Mecanismo de ação vasorrelaxante da 6 [(E) estiril] - 2 - pirona extraída da Aniba panurensis (Meisn)Mez(Lauraceae) em ratos
Autor(a) principal: | |
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Data de Publicação: | 2012 |
Tipo de documento: | Tese |
Idioma: | por |
Título da fonte: | Biblioteca Digital de Teses e Dissertações da UFPB |
Texto Completo: | https://repositorio.ufpb.br/jspui/handle/tede/6793 |
Resumo: | The aim of this study was to evaluate the mechanism of vasorrelaxante 6 - [(E) - styryl] - 2 - pyrone (pyrone-198), a natural estirilpirona isolated from the fruit of Aniba panurensis (Meisn.) Mez (Lauraceae), with protocols in normotensive rats in vivo and in vitro on the superior mesenteric artery rings isolated from rats. In non-anesthetized normotensive rats, 198-pyrone (10, 20, 30 and 40 mg / kg; iv) induced bradycardia and hypotension. In the superior mesenteric artery rings isolated from rats pyrone-198 (1 nM - 1 mM) induced relaxation of contractions induced by phenylephrine (Phe, 10 mM) concentration dependent manner and this effect was significantly attenuated after removal of the vascular endothelium. A similar effect occurred in rings pre-contracted with 1 mM of Phe, an effect significantly attenuated after removal of the endothelium. In the presence of 100 mM of L-NAME, 10 M ODQ, 300 mM of PTIO, the relaxation was attenuated. The effect of blocking with L-NAME was completely reversed in preparations with 1 mM L-arginine. In the presence of atropine (1 nM) and indomethacin (10 M), the response induced by pyrone-198 was not changed. The pyrone-198 inhibited contractions induced by increasing concentrations of Phe (1 nM - 1 mM) as well as the relaxation induced contractions induced by U46619 (10 M). In rings pre-contracted with S (-) Bay K8644 (200 nM) caused a relaxation pyrone the like, in rings pre-contracted with Phe (1 and 10 mM) in the presence of nifedipine. The pyrone-198 also interfered in the release of Ca+2 from intracellular stores mediated by Phe (1 and 10 M). In preparations incubated with 3 mM TEA and pre-contracted with 1 M Phe, relaxation of pyrone-198 was not attenuated, unlike the rings incubated with 3 mM TEA and pre-contracted with FEN 10 M. In preparations without endothelium preincubated with 1 mM TEA, relaxation to pyrone-198 was significantly attenuated, however, in the ring without endothelium preincubation with BaCl2 (30 M), 4-AP (1 mM) or GLIB (10 M) did not alter the relaxation induced by pyrone-198. The results suggest the action of pyrone-198 on hemodynamic parameters, alémde vasorrelaxante present a potent effect, an effect mediated in part by endothelium-dependent mechanisms involving via eNOS / CGs. But also by mechanisms independent of the vascular endothelium and the ability to promote relaxation in vascular smooth muscle seems to act interfering with contractile mechanisms subsequent to the entry of calcium, prinicpalmente by inhibiting the release of Ca+2 from intracellular stores sensitive to IP3, and engagement channels sensitive potassium calcium, these effects with different presentation by submaximal and maximal concentrations of phenylephrine. |
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Mecanismo de ação vasorrelaxante da 6 [(E) estiril] - 2 - pirona extraída da Aniba panurensis (Meisn)Mez(Lauraceae) em ratosMechanism of action vasorrelaxante of 6 - [(E) - styryl] - 2 - pyrone extracted from Aniba panurensis (Meisn) Mez (Lauraceae) in ratsAniba panurensisPironaHipotensãoAnéis mesentéricosVasorrelaxamentoeNOS/CGsCálcioFenilefrinaAniba panurensisPyroneHypotensionMesenteric ringsVasorelaxationeNOS / CGsCa2 +PhenylephrineCIENCIAS BIOLOGICAS::FARMACOLOGIAThe aim of this study was to evaluate the mechanism of vasorrelaxante 6 - [(E) - styryl] - 2 - pyrone (pyrone-198), a natural estirilpirona isolated from the fruit of Aniba panurensis (Meisn.) Mez (Lauraceae), with protocols in normotensive rats in vivo and in vitro on the superior mesenteric artery rings isolated from rats. In non-anesthetized normotensive rats, 198-pyrone (10, 20, 30 and 40 mg / kg; iv) induced bradycardia and hypotension. In the superior mesenteric artery rings isolated from rats pyrone-198 (1 nM - 1 mM) induced relaxation of contractions induced by phenylephrine (Phe, 10 mM) concentration dependent manner and this effect was significantly attenuated after removal of the vascular endothelium. A similar effect occurred in rings pre-contracted with 1 mM of Phe, an effect significantly attenuated after removal of the endothelium. In the presence of 100 mM of L-NAME, 10 M ODQ, 300 mM of PTIO, the relaxation was attenuated. The effect of blocking with L-NAME was completely reversed in preparations with 1 mM L-arginine. In the presence of atropine (1 nM) and indomethacin (10 M), the response induced by pyrone-198 was not changed. The pyrone-198 inhibited contractions induced by increasing concentrations of Phe (1 nM - 1 mM) as well as the relaxation induced contractions induced by U46619 (10 M). In rings pre-contracted with S (-) Bay K8644 (200 nM) caused a relaxation pyrone the like, in rings pre-contracted with Phe (1 and 10 mM) in the presence of nifedipine. The pyrone-198 also interfered in the release of Ca+2 from intracellular stores mediated by Phe (1 and 10 M). In preparations incubated with 3 mM TEA and pre-contracted with 1 M Phe, relaxation of pyrone-198 was not attenuated, unlike the rings incubated with 3 mM TEA and pre-contracted with FEN 10 M. In preparations without endothelium preincubated with 1 mM TEA, relaxation to pyrone-198 was significantly attenuated, however, in the ring without endothelium preincubation with BaCl2 (30 M), 4-AP (1 mM) or GLIB (10 M) did not alter the relaxation induced by pyrone-198. The results suggest the action of pyrone-198 on hemodynamic parameters, alémde vasorrelaxante present a potent effect, an effect mediated in part by endothelium-dependent mechanisms involving via eNOS / CGs. But also by mechanisms independent of the vascular endothelium and the ability to promote relaxation in vascular smooth muscle seems to act interfering with contractile mechanisms subsequent to the entry of calcium, prinicpalmente by inhibiting the release of Ca+2 from intracellular stores sensitive to IP3, and engagement channels sensitive potassium calcium, these effects with different presentation by submaximal and maximal concentrations of phenylephrine.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPESO objetivo deste estudo foi avaliar o mecanismo vasorrelaxante da 6 [(E) estiril] - 2 - pirona (pirona-198), uma estirilpirona natural isolada a partir dos frutos de Aniba panurensis (Meisn.) Mez (Lauraceae), com protocolos in vivo em ratos normotensos e in vitro sobre anéis de artéria mesentérica superior isolada de ratos. Em ratos normotensos não anestesiados, pirona-198 (10, 20, 30 e 40 mg/kg, i.v.) induziu hipotensão e bradicardia. Em anéis de artéria mesentérica superior isolada de rato, pirona-198 (1 nM - 1 μM) induziu relaxamento das contrações induzidas por fenilefrina (FEN, 10 μM) de maneira dependente de concentração e esse efeito foi significativamente atenuado após a remoção do endotélio vascular. Efeito semelhante ocorreu em anéis pré-contraidos com 1 μM de FEN 7, efeito significativamente atenuado após a remoção do endotélio. Na presença de 100 μM de L- NAME, 10 M de ODQ, 300 μM de PTIO, o relaxamento foi atenuado. O efeito do bloqueio com L-NAME foi completamente revertido em preparações com 1 mM de L-arginina. Na presença de atropina (1 nM) e indometacina (10 M), a resposta induzida pela pirona-198 não foi alterada. A pirona-198 inibiu contrações induzidas por concentrações crescentes de FEN (1 nM 1 mM), como também induziu relaxamento nas contrações induzidas por U46619 (10 M). Em anéis pré-contraídos com S(-) Bay K8644 (200 nM), a pirona promoveu relaxamento tal como, em anéis pré-contraidos com FEN (1 e 10 μM) na presença de nifedipino. A pirona-198 também interferiu na liberação do Ca+2 dos estoques intracelulares mediado por FEN (1 e 10 M). Em preparações incubadas com TEA 3 mM e pré-contraídas com 1 M FEN, o relaxamento da pirona-198 não foi atenuado, diferentemente dos anéis incubados com TEA 3 mM e pré-contraídos com FEN 10 M. Em preparações sem endotélio pré-incubadas com 1 mM de TEA, o relaxamento para pirona-198 foi significantemente atenuado, entretanto, nos anéis sem endotélio a pré-incubação com BaCl2 (30 M), 4-AP (1 mM) ou GLIB (10 M) não modificou o relaxamento induzido pela pirona-198. Os resultados sugerem a ação da pirona-198 sobre os parâmetros hemodinâmicos, alémde apresentar um potente efeito vasorrelaxante, efeito este mediado parcialmente por mecanismos dependentes do endotélio, envolvendo a via eNOS/CGs. Como também por mecanismos independentes do endotélio vascular e essa capacidade de promover relaxamento no músculo liso vascular parece atuar interferindo em mecanismos contratéis posteriores à entrada de cálcio, prinicpalmente pela inibição da liberação de Ca+2 dos estoques intracelulares sensíveis ao IP3, e envolvimento dos canais de potássio sensíveis ao cálcio, efeitos estes com apresentação diferente mediante as concentrações submáxima e máxima de fenilefrina.Universidade Federal da ParaíbaBRFarmacologiaPrograma de Pós-Graduação em Produtos Naturais e Sintéticos BioativosUFPBMedeiros, Isac Almeida dehttp://lattes.cnpq.br/3412816427200150Assis, Thais Josy Castro Freire de2015-05-14T12:59:54Z2018-07-21T00:26:12Z2014-07-182018-07-21T00:26:12Z2012-08-14info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/doctoralThesisapplication/pdfASSIS, Thais Josy Castro Freire de. Mecanismo de ação vasorrelaxante da 6 [(E) estiril] - 2 - pirona extraída da Aniba panurensis (Meisn)Mez(Lauraceae) em ratos. 2012. 150 f. Tese (Doutorado em Produtos Naturais e Sintéticos Bioativos) - Universidade Federal da Paraíba, João Pessoa, 2012.https://repositorio.ufpb.br/jspui/handle/tede/6793porinfo:eu-repo/semantics/openAccessreponame:Biblioteca Digital de Teses e Dissertações da UFPBinstname:Universidade Federal da Paraíba (UFPB)instacron:UFPB2018-09-06T02:41:24Zoai:repositorio.ufpb.br:tede/6793Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufpb.br/PUBhttp://tede.biblioteca.ufpb.br:8080/oai/requestdiretoria@ufpb.br|| diretoria@ufpb.bropendoar:2018-09-06T02:41:24Biblioteca Digital de Teses e Dissertações da UFPB - Universidade Federal da Paraíba (UFPB)false |
dc.title.none.fl_str_mv |
Mecanismo de ação vasorrelaxante da 6 [(E) estiril] - 2 - pirona extraída da Aniba panurensis (Meisn)Mez(Lauraceae) em ratos Mechanism of action vasorrelaxante of 6 - [(E) - styryl] - 2 - pyrone extracted from Aniba panurensis (Meisn) Mez (Lauraceae) in rats |
title |
Mecanismo de ação vasorrelaxante da 6 [(E) estiril] - 2 - pirona extraída da Aniba panurensis (Meisn)Mez(Lauraceae) em ratos |
spellingShingle |
Mecanismo de ação vasorrelaxante da 6 [(E) estiril] - 2 - pirona extraída da Aniba panurensis (Meisn)Mez(Lauraceae) em ratos Assis, Thais Josy Castro Freire de Aniba panurensis Pirona Hipotensão Anéis mesentéricos Vasorrelaxamento eNOS/CGs Cálcio Fenilefrina Aniba panurensis Pyrone Hypotension Mesenteric rings Vasorelaxation eNOS / CGs Ca2 + Phenylephrine CIENCIAS BIOLOGICAS::FARMACOLOGIA |
title_short |
Mecanismo de ação vasorrelaxante da 6 [(E) estiril] - 2 - pirona extraída da Aniba panurensis (Meisn)Mez(Lauraceae) em ratos |
title_full |
Mecanismo de ação vasorrelaxante da 6 [(E) estiril] - 2 - pirona extraída da Aniba panurensis (Meisn)Mez(Lauraceae) em ratos |
title_fullStr |
Mecanismo de ação vasorrelaxante da 6 [(E) estiril] - 2 - pirona extraída da Aniba panurensis (Meisn)Mez(Lauraceae) em ratos |
title_full_unstemmed |
Mecanismo de ação vasorrelaxante da 6 [(E) estiril] - 2 - pirona extraída da Aniba panurensis (Meisn)Mez(Lauraceae) em ratos |
title_sort |
Mecanismo de ação vasorrelaxante da 6 [(E) estiril] - 2 - pirona extraída da Aniba panurensis (Meisn)Mez(Lauraceae) em ratos |
author |
Assis, Thais Josy Castro Freire de |
author_facet |
Assis, Thais Josy Castro Freire de |
author_role |
author |
dc.contributor.none.fl_str_mv |
Medeiros, Isac Almeida de http://lattes.cnpq.br/3412816427200150 |
dc.contributor.author.fl_str_mv |
Assis, Thais Josy Castro Freire de |
dc.subject.por.fl_str_mv |
Aniba panurensis Pirona Hipotensão Anéis mesentéricos Vasorrelaxamento eNOS/CGs Cálcio Fenilefrina Aniba panurensis Pyrone Hypotension Mesenteric rings Vasorelaxation eNOS / CGs Ca2 + Phenylephrine CIENCIAS BIOLOGICAS::FARMACOLOGIA |
topic |
Aniba panurensis Pirona Hipotensão Anéis mesentéricos Vasorrelaxamento eNOS/CGs Cálcio Fenilefrina Aniba panurensis Pyrone Hypotension Mesenteric rings Vasorelaxation eNOS / CGs Ca2 + Phenylephrine CIENCIAS BIOLOGICAS::FARMACOLOGIA |
description |
The aim of this study was to evaluate the mechanism of vasorrelaxante 6 - [(E) - styryl] - 2 - pyrone (pyrone-198), a natural estirilpirona isolated from the fruit of Aniba panurensis (Meisn.) Mez (Lauraceae), with protocols in normotensive rats in vivo and in vitro on the superior mesenteric artery rings isolated from rats. In non-anesthetized normotensive rats, 198-pyrone (10, 20, 30 and 40 mg / kg; iv) induced bradycardia and hypotension. In the superior mesenteric artery rings isolated from rats pyrone-198 (1 nM - 1 mM) induced relaxation of contractions induced by phenylephrine (Phe, 10 mM) concentration dependent manner and this effect was significantly attenuated after removal of the vascular endothelium. A similar effect occurred in rings pre-contracted with 1 mM of Phe, an effect significantly attenuated after removal of the endothelium. In the presence of 100 mM of L-NAME, 10 M ODQ, 300 mM of PTIO, the relaxation was attenuated. The effect of blocking with L-NAME was completely reversed in preparations with 1 mM L-arginine. In the presence of atropine (1 nM) and indomethacin (10 M), the response induced by pyrone-198 was not changed. The pyrone-198 inhibited contractions induced by increasing concentrations of Phe (1 nM - 1 mM) as well as the relaxation induced contractions induced by U46619 (10 M). In rings pre-contracted with S (-) Bay K8644 (200 nM) caused a relaxation pyrone the like, in rings pre-contracted with Phe (1 and 10 mM) in the presence of nifedipine. The pyrone-198 also interfered in the release of Ca+2 from intracellular stores mediated by Phe (1 and 10 M). In preparations incubated with 3 mM TEA and pre-contracted with 1 M Phe, relaxation of pyrone-198 was not attenuated, unlike the rings incubated with 3 mM TEA and pre-contracted with FEN 10 M. In preparations without endothelium preincubated with 1 mM TEA, relaxation to pyrone-198 was significantly attenuated, however, in the ring without endothelium preincubation with BaCl2 (30 M), 4-AP (1 mM) or GLIB (10 M) did not alter the relaxation induced by pyrone-198. The results suggest the action of pyrone-198 on hemodynamic parameters, alémde vasorrelaxante present a potent effect, an effect mediated in part by endothelium-dependent mechanisms involving via eNOS / CGs. But also by mechanisms independent of the vascular endothelium and the ability to promote relaxation in vascular smooth muscle seems to act interfering with contractile mechanisms subsequent to the entry of calcium, prinicpalmente by inhibiting the release of Ca+2 from intracellular stores sensitive to IP3, and engagement channels sensitive potassium calcium, these effects with different presentation by submaximal and maximal concentrations of phenylephrine. |
publishDate |
2012 |
dc.date.none.fl_str_mv |
2012-08-14 2014-07-18 2015-05-14T12:59:54Z 2018-07-21T00:26:12Z 2018-07-21T00:26:12Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/doctoralThesis |
format |
doctoralThesis |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
ASSIS, Thais Josy Castro Freire de. Mecanismo de ação vasorrelaxante da 6 [(E) estiril] - 2 - pirona extraída da Aniba panurensis (Meisn)Mez(Lauraceae) em ratos. 2012. 150 f. Tese (Doutorado em Produtos Naturais e Sintéticos Bioativos) - Universidade Federal da Paraíba, João Pessoa, 2012. https://repositorio.ufpb.br/jspui/handle/tede/6793 |
identifier_str_mv |
ASSIS, Thais Josy Castro Freire de. Mecanismo de ação vasorrelaxante da 6 [(E) estiril] - 2 - pirona extraída da Aniba panurensis (Meisn)Mez(Lauraceae) em ratos. 2012. 150 f. Tese (Doutorado em Produtos Naturais e Sintéticos Bioativos) - Universidade Federal da Paraíba, João Pessoa, 2012. |
url |
https://repositorio.ufpb.br/jspui/handle/tede/6793 |
dc.language.iso.fl_str_mv |
por |
language |
por |
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info:eu-repo/semantics/openAccess |
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openAccess |
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application/pdf |
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Universidade Federal da Paraíba BR Farmacologia Programa de Pós-Graduação em Produtos Naturais e Sintéticos Bioativos UFPB |
publisher.none.fl_str_mv |
Universidade Federal da Paraíba BR Farmacologia Programa de Pós-Graduação em Produtos Naturais e Sintéticos Bioativos UFPB |
dc.source.none.fl_str_mv |
reponame:Biblioteca Digital de Teses e Dissertações da UFPB instname:Universidade Federal da Paraíba (UFPB) instacron:UFPB |
instname_str |
Universidade Federal da Paraíba (UFPB) |
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UFPB |
institution |
UFPB |
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Biblioteca Digital de Teses e Dissertações da UFPB |
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Biblioteca Digital de Teses e Dissertações da UFPB |
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Biblioteca Digital de Teses e Dissertações da UFPB - Universidade Federal da Paraíba (UFPB) |
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diretoria@ufpb.br|| diretoria@ufpb.br |
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1801842917744050176 |