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具有麻醉活性的单萜类化合物(百里香酚、香芹酚和S-(+)-芳樟醇)在淡水鲶鱼(Rhamdia quelen)中的研究:乙酰胆碱酯酶和γ-氨基丁酸能活性评估

Monoterpenoids (thymol, carvacrol and S-(+)-linalool) with anesthetic activity in silver catfish (Rhamdia quelen): evaluation of acetylcholinesterase and GABAergic activity.

作者信息

Bianchini A E, Garlet Q I, da Cunha J A, Bandeira G, Brusque I C M, Salbego J, Heinzmann B M, Baldisserotto B

机构信息

Programa de Pós-Graduação em Farmacologia, Universidade Federal de Santa Maria, Santa Maria, RS, Brasil.

Curso de Medicina Veterinária, Universidade Federal de Santa Maria, Santa Maria, RS, Brasil.

出版信息

Braz J Med Biol Res. 2017 Oct 19;50(12):e6346. doi: 10.1590/1414-431X20176346.

Abstract

This study evaluated the anesthetic potential of thymol and carvacrol, and their influence on acetylcholinesterase (AChE) activity in the muscle and brain of silver catfish (Rhamdia quelen). The AChE activity of S-(+)-linalool was also evaluated. We subsequently assessed the effects of thymol and S-(+)-linalool on the GABAergic system. Fish were exposed to thymol and carvacrol (25, 50, 75, and 100 mg/L) to evaluate time for anesthesia and recovery. Both compounds induced sedation at 25 mg/L and anesthesia with 50-100 mg/L. However, fish exposed to carvacrol presented strong muscle contractions and mortality. AChE activity was increased in the brain of fish at 50 mg/L carvacrol and 100 mg/L thymol, and decreased in the muscle at 100 mg/L carvacrol. S-(+)-linalool did not alter AChE activity. Anesthesia with thymol was reversed by exposure to picrotoxin (GABAA antagonist), similar to the positive control propofol, but was not reversed by flumazenil (antagonist of benzodiazepine binding site), as observed for the positive control diazepam. Picrotoxin did not reverse the effect of S-(+)-linalool. Thymol exposure at 50 mg/L is more suitable than carvacrol for anesthesia in silver catfish, because this concentration did not cause any mortality or interference with AChE activity. Thymol interacted with GABAA receptors, but not with the GABAA/benzodiazepine site. In contrast, S-(+)-linalool did not act in GABAA receptors in silver catfish.

摘要

本研究评估了百里香酚和香芹酚的麻醉潜力,以及它们对银鲶(Rhamdia quelen)肌肉和大脑中乙酰胆碱酯酶(AChE)活性的影响。还评估了S-(+)-芳樟醇的AChE活性。随后,我们评估了百里香酚和S-(+)-芳樟醇对GABA能系统的影响。将鱼暴露于百里香酚和香芹酚(25、50、75和100mg/L)中,以评估麻醉和恢复时间。两种化合物在25mg/L时诱导镇静,在50-100mg/L时诱导麻醉。然而,暴露于香芹酚的鱼出现强烈的肌肉收缩和死亡。在50mg/L香芹酚和100mg/L百里香酚处理的鱼脑中,AChE活性增加,而在100mg/L香芹酚处理的鱼肌肉中,AChE活性降低。S-(+)-芳樟醇不改变AChE活性。与阳性对照丙泊酚类似,暴露于苦味毒(GABAA拮抗剂)可逆转百里香酚引起的麻醉,但与阳性对照地西泮一样,氟马西尼(苯二氮䓬结合位点拮抗剂)不能逆转。苦味毒不能逆转S-(+)-芳樟醇的作用。50mg/L的百里香酚暴露比香芹酚更适合用于银鲶的麻醉,因为该浓度不会导致任何死亡或对AChE活性产生干扰。百里香酚与GABAA受体相互作用,但不与GABAA/苯二氮䓬位点相互作用。相比之下,S-(+)-芳樟醇在银鲶的GABAA受体中不起作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7e8/5649867/3521e0e56b9d/1414-431X-bjmbr-1414-431X20176346-gf01.jpg

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