Mecanismo de ação de monoterpenoides com atividade sedativa e anestésica em jundiás (Rhamdia quelen)

Detalhes bibliográficos
Autor(a) principal: Bianchini, Adriane Erbice
Data de Publicação: 2017
Tipo de documento: Dissertação
Idioma: por
Título da fonte: Biblioteca Digital de Teses e Dissertações do UFSM
Texto Completo: http://repositorio.ufsm.br/handle/1/18150
Resumo: Monoterpenoids are present in a large proportion in essential oils of aromatic plants and are important sources of bioactive molecules. Thymol, carvacrol and linalool are examples of these compounds and among their biological properties the depressant activity in the central nervous system stands out. In this context, the objective of this study was to evaluate 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-1) to evaluate time for anesthesia and recovery. Both compounds induced sedation at 25 mg L-1 and anesthesia with 50–100 mg L-1. However, fish exposed to carvacrol presented strong muscle contractions and mortality. AChE activity increased about two-fold in the brain of fish exposed to 50 mg L -1 carvacrol and about three-fold at 100 mg L -1 thymol, however AChE activity decreased (about five-fold) in the muscle of silver catfish exposed to 100 mg L -1 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 50 mg L-1 is more suitable than carvacrol for anesthesia in silver catfish, as we observed good anesthetic performance and no interference with AChE activity. Its anesthetic effect appeared to involve the GABAA receptors, but was not related to the benzodiazepine site. Therefore, the anesthetic effect of S-(+)-linalool in silver catfish does not appear to involve the GABAA receptors.
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spelling 2019-09-05T18:34:09Z2019-09-05T18:34:09Z2017-02-02http://repositorio.ufsm.br/handle/1/18150Monoterpenoids are present in a large proportion in essential oils of aromatic plants and are important sources of bioactive molecules. Thymol, carvacrol and linalool are examples of these compounds and among their biological properties the depressant activity in the central nervous system stands out. In this context, the objective of this study was to evaluate 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-1) to evaluate time for anesthesia and recovery. Both compounds induced sedation at 25 mg L-1 and anesthesia with 50–100 mg L-1. However, fish exposed to carvacrol presented strong muscle contractions and mortality. AChE activity increased about two-fold in the brain of fish exposed to 50 mg L -1 carvacrol and about three-fold at 100 mg L -1 thymol, however AChE activity decreased (about five-fold) in the muscle of silver catfish exposed to 100 mg L -1 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 50 mg L-1 is more suitable than carvacrol for anesthesia in silver catfish, as we observed good anesthetic performance and no interference with AChE activity. Its anesthetic effect appeared to involve the GABAA receptors, but was not related to the benzodiazepine site. Therefore, the anesthetic effect of S-(+)-linalool in silver catfish does not appear to involve the GABAA receptors.Os monoterpenoides estão presentes em grande proporção em óleos essenciais de plantas aromáticas e são fontes importantes de moléculas bioativas. Timol, carvacrol e linalol são exemplos destes compostos e dentre suas propriedades biológicas destacam-se a atividade depressora no sistema nervoso central. Neste contexto, o objetivo deste estudo foi avaliar o potencial anestésico do timol e do carvacrol e a influência na atividade da acetilcolinesterase (AChE) no músculo e no cérebro de jundiás (Rhamdia quelen). A atividade da AChE em jundiás expostos ao S-(+)-linalol também foi avaliada. Posteriormente, avaliamos a ação do timol e do S-(+)-linalol no sistema GABAérgico. Os peixes foram expostos a timol e carvacrol (25, 50, 75 e 100 mg/L) para avaliar o tempo de anestesia e recuperação. Ambos os compostos induziram sedação com 25 mg/L e anestesia com 50-100 mg/L. No entanto, os peixes expostos ao carvacrol apresentaram fortes contrações musculares e mortalidade. A atividade da AChE aumentou cerca de duas vezes no cérebro de peixes expostos a 50 mg/L de carvacrol e cerca de três vezes com 100 mg/L de timol, contudo a atividade da AChE diminuiu (cerca de cinco vezes) no músculo de jundiás expostos à 100 mg/L de carvacrol. O S-(+)-linalol não alterou a atividade da AChE. A anestesia com timol foi revertida por exposição à picrotoxina (antagonista de GABAA), semelhante ao controle positivo propofol, mas não foi revertida pelo flumazenil (antagonista do sítio de ligação benzodiazepínico), como observado para o diazepam, controle positivo. A picrotoxina não reverteu o efeito de S- (+)-linalol. Timol 50 mg/L é mais adequado que carvacrol para anestesia em jundiás, uma vez que observamos um bom desempenho anestésico e nenhuma interferência com a atividade da AChE. O efeito anestésico do timol parece envolver os receptores GABAA, mas não está relacionado com o sítio de ligação benzodiazepínico. Contudo, o efeito anestésico de S-(+)- linalol em jundiás não parece envolver os receptores GABAA.porUniversidade Federal de Santa MariaCentro de Ciências da SaúdePrograma de Pós-Graduação em FarmacologiaUFSMBrasilFarmacologiaAttribution-NonCommercial-NoDerivatives 4.0 Internationalhttp://creativecommons.org/licenses/by-nc-nd/4.0/info:eu-repo/semantics/openAccessBenzodiazepínicoCarvacrolGABAAS-(+)-linalolTimolBenzodiazepineS-(+)-linaloolThymolCNPQ::CIENCIAS DA SAUDE::FARMACIAMecanismo de ação de monoterpenoides com atividade sedativa e anestésica em jundiás (Rhamdia quelen)Mechanism of action of monoterpenoids with sedative and anesthetic activity in silver catfish (Rhamdia quelen)info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisBaldisserotto, Bernardohttp://lattes.cnpq.br/1036046601275319Assis, Helena Cristina da Silva dehttp://lattes.cnpq.br/5097375710591157Burger, Marilise Escobarhttp://lattes.cnpq.br/9128090974948413http://lattes.cnpq.br/1491614242432359Bianchini, Adriane Erbice4003000000056004948adb8-9408-43d6-82b1-b9df8481e3daea9cd446-eb61-45e4-9769-35f743d06052e62ff99c-b0e8-41fa-9cc8-9b79eda4c882a609a359-a0e0-4c67-b9c2-5c029e49529creponame:Biblioteca Digital de Teses e Dissertações do UFSMinstname:Universidade Federal de Santa Maria (UFSM)instacron:UFSMORIGINALDIS_PPGFARMACOLOGIA_2017_BIANCHINI_ADRIANE.pdfDIS_PPGFARMACOLOGIA_2017_BIANCHINI_ADRIANE.pdfDissertação de Mestradoapplication/pdf946816http://repositorio.ufsm.br/bitstream/1/18150/1/DIS_PPGFARMACOLOGIA_2017_BIANCHINI_ADRIANE.pdfad565a11aae525846c3e383595679c76MD51CC-LICENSElicense_rdflicense_rdfapplication/rdf+xml; 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dc.title.por.fl_str_mv Mecanismo de ação de monoterpenoides com atividade sedativa e anestésica em jundiás (Rhamdia quelen)
dc.title.alternative.eng.fl_str_mv Mechanism of action of monoterpenoids with sedative and anesthetic activity in silver catfish (Rhamdia quelen)
title Mecanismo de ação de monoterpenoides com atividade sedativa e anestésica em jundiás (Rhamdia quelen)
spellingShingle Mecanismo de ação de monoterpenoides com atividade sedativa e anestésica em jundiás (Rhamdia quelen)
Bianchini, Adriane Erbice
Benzodiazepínico
Carvacrol
GABAA
S-(+)-linalol
Timol
Benzodiazepine
S-(+)-linalool
Thymol
CNPQ::CIENCIAS DA SAUDE::FARMACIA
title_short Mecanismo de ação de monoterpenoides com atividade sedativa e anestésica em jundiás (Rhamdia quelen)
title_full Mecanismo de ação de monoterpenoides com atividade sedativa e anestésica em jundiás (Rhamdia quelen)
title_fullStr Mecanismo de ação de monoterpenoides com atividade sedativa e anestésica em jundiás (Rhamdia quelen)
title_full_unstemmed Mecanismo de ação de monoterpenoides com atividade sedativa e anestésica em jundiás (Rhamdia quelen)
title_sort Mecanismo de ação de monoterpenoides com atividade sedativa e anestésica em jundiás (Rhamdia quelen)
author Bianchini, Adriane Erbice
author_facet Bianchini, Adriane Erbice
author_role author
dc.contributor.advisor1.fl_str_mv Baldisserotto, Bernardo
dc.contributor.advisor1Lattes.fl_str_mv http://lattes.cnpq.br/1036046601275319
dc.contributor.referee1.fl_str_mv Assis, Helena Cristina da Silva de
dc.contributor.referee1Lattes.fl_str_mv http://lattes.cnpq.br/5097375710591157
dc.contributor.referee2.fl_str_mv Burger, Marilise Escobar
dc.contributor.referee2Lattes.fl_str_mv http://lattes.cnpq.br/9128090974948413
dc.contributor.authorLattes.fl_str_mv http://lattes.cnpq.br/1491614242432359
dc.contributor.author.fl_str_mv Bianchini, Adriane Erbice
contributor_str_mv Baldisserotto, Bernardo
Assis, Helena Cristina da Silva de
Burger, Marilise Escobar
dc.subject.por.fl_str_mv Benzodiazepínico
Carvacrol
GABAA
S-(+)-linalol
Timol
topic Benzodiazepínico
Carvacrol
GABAA
S-(+)-linalol
Timol
Benzodiazepine
S-(+)-linalool
Thymol
CNPQ::CIENCIAS DA SAUDE::FARMACIA
dc.subject.eng.fl_str_mv Benzodiazepine
S-(+)-linalool
Thymol
dc.subject.cnpq.fl_str_mv CNPQ::CIENCIAS DA SAUDE::FARMACIA
description Monoterpenoids are present in a large proportion in essential oils of aromatic plants and are important sources of bioactive molecules. Thymol, carvacrol and linalool are examples of these compounds and among their biological properties the depressant activity in the central nervous system stands out. In this context, the objective of this study was to evaluate 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-1) to evaluate time for anesthesia and recovery. Both compounds induced sedation at 25 mg L-1 and anesthesia with 50–100 mg L-1. However, fish exposed to carvacrol presented strong muscle contractions and mortality. AChE activity increased about two-fold in the brain of fish exposed to 50 mg L -1 carvacrol and about three-fold at 100 mg L -1 thymol, however AChE activity decreased (about five-fold) in the muscle of silver catfish exposed to 100 mg L -1 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 50 mg L-1 is more suitable than carvacrol for anesthesia in silver catfish, as we observed good anesthetic performance and no interference with AChE activity. Its anesthetic effect appeared to involve the GABAA receptors, but was not related to the benzodiazepine site. Therefore, the anesthetic effect of S-(+)-linalool in silver catfish does not appear to involve the GABAA receptors.
publishDate 2017
dc.date.issued.fl_str_mv 2017-02-02
dc.date.accessioned.fl_str_mv 2019-09-05T18:34:09Z
dc.date.available.fl_str_mv 2019-09-05T18:34:09Z
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dc.rights.driver.fl_str_mv Attribution-NonCommercial-NoDerivatives 4.0 International
http://creativecommons.org/licenses/by-nc-nd/4.0/
info:eu-repo/semantics/openAccess
rights_invalid_str_mv Attribution-NonCommercial-NoDerivatives 4.0 International
http://creativecommons.org/licenses/by-nc-nd/4.0/
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Universidade Federal de Santa Maria
Centro de Ciências da Saúde
dc.publisher.program.fl_str_mv Programa de Pós-Graduação em Farmacologia
dc.publisher.initials.fl_str_mv UFSM
dc.publisher.country.fl_str_mv Brasil
dc.publisher.department.fl_str_mv Farmacologia
publisher.none.fl_str_mv Universidade Federal de Santa Maria
Centro de Ciências da Saúde
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