Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase)

Detalhes bibliográficos
Ano de defesa: 2015
Autor(a) principal: Recalde Gil, Maria Angélica
Orientador(a): Henriques, Amelia Teresinha
Banca de defesa: Não Informado pela instituição
Tipo de documento: Dissertação
Tipo de acesso: Acesso aberto
Idioma: por
Instituição de defesa: Não Informado pela instituição
Programa de Pós-Graduação: Não Informado pela instituição
Departamento: Não Informado pela instituição
País: Não Informado pela instituição
Palavras-chave em Português:
Farmácia
Palavras-chave em Inglês:
Garcinia gardneriana
Biflavonoids
Aromatase
Monoamine oxidase inhibitors
Palavras-chave em Espanhol:
Biflavonoides
Aromatasa
Monoaminooxidasa
Inhibidores
Link de acesso: http://hdl.handle.net/10183/149485
Resumo: The plant Garcinia gardneriana (Planch. & Triana) Zappi, popularly known in Brazil as "bacupari" has traditionally been used for various types of inflammatory diseases and the evaluation of their chemical composition, mainly of leaves, has resulted in biflavonoids as major compounds. These phenolic compounds have shown anti-inflammatory activity validating the popular use of the plant. In this work was isolated from dried branches of Garcinia gardneriana the biflavonoids: morelloflavone, that is an naringenin covalently linked to luteolin, Gb-2a which is an naringenin linked to eriodictyol and Gb-2a- 7-O-glucose. These compounds have been previously evaluated in various activities such as anti-inflammatory and anti-antioxidants but there is no report of its activity as enzymatic inhibitors. However, the monomers that form it, have been evaluated in the inhibition of aromatase and antidepressant activity with positive outcome, which commonly are used MAO-A inhibitors. In the isolation process were also founded terpenoid compounds as lupeol and friedelin The isolated and purified biflavonoids were used to evaluate enzyme inhibition "in vitro" in monoamine oxidases (MAO-A MAO-B) and aromatase. The compounds showed a positive response even of IC50 5,47 μM and 1,35 μM for MAO-A inhibition of and aromatase enzyme respectively; discovering a way for a new proposal to link both enzymes for treatment of hormone-dependent cancers and anxiety and depression disorders.
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spelling Recalde Gil, Maria AngélicaHenriques, Amelia Teresinha2016-11-08T02:13:05Z2015http://hdl.handle.net/10183/149485001004061The plant Garcinia gardneriana (Planch. & Triana) Zappi, popularly known in Brazil as "bacupari" has traditionally been used for various types of inflammatory diseases and the evaluation of their chemical composition, mainly of leaves, has resulted in biflavonoids as major compounds. These phenolic compounds have shown anti-inflammatory activity validating the popular use of the plant. In this work was isolated from dried branches of Garcinia gardneriana the biflavonoids: morelloflavone, that is an naringenin covalently linked to luteolin, Gb-2a which is an naringenin linked to eriodictyol and Gb-2a- 7-O-glucose. These compounds have been previously evaluated in various activities such as anti-inflammatory and anti-antioxidants but there is no report of its activity as enzymatic inhibitors. However, the monomers that form it, have been evaluated in the inhibition of aromatase and antidepressant activity with positive outcome, which commonly are used MAO-A inhibitors. In the isolation process were also founded terpenoid compounds as lupeol and friedelin The isolated and purified biflavonoids were used to evaluate enzyme inhibition "in vitro" in monoamine oxidases (MAO-A MAO-B) and aromatase. The compounds showed a positive response even of IC50 5,47 μM and 1,35 μM for MAO-A inhibition of and aromatase enzyme respectively; discovering a way for a new proposal to link both enzymes for treatment of hormone-dependent cancers and anxiety and depression disorders.La planta Garcinia gardneriana (Planch. & Triana) Zappi, popularmente conocida en Brasil como "bacupari" ha sido tradicionalmente usada para varios tipos de enfermedades inflamatorias y la evaluación de su composición química, principalmente de las hojas, ha resultado en biflavonoides como compuestos mayoritarios. Estos compuestos fenólicos han demostrado actividad anti-inflamatória validando el uso popular de la planta. En este trabajo se asilaron a partir de tallos secos de la Garcinia gardneriana los biflavonoides: moreloflavona, que consiste en una naringenina unida covalentemente a luteolina, Gb-2a que es un compuesto que consiste en una naringenina unida a un eriodictyol y Gb-2a-7-O-glucose. Estos compuestos ya han sido previamente evaluados en diversas actividades como anti inflamatorios y anti antioxidantes pero no se tiene reporte de su actividad como inhibidores enzimáticos. Sin embargo, los monomeros que los conforman han sido evaluados en la inhibición de la aromatasa y con resultados positivos como en la actividad antidepresiva, para la cual comúnmente son usados los inibidores de MAO-A. En el proceso de aislamiento también fueron encontrados compuestos terpenoides como lupeol y friedelina. Los biflavonoides aislados y purificados se usaron para evaluar la inhibición enzimática “in vitro” en monoaminooxidasas (MAO-A, MAO-B) y aromatasa. Los compuestos presentaron una respuesta positiva calculada con IC50 de hasta 5,47 μM y 1,35 μM para la inhibición de las enzimas MAO-A y aromatasa respectivamente, abriendo el camino a una nueva propuesta de relacionar estas dos enzimas para tratamiento de cánceres hormonodependientes y transtornos de ansiedad y depresión.application/pdfporFarmáciaGarcinia gardnerianaBiflavonoidsAromataseMonoamine oxidase inhibitorsBiflavonoidesAromatasaMonoaminooxidasaInhibidoresPotencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase)info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisUniversidade Federal do Rio Grande do SulFaculdade de FarmáciaPrograma de Pós-Graduação em Ciências FarmacêuticasPorto Alegre, BR-RS2015mestradoinfo:eu-repo/semantics/openAccessreponame:Biblioteca Digital de Teses e Dissertações da UFRGSinstname:Universidade Federal do Rio Grande do Sul (UFRGS)instacron:UFRGSTEXT001004061.pdf.txt001004061.pdf.txtExtracted Texttext/plain72530http://www.lume.ufrgs.br/bitstream/10183/149485/2/001004061.pdf.txtcf512cf2edae1eed92af0da5843f99dcMD52ORIGINAL001004061.pdf001004061.pdfTexto completoapplication/pdf1080996http://www.lume.ufrgs.br/bitstream/10183/149485/1/001004061.pdf3a9789605e8233abca692e31c01b1d35MD5110183/1494852019-12-11 04:58:03.413929oai:www.lume.ufrgs.br:10183/149485Biblioteca Digital de Teses e Dissertaçõeshttps://lume.ufrgs.br/handle/10183/2PUBhttps://lume.ufrgs.br/oai/requestlume@ufrgs.br||lume@ufrgs.bropendoar:18532019-12-11T06:58:03Biblioteca Digital de Teses e Dissertações da UFRGS - Universidade Federal do Rio Grande do Sul (UFRGS)false
dc.title.pt_BR.fl_str_mv Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase)
title Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase)
spellingShingle Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase)
Recalde Gil, Maria Angélica
Farmácia
Garcinia gardneriana
Biflavonoids
Aromatase
Monoamine oxidase inhibitors
Biflavonoides
Aromatasa
Monoaminooxidasa
Inhibidores
title_short Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase)
title_full Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase)
title_fullStr Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase)
title_full_unstemmed Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase)
title_sort Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase)
author Recalde Gil, Maria Angélica
author_facet Recalde Gil, Maria Angélica
author_role author
dc.contributor.author.fl_str_mv Recalde Gil, Maria Angélica
dc.contributor.advisor1.fl_str_mv Henriques, Amelia Teresinha
contributor_str_mv Henriques, Amelia Teresinha
dc.subject.por.fl_str_mv Farmácia
topic Farmácia
Garcinia gardneriana
Biflavonoids
Aromatase
Monoamine oxidase inhibitors
Biflavonoides
Aromatasa
Monoaminooxidasa
Inhibidores
dc.subject.eng.fl_str_mv Garcinia gardneriana
Biflavonoids
Aromatase
Monoamine oxidase inhibitors
dc.subject.spa.fl_str_mv Biflavonoides
Aromatasa
Monoaminooxidasa
Inhibidores
description The plant Garcinia gardneriana (Planch. & Triana) Zappi, popularly known in Brazil as "bacupari" has traditionally been used for various types of inflammatory diseases and the evaluation of their chemical composition, mainly of leaves, has resulted in biflavonoids as major compounds. These phenolic compounds have shown anti-inflammatory activity validating the popular use of the plant. In this work was isolated from dried branches of Garcinia gardneriana the biflavonoids: morelloflavone, that is an naringenin covalently linked to luteolin, Gb-2a which is an naringenin linked to eriodictyol and Gb-2a- 7-O-glucose. These compounds have been previously evaluated in various activities such as anti-inflammatory and anti-antioxidants but there is no report of its activity as enzymatic inhibitors. However, the monomers that form it, have been evaluated in the inhibition of aromatase and antidepressant activity with positive outcome, which commonly are used MAO-A inhibitors. In the isolation process were also founded terpenoid compounds as lupeol and friedelin The isolated and purified biflavonoids were used to evaluate enzyme inhibition "in vitro" in monoamine oxidases (MAO-A MAO-B) and aromatase. The compounds showed a positive response even of IC50 5,47 μM and 1,35 μM for MAO-A inhibition of and aromatase enzyme respectively; discovering a way for a new proposal to link both enzymes for treatment of hormone-dependent cancers and anxiety and depression disorders.
publishDate 2015
dc.date.issued.fl_str_mv 2015
dc.date.accessioned.fl_str_mv 2016-11-08T02:13:05Z
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identifier_str_mv 001004061
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