Estudo comparativo das ações vasodilatadoras de (+)-Óxido rosa, β-Citronelol e Geraniol em aorta de rato

Detalhes bibliográficos
Autor(a) principal: Silva, Alfredo Augusto Vasconcelos da
Data de Publicação: 2017
Tipo de documento: Dissertação
Idioma: por
Título da fonte: Repositório Institucional da Universidade Federal do Ceará (UFC)
Texto Completo: http://www.repositorio.ufc.br/handle/riufc/22409
Resumo: (+)-Rose oxide (OR), β-citronellol (BC) and geraniol (GE) are chemically related monoterpenes found naturally in several essential oils, such as in bulgarian rose and geranium oil. While the pharmacological actions of OR are still scarce, some reports show that BC and GE act potentially as inhibitors of Ca2+ channels in vascular smooth muscle. As chemically related molecules, the objective of this study was to compare the effects of OR, BC and GE on aortic contractility isolated from rats. Isometric records were obtained from aortic rings through a data acquisition system. In aortic rings with intact endothelium, OR, BC and GE (1 - 3000 μM) relaxed the contraction induced by phenylephrine with EC50 values [I.C. 95%] of 1715.9 [1386.6-2123.4], 342.6 [110.2-1065.8] and 930.8 [758.8-1141.7] μM, respectively. Already in KCl induced contraction (60 mM) the OR had EC50 of 550.6 [245.6-1234.4] μM, BC of 98.3 [42.8 - 225.7] μM and GE of 217,5 [156.4-302.5] μM. The vasorelaxant effects of monoterpenes on contractions induced by phenylephrine or KCl were not significantly (P> 0.05, Mann-Whitney) altered by endothelial removal, treatment with L-NAME or tetraethylammonium. The EC50 values of the monoterpenes in phorbol ester pre-contracted preparations (973.6 [389.7-2432.2] μM for OR, 77.8 [14.4-419.2] μM for BC and 151, 2 [46.21 - 494.6] μM for GE) and U46619 (533.6 [212.4-1340.8] μM for OR, 106.7 [53.6 - 212.1] μM for BC and 386,8 [207.1 - 722.4] μM for GE), were significantly lower (p <0.01, Mann-Whitney) than the values obtained in pre-contraction induced by phenylephrine in the aorta. In Ca2+-free medium in the presence of KCl (60 mM), contractions caused by the addition of Ca2+ were significantly reduced by OR, BC and GE (from 600μM), but when phenylephrine was added instead of K+, there was no decrease in the magnitude of the contractile response. The present study suggests that the vasorelaxant activity of these monoterpenes in rat aorta involves inhibition of voltage-operated calcium channels in the following order of pharmacological potency: BC > GE > OR.
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spelling Estudo comparativo das ações vasodilatadoras de (+)-Óxido rosa, β-Citronelol e Geraniol em aorta de ratoComparative study of vasodilating actions of (+) – Rose oxide, β-Citronelol and Geraniol in rat aortaFarmacologiaVasodilatadoresMonoterpenos(+)-Rose oxide (OR), β-citronellol (BC) and geraniol (GE) are chemically related monoterpenes found naturally in several essential oils, such as in bulgarian rose and geranium oil. While the pharmacological actions of OR are still scarce, some reports show that BC and GE act potentially as inhibitors of Ca2+ channels in vascular smooth muscle. As chemically related molecules, the objective of this study was to compare the effects of OR, BC and GE on aortic contractility isolated from rats. Isometric records were obtained from aortic rings through a data acquisition system. In aortic rings with intact endothelium, OR, BC and GE (1 - 3000 μM) relaxed the contraction induced by phenylephrine with EC50 values [I.C. 95%] of 1715.9 [1386.6-2123.4], 342.6 [110.2-1065.8] and 930.8 [758.8-1141.7] μM, respectively. Already in KCl induced contraction (60 mM) the OR had EC50 of 550.6 [245.6-1234.4] μM, BC of 98.3 [42.8 - 225.7] μM and GE of 217,5 [156.4-302.5] μM. The vasorelaxant effects of monoterpenes on contractions induced by phenylephrine or KCl were not significantly (P> 0.05, Mann-Whitney) altered by endothelial removal, treatment with L-NAME or tetraethylammonium. The EC50 values of the monoterpenes in phorbol ester pre-contracted preparations (973.6 [389.7-2432.2] μM for OR, 77.8 [14.4-419.2] μM for BC and 151, 2 [46.21 - 494.6] μM for GE) and U46619 (533.6 [212.4-1340.8] μM for OR, 106.7 [53.6 - 212.1] μM for BC and 386,8 [207.1 - 722.4] μM for GE), were significantly lower (p <0.01, Mann-Whitney) than the values obtained in pre-contraction induced by phenylephrine in the aorta. In Ca2+-free medium in the presence of KCl (60 mM), contractions caused by the addition of Ca2+ were significantly reduced by OR, BC and GE (from 600μM), but when phenylephrine was added instead of K+, there was no decrease in the magnitude of the contractile response. The present study suggests that the vasorelaxant activity of these monoterpenes in rat aorta involves inhibition of voltage-operated calcium channels in the following order of pharmacological potency: BC > GE > OR.(+)-Óxido rosa (OR), β-citronelol (BC) e geraniol (GE) são monoterpenos quimicamente relacionados naturalmente encontrados em diversos óleos essenciais, como na rosa búlgara e óleo de gerânio. Enquanto as ações farmacológicas do OR são ainda escassas, alguns relatos preliminares apontam que BC e GE agem potencialmente como inibidores de canais de Ca2+ no músculo liso vascular. Por isso, o objetivo deste estudo foi comparar os efeitos do OR, BC e GE na contratilidade da aorta isolada de ratos. Registros isométricos foram obtidos a partir de anéis de aorta através de sistema de aquisição de dados. Em anéis de aorta com endotélio intacto, OR, BC e GE (1 – 3000 µM) relaxaram a contração induzida por fenilefrina com valores de CE50 [I.C. 95%] de 1715,9 [1386,6 – 2123,4], 342,6 [110,2 – 1065,8] e 930,8 [758,8 – 1141,7] µM, respectivamente. Já em contração induzida por KCl (60 mM), OR teve CE50 de 550,6 [245,6 – 1234,4] µM, BC de 98,3 [42,8 – 225,7] µM e GE de 217,5 [156,4 – 302,5] µM. Os efeitos vasorrelaxantes dos monoterpenos sobre as contrações induzidas por fenilefrina ou KCl não foram significativamente (P > 0,05, Mann-Whitney) alterados pela remoção do endotélio, tratamento com L-NAME ou tetraetilamônio. Os valores de CE50 dos monoterpenos nas preparações pré-contraídas com éster de forbol (973,6 [389,7 – 2432,2] µM para OR; 77,8 [14,4 – 419,2] µM para BC e 151,2 [46,21 – 494,6] µM para GE) e U46619 (533,6 [212,4 – 1340,8] µM para OR, 106,7 [53,6 – 212,1] µM para BC e 386,8 [207,1 – 722,4] µM para GE), foram significantemente menores (p < 0,01, Mann-Whitney) do que os valores obtidos na pré-contração induzida por fenilefrina em aorta.Em meio sem Ca2+ na presença de KCl (60 mM), as contrações provocadas pela adição de Ca2+ foram significativamente reduzidas por OR, BC e GE (a partir de 600µM), mas quando fenilefrina foi adicionada em lugar de K+, não ocorreu diminuição da magnitude da resposta contrátil. O presente estudo sugere que a atividade vasorrelaxante desses monoterpenos em aorta de rato envolve inibição de canais de cálcio operados por voltagem na seguinte ordem de potência farmacológica: BC > GE > OR.Magalhães, Pedro Jorge CaldasSilva, Alfredo Augusto Vasconcelos da2017-03-27T16:20:43Z2017-03-27T16:20:43Z2017-02-09info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfSILVA, A. A. V. Estudo comparativo das ações vasodilatadoras de (+)-Óxido rosa, β-Citronelol e Geraniol em aorta de rato. 2017. 60 f. Dissertação (Mestrado em Farmacologia) - Faculdade de Farmácia, Odontologia e Enfermagem, Universidade Federal do Ceará, Fortaleza, 2017.http://www.repositorio.ufc.br/handle/riufc/22409porreponame:Repositório Institucional da Universidade Federal do Ceará (UFC)instname:Universidade Federal do Ceará (UFC)instacron:UFCinfo:eu-repo/semantics/openAccess2019-10-17T14:10:13Zoai:repositorio.ufc.br:riufc/22409Repositório InstitucionalPUBhttp://www.repositorio.ufc.br/ri-oai/requestbu@ufc.br || repositorio@ufc.bropendoar:2024-09-11T18:16:15.278856Repositório Institucional da Universidade Federal do Ceará (UFC) - Universidade Federal do Ceará (UFC)false
dc.title.none.fl_str_mv Estudo comparativo das ações vasodilatadoras de (+)-Óxido rosa, β-Citronelol e Geraniol em aorta de rato
Comparative study of vasodilating actions of (+) – Rose oxide, β-Citronelol and Geraniol in rat aorta
title Estudo comparativo das ações vasodilatadoras de (+)-Óxido rosa, β-Citronelol e Geraniol em aorta de rato
spellingShingle Estudo comparativo das ações vasodilatadoras de (+)-Óxido rosa, β-Citronelol e Geraniol em aorta de rato
Silva, Alfredo Augusto Vasconcelos da
Farmacologia
Vasodilatadores
Monoterpenos
title_short Estudo comparativo das ações vasodilatadoras de (+)-Óxido rosa, β-Citronelol e Geraniol em aorta de rato
title_full Estudo comparativo das ações vasodilatadoras de (+)-Óxido rosa, β-Citronelol e Geraniol em aorta de rato
title_fullStr Estudo comparativo das ações vasodilatadoras de (+)-Óxido rosa, β-Citronelol e Geraniol em aorta de rato
title_full_unstemmed Estudo comparativo das ações vasodilatadoras de (+)-Óxido rosa, β-Citronelol e Geraniol em aorta de rato
title_sort Estudo comparativo das ações vasodilatadoras de (+)-Óxido rosa, β-Citronelol e Geraniol em aorta de rato
author Silva, Alfredo Augusto Vasconcelos da
author_facet Silva, Alfredo Augusto Vasconcelos da
author_role author
dc.contributor.none.fl_str_mv Magalhães, Pedro Jorge Caldas
dc.contributor.author.fl_str_mv Silva, Alfredo Augusto Vasconcelos da
dc.subject.por.fl_str_mv Farmacologia
Vasodilatadores
Monoterpenos
topic Farmacologia
Vasodilatadores
Monoterpenos
description (+)-Rose oxide (OR), β-citronellol (BC) and geraniol (GE) are chemically related monoterpenes found naturally in several essential oils, such as in bulgarian rose and geranium oil. While the pharmacological actions of OR are still scarce, some reports show that BC and GE act potentially as inhibitors of Ca2+ channels in vascular smooth muscle. As chemically related molecules, the objective of this study was to compare the effects of OR, BC and GE on aortic contractility isolated from rats. Isometric records were obtained from aortic rings through a data acquisition system. In aortic rings with intact endothelium, OR, BC and GE (1 - 3000 μM) relaxed the contraction induced by phenylephrine with EC50 values [I.C. 95%] of 1715.9 [1386.6-2123.4], 342.6 [110.2-1065.8] and 930.8 [758.8-1141.7] μM, respectively. Already in KCl induced contraction (60 mM) the OR had EC50 of 550.6 [245.6-1234.4] μM, BC of 98.3 [42.8 - 225.7] μM and GE of 217,5 [156.4-302.5] μM. The vasorelaxant effects of monoterpenes on contractions induced by phenylephrine or KCl were not significantly (P> 0.05, Mann-Whitney) altered by endothelial removal, treatment with L-NAME or tetraethylammonium. The EC50 values of the monoterpenes in phorbol ester pre-contracted preparations (973.6 [389.7-2432.2] μM for OR, 77.8 [14.4-419.2] μM for BC and 151, 2 [46.21 - 494.6] μM for GE) and U46619 (533.6 [212.4-1340.8] μM for OR, 106.7 [53.6 - 212.1] μM for BC and 386,8 [207.1 - 722.4] μM for GE), were significantly lower (p <0.01, Mann-Whitney) than the values obtained in pre-contraction induced by phenylephrine in the aorta. In Ca2+-free medium in the presence of KCl (60 mM), contractions caused by the addition of Ca2+ were significantly reduced by OR, BC and GE (from 600μM), but when phenylephrine was added instead of K+, there was no decrease in the magnitude of the contractile response. The present study suggests that the vasorelaxant activity of these monoterpenes in rat aorta involves inhibition of voltage-operated calcium channels in the following order of pharmacological potency: BC > GE > OR.
publishDate 2017
dc.date.none.fl_str_mv 2017-03-27T16:20:43Z
2017-03-27T16:20:43Z
2017-02-09
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/masterThesis
format masterThesis
status_str publishedVersion
dc.identifier.uri.fl_str_mv SILVA, A. A. V. Estudo comparativo das ações vasodilatadoras de (+)-Óxido rosa, β-Citronelol e Geraniol em aorta de rato. 2017. 60 f. Dissertação (Mestrado em Farmacologia) - Faculdade de Farmácia, Odontologia e Enfermagem, Universidade Federal do Ceará, Fortaleza, 2017.
http://www.repositorio.ufc.br/handle/riufc/22409
identifier_str_mv SILVA, A. A. V. Estudo comparativo das ações vasodilatadoras de (+)-Óxido rosa, β-Citronelol e Geraniol em aorta de rato. 2017. 60 f. Dissertação (Mestrado em Farmacologia) - Faculdade de Farmácia, Odontologia e Enfermagem, Universidade Federal do Ceará, Fortaleza, 2017.
url http://www.repositorio.ufc.br/handle/riufc/22409
dc.language.iso.fl_str_mv por
language por
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.source.none.fl_str_mv reponame:Repositório Institucional da Universidade Federal do Ceará (UFC)
instname:Universidade Federal do Ceará (UFC)
instacron:UFC
instname_str Universidade Federal do Ceará (UFC)
instacron_str UFC
institution UFC
reponame_str Repositório Institucional da Universidade Federal do Ceará (UFC)
collection Repositório Institucional da Universidade Federal do Ceará (UFC)
repository.name.fl_str_mv Repositório Institucional da Universidade Federal do Ceará (UFC) - Universidade Federal do Ceará (UFC)
repository.mail.fl_str_mv bu@ufc.br || repositorio@ufc.br
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