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丁鱥体内的胆碱酯酶和羧酸酯酶对药物的敏感性。

Sensitivity of cholinesterases and carboxylesterases to pharmaceutical products in Tinca tinca.

机构信息

Área de Toxicología, Facultad de Veterinaria, Universidad de Extremadura, Cáceres, Spain.

Instituto Universitario de Investigación en Biotecnología Ganadera y Cinegética (INBIO G+C), Universidad de Extremadura, Cáceres, Spain.

出版信息

Environ Toxicol. 2024 Jul;39(7):3856-3871. doi: 10.1002/tox.24234. Epub 2024 Apr 1.

Abstract

Discharges to the aquatic environment of pharmaceuticals represent a hazard to the aquatic organisms. Subchronic assay with 17-alpha-ethinylestradiol (EE) and in vitro essays with pharmaceuticals of environmental concern were conducted to examine the sensitivity of tissue acetylcholinesterase (AChE) and carboxylesterase (CbE) activities of Tinca tinca to them. Subchronic exposure to 17-alpha-EE caused significant effects on brain, liver, and muscle CbE, but no on AChE activities. Most of the pharmaceuticals tested in vitro were considered as weak inhibitors of tissular AChE activity. Depending on the tissues, some compounds were classified as moderate inhibitors of CbE activity while other were categorized as weak enzymatic inhibitors. An opposite trend was observed depending on the tissue, while brain and liver CbE activities were inhibited, the muscle CbE activity was induced. Changes experienced on enzymatic activities after exposure to pharmaceuticals might affect the physiological functions in which these enzymes are involved. In vitro exposure to 17-alpha-EE in tench could be an informative, but not a surrogate model to know the effect of this synthetic estrogen on AChE and CbE activities.

摘要

向水生环境中排放药品会对水生生物造成危害。本研究进行了 17-α-乙炔基雌二醇(EE)的亚慢性检测和环境关注药品的体外检测,以研究欧鳗组织乙酰胆碱酯酶(AChE)和羧酸酯酶(CbE)活性对它们的敏感性。亚慢性暴露于 17-α-EE 会对大脑、肝脏和肌肉的 CbE 产生显著影响,但对 AChE 活性没有影响。在体外测试的大多数药物被认为是组织 AChE 活性的弱抑制剂。根据组织的不同,一些化合物被归类为 CbE 活性的中度抑制剂,而其他化合物则被归类为弱酶抑制剂。根据组织的不同,观察到了相反的趋势,大脑和肝脏的 CbE 活性受到抑制,而肌肉的 CbE 活性则被诱导。暴露于药物后酶活性的变化可能会影响这些酶参与的生理功能。在欧鳗中进行的体外接触 17-α-EE 可能是一种信息丰富的模型,但不是替代模型,无法了解这种合成雌激素对 AChE 和 CbE 活性的影响。

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