J]. Asian Journal of Ecotoxicology, 2020, 15(3): 64-70. doi: 10.7524/AJE.1673-5897.20190903001

恩诺沙星在鲫鱼肝微粒体中的代谢及代谢关键酶

    作者简介: 刘婉玉(1995-),女,硕士研究生,研究方向为污染生态化学,E-mail:wwanai@mail.dlut.edu.cn
  • 基金项目:

    国家自然科学基金资助项目(21677023)

  • 中图分类号: X171.5

Metabolism of Enrofloxacin in Liver Microsomes of Crucian Carp (Carassius auratus) and Its Key Enzymes in vitro

  • Fund Project:
  • 摘要: 抗生素因具有抗菌谱广、杀菌性强等特点而被广泛应用于人类医药、畜牧业、农业和水产养殖业。其进入水生生物体内后,会在药物代谢酶的作用下发生代谢转化,产生生态毒性。采用鲫鱼肝微粒体体外孵育法,探究恩诺沙星细胞色素P450酶作用下的代谢转化过程,并通过代谢抑制实验确定关键的代谢酶。结果表明,恩诺沙星体外代谢过程符合一级动力学方程,当恩诺沙星暴露浓度为1 mg·L-1时,其在肝微粒体中的消除速率常数(k)最大为0.00303 min-1,半衰期(t1/2)最短为228.8 min,应用高效液相色谱串联质谱(HPLC-MS/MS)技术,检测到了恩诺沙星脱乙基产物和羟基化产物;代谢抑制实验结果表明,CYP3A4在恩诺沙星代谢过程中起主要作用,是恩诺沙星代谢的关键酶。本研究结果为深入了解恩诺沙星在水生生物体内的代谢转化及其生态风险提供了基础数据。
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  • 收稿日期:  2019-09-03
刘婉玉, Tadiyose Girma Bekele, 赵洪霞. 恩诺沙星在鲫鱼肝微粒体中的代谢及代谢关键酶[J]. 生态毒理学报, 2020, 15(3): 64-70. doi: 10.7524/AJE.1673-5897.20190903001
引用本文: 刘婉玉, Tadiyose Girma Bekele, 赵洪霞. 恩诺沙星在鲫鱼肝微粒体中的代谢及代谢关键酶[J]. 生态毒理学报, 2020, 15(3): 64-70. doi: 10.7524/AJE.1673-5897.20190903001
Liu Wanyu, Tadiyose Girma Bekele, Zhao Hongxia. Metabolism of Enrofloxacin in Liver Microsomes of Crucian Carp (Carassius auratus) and Its Key Enzymes in vitro[J]. Asian Journal of Ecotoxicology, 2020, 15(3): 64-70. doi: 10.7524/AJE.1673-5897.20190903001
Citation: Liu Wanyu, Tadiyose Girma Bekele, Zhao Hongxia. Metabolism of Enrofloxacin in Liver Microsomes of Crucian Carp (Carassius auratus) and Its Key Enzymes in vitro[J]. Asian Journal of Ecotoxicology, 2020, 15(3): 64-70. doi: 10.7524/AJE.1673-5897.20190903001

恩诺沙星在鲫鱼肝微粒体中的代谢及代谢关键酶

    作者简介: 刘婉玉(1995-),女,硕士研究生,研究方向为污染生态化学,E-mail:wwanai@mail.dlut.edu.cn
  • 大连理工大学环境学院, 工业生态和环境工程教育部重点实验室, 大连 116024
基金项目:

国家自然科学基金资助项目(21677023)

摘要: 抗生素因具有抗菌谱广、杀菌性强等特点而被广泛应用于人类医药、畜牧业、农业和水产养殖业。其进入水生生物体内后,会在药物代谢酶的作用下发生代谢转化,产生生态毒性。采用鲫鱼肝微粒体体外孵育法,探究恩诺沙星细胞色素P450酶作用下的代谢转化过程,并通过代谢抑制实验确定关键的代谢酶。结果表明,恩诺沙星体外代谢过程符合一级动力学方程,当恩诺沙星暴露浓度为1 mg·L-1时,其在肝微粒体中的消除速率常数(k)最大为0.00303 min-1,半衰期(t1/2)最短为228.8 min,应用高效液相色谱串联质谱(HPLC-MS/MS)技术,检测到了恩诺沙星脱乙基产物和羟基化产物;代谢抑制实验结果表明,CYP3A4在恩诺沙星代谢过程中起主要作用,是恩诺沙星代谢的关键酶。本研究结果为深入了解恩诺沙星在水生生物体内的代谢转化及其生态风险提供了基础数据。

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