Inhibition of intracellular Ca2+ mobilization and potassium channels activation are involved in the vasorelaxation induced by 7-hydroxycoumarin
| Autor(a) principal: | |
|---|---|
| Data de Publicação: | 2020 |
| Outros Autores: | , , , , , , , |
| Tipo de documento: | Artigo |
| Idioma: | eng |
| Título da fonte: | Repositório Institucional da FIOCRUZ (ARCA) |
| Texto Completo: | https://www.arca.fiocruz.br/handle/icict/44667 |
Resumo: | National Council for Scientific and Technological Development (CNPq) 306106/2017–5 and Coordination for the Improvement of Higher Education Personnel (CAPES) - Finance Code 001. We acknowledge the computational support from SCC1 (Boston University) and technical support from Pedro S. Lacerda. |
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Alves, Quiara LovattiMoraes, Raiana dos AnjosFroes, Thamires QuadrosCastilho, Marcelo SantosAraújo, Rodrigo Santos Aquino deBarbosa Filho, José MariaMeira, Cássio SantanaSoares, Milena Botelho PereiraSilva, Darízy Flávia2020-11-30T12:18:34Z2020-11-30T12:18:34Z2020ALVES, Quiara Lovatti et al. Inhibition of intracellular Ca2+ mobilization and potassium channels activation are involved in the vasorelaxation induced by 7-hydroxycoumarin. European Journal of Pharmacology, v. 887, p. 173525, 2020.0014-2999https://www.arca.fiocruz.br/handle/icict/4466710.1016/j.ejphar.2020.173525National Council for Scientific and Technological Development (CNPq) 306106/2017–5 and Coordination for the Improvement of Higher Education Personnel (CAPES) - Finance Code 001. We acknowledge the computational support from SCC1 (Boston University) and technical support from Pedro S. Lacerda.Federal University of Bahia. Laboratory of Cardiovascular Physiology and Pharmacology. Salvador, BA, Brazil / Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil.Federal University of Bahia. Laboratory of Cardiovascular Physiology and Pharmacology. Salvador, BA, Brazil / Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil.Federal University of Bahia. Faculty of Pharmacy. Laboratory of Bioinformatics and Molecular Modeling, Salvador, BA, Brazil.Federal University of Bahia. Faculty of Pharmacy. Laboratory of Bioinformatics and Molecular Modeling, Salvador, BA, Brazil.Federal University of Paraíba. Laboratory of Pharmaceutical Technology. Department of Physiology and Pathology. João Pessoa, PB, Brazil.Federal University of Paraíba. Laboratory of Pharmaceutical Technology. Department of Physiology and Pathology. João Pessoa, PB, Brazil.Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil.Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil.Federal University of Bahia. Laboratory of Cardiovascular Physiology and Pharmacology. Salvador, BA, Brazil / Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil.Coumarins exhibit a wide variety of biological effects, including activities in the cardiovascular system and the aim of this study was to evaluate the vascular therapeutic potential of 7-Hydroxicoumarin (7-HC). The vascular effects induced by 7-HC (0.001 μM–300 μM), were investigated by in vitro approaches using isometric tension measurements in rat superior mesenteric arteries and by in silico assays using Ligand-based analysis. Our results suggest that the vasorelaxant effect of 7-HC seems to rely on potassium channels, notably through large conductance Ca2+-activated K+ (BKCa) channels activation. In fact, 7-HC (300 μM) significantly reduced CaCl2- induced contraction as well as the reduction of intracellular calcium mobilization. However, the relaxation induced by 7-HC was independent of store-operated calcium entry (SOCE). Moreover, in silico analysis suggests that potassium channels have a common binding pocket, where 7-HC may bind and hint that its binding profile is more similar to quinine’s than verapamil’s. These results are compatible with the inhibition of Ca2+ release from intracellular stores, which is prompted by phenylephrine and caffeine. Taken together, these results demonstrate a therapeutic potential of 7-HC on the cardiovascular system, making it a promising lead compound for the development of drugs useful in the treatment of cardiovascular diseases.engElsevierCumarinasVasorrelaxamentoCanais KDoenças cardiovasculares.7-HydroxycoumarinVasorelaxationK+ channelsFTMapDockingInhibition of intracellular Ca2+ mobilization and potassium channels activation are involved in the vasorelaxation induced by 7-hydroxycoumarininfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-83097https://www.arca.fiocruz.br/bitstream/icict/44667/1/license.txt36b51ef91c52b5338d9d29ba0cc807bcMD51ORIGINALAlves Quiara Lovatti Inhibition...2020.pdfAlves Quiara Lovatti 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| dc.title.pt_BR.fl_str_mv |
Inhibition of intracellular Ca2+ mobilization and potassium channels activation are involved in the vasorelaxation induced by 7-hydroxycoumarin |
| title |
Inhibition of intracellular Ca2+ mobilization and potassium channels activation are involved in the vasorelaxation induced by 7-hydroxycoumarin |
| spellingShingle |
Inhibition of intracellular Ca2+ mobilization and potassium channels activation are involved in the vasorelaxation induced by 7-hydroxycoumarin Alves, Quiara Lovatti Cumarinas Vasorrelaxamento Canais K Doenças cardiovasculares. 7-Hydroxycoumarin Vasorelaxation K+ channels FTMap Docking |
| title_short |
Inhibition of intracellular Ca2+ mobilization and potassium channels activation are involved in the vasorelaxation induced by 7-hydroxycoumarin |
| title_full |
Inhibition of intracellular Ca2+ mobilization and potassium channels activation are involved in the vasorelaxation induced by 7-hydroxycoumarin |
| title_fullStr |
Inhibition of intracellular Ca2+ mobilization and potassium channels activation are involved in the vasorelaxation induced by 7-hydroxycoumarin |
| title_full_unstemmed |
Inhibition of intracellular Ca2+ mobilization and potassium channels activation are involved in the vasorelaxation induced by 7-hydroxycoumarin |
| title_sort |
Inhibition of intracellular Ca2+ mobilization and potassium channels activation are involved in the vasorelaxation induced by 7-hydroxycoumarin |
| author |
Alves, Quiara Lovatti |
| author_facet |
Alves, Quiara Lovatti Moraes, Raiana dos Anjos Froes, Thamires Quadros Castilho, Marcelo Santos Araújo, Rodrigo Santos Aquino de Barbosa Filho, José Maria Meira, Cássio Santana Soares, Milena Botelho Pereira Silva, Darízy Flávia |
| author_role |
author |
| author2 |
Moraes, Raiana dos Anjos Froes, Thamires Quadros Castilho, Marcelo Santos Araújo, Rodrigo Santos Aquino de Barbosa Filho, José Maria Meira, Cássio Santana Soares, Milena Botelho Pereira Silva, Darízy Flávia |
| author2_role |
author author author author author author author author |
| dc.contributor.author.fl_str_mv |
Alves, Quiara Lovatti Moraes, Raiana dos Anjos Froes, Thamires Quadros Castilho, Marcelo Santos Araújo, Rodrigo Santos Aquino de Barbosa Filho, José Maria Meira, Cássio Santana Soares, Milena Botelho Pereira Silva, Darízy Flávia |
| dc.subject.other.pt_BR.fl_str_mv |
Cumarinas Vasorrelaxamento Canais K Doenças cardiovasculares. |
| topic |
Cumarinas Vasorrelaxamento Canais K Doenças cardiovasculares. 7-Hydroxycoumarin Vasorelaxation K+ channels FTMap Docking |
| dc.subject.en.pt_BR.fl_str_mv |
7-Hydroxycoumarin Vasorelaxation K+ channels FTMap Docking |
| description |
National Council for Scientific and Technological Development (CNPq) 306106/2017–5 and Coordination for the Improvement of Higher Education Personnel (CAPES) - Finance Code 001. We acknowledge the computational support from SCC1 (Boston University) and technical support from Pedro S. Lacerda. |
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2020 |
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2020-11-30T12:18:34Z |
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2020-11-30T12:18:34Z |
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2020 |
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info:eu-repo/semantics/publishedVersion |
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info:eu-repo/semantics/article |
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publishedVersion |
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ALVES, Quiara Lovatti et al. Inhibition of intracellular Ca2+ mobilization and potassium channels activation are involved in the vasorelaxation induced by 7-hydroxycoumarin. European Journal of Pharmacology, v. 887, p. 173525, 2020. |
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https://www.arca.fiocruz.br/handle/icict/44667 |
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0014-2999 |
| dc.identifier.doi.none.fl_str_mv |
10.1016/j.ejphar.2020.173525 |
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ALVES, Quiara Lovatti et al. Inhibition of intracellular Ca2+ mobilization and potassium channels activation are involved in the vasorelaxation induced by 7-hydroxycoumarin. European Journal of Pharmacology, v. 887, p. 173525, 2020. 0014-2999 10.1016/j.ejphar.2020.173525 |
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