(E)-2-styrylchromones: synthesis and evaluation of the inhibitory effects on the oxidative burst produced by human monocytes
Autor(a) principal: | |
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Data de Publicação: | 2021 |
Tipo de documento: | Dissertação |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | http://hdl.handle.net/10773/33584 |
Resumo: | Several studies have attributed the onset and progression of several diseases, including degenerative and cardiovascular diseases, cell aging and cancer, to the production of free radicals and inflammatory processes. Consequently, a large number of investigations have been carried out in order to find new, safer and potent antioxidant and anti-inflammatory drugs, and to elucidate their corresponding mechanisms of action. The evaluation of antioxidant vs antiradicalar and anti-inflammatory activity of phenolic compounds, either of natural or synthetic origin, is nowadays an important area of research in the field of medicinal chemistry. This work presents a brief introduction about oxidative stress and the origin of reactive oxygen and nitrogen species, and about inflammation and the cells involved in this process, specifically monocytes. The relationship between the inflammatory process and the oxidative burst produced by human monocytes is addressed. Polyphenols, secondary metabolites of several plants, are recognized as an important source of flavonoids, including 2-styrylchromones, which have demonstrated important biological activities. Thus, several examples of (E)-2- styrylchromones of natural and synthetic origin and the biological activities associated with them are presented herein, with emphasis on antioxidant and anti-inflammatory activities. The major goal of this work relies on the design and synthesis of a library of nine (E)-2-styrylchromones and their inhibitory effects on the oxidative burst produced by human monocytes and the establishment of structure-activity relationship studies (SARS). At last, the most used methods for the synthesis of (E)-2-styrylchromones containing relevant substituent groups to their antioxidant and anti-inflammatory activity, namely hydroxyl and halogen groups, as well as the procedures for the in chemico and in vitro biological assays, are described. |
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(E)-2-styrylchromones: synthesis and evaluation of the inhibitory effects on the oxidative burst produced by human monocytesOxidative stressInflammationHuman monocytesPolyphenols(E)-2-styrylchromonesAntioxidant activityAnti-inflammatory activityOxidative burstFlow cytometrySeveral studies have attributed the onset and progression of several diseases, including degenerative and cardiovascular diseases, cell aging and cancer, to the production of free radicals and inflammatory processes. Consequently, a large number of investigations have been carried out in order to find new, safer and potent antioxidant and anti-inflammatory drugs, and to elucidate their corresponding mechanisms of action. The evaluation of antioxidant vs antiradicalar and anti-inflammatory activity of phenolic compounds, either of natural or synthetic origin, is nowadays an important area of research in the field of medicinal chemistry. This work presents a brief introduction about oxidative stress and the origin of reactive oxygen and nitrogen species, and about inflammation and the cells involved in this process, specifically monocytes. The relationship between the inflammatory process and the oxidative burst produced by human monocytes is addressed. Polyphenols, secondary metabolites of several plants, are recognized as an important source of flavonoids, including 2-styrylchromones, which have demonstrated important biological activities. Thus, several examples of (E)-2- styrylchromones of natural and synthetic origin and the biological activities associated with them are presented herein, with emphasis on antioxidant and anti-inflammatory activities. The major goal of this work relies on the design and synthesis of a library of nine (E)-2-styrylchromones and their inhibitory effects on the oxidative burst produced by human monocytes and the establishment of structure-activity relationship studies (SARS). At last, the most used methods for the synthesis of (E)-2-styrylchromones containing relevant substituent groups to their antioxidant and anti-inflammatory activity, namely hydroxyl and halogen groups, as well as the procedures for the in chemico and in vitro biological assays, are described.O aparecimento e progressão de várias doenças, incluindo doenças neurodegenerativas, cardiovasculares, envelhecimento celular e cancro, têm sido associados à produção de radicais livres assim como a processos inflamatórios, de acordo com vários estudos realizados. Por conseguinte, têm sido realizadas diversas investigações com a finalidade de encontrar novos fármacos com potencial antioxidante e anti-inflamatório, mais eficazes e seguros, e de compreender os seus mecanismos de ação. Atualmente, a avaliação da atividade antioxidante e/ou antirradicalar e anti-inflamatória de compostos polifenólicos, classe de compostos onde se incluem as 2- estirilcromonas, quer de origem natural quer sintéticos, é uma área de estudo de grande interesse. Neste trabalho apresenta-se uma breve introdução sobre o stress oxidativo e a origem das espécies reativas de oxigénio e nitrogénio e sobre a inflamação e as células intervenientes neste processo, mais especificamente, acerca dos monócitos. Aborda-se a relação entre o processo inflamatório e o burst oxidativo produzido por monócitos humanos. Os polifenóis, metabolitos secundários de várias plantas, são reconhecidos como uma fonte importante de flavonóides, incluindo 2-estirilcromonas, que têm demonstrado importantes atividades biológicas. Seguidamente são apresentados vários exemplos de (E)-2-estirilcromonas de origem natural e sintética e as atividades biológicas que lhes estão associadas, destacando-se as atividades antioxidantes e anti-inflamatórias. O grande foco deste trabalho reside no desenho e síntese de um painel de nove (E)-2-estirilcromonas e o seu efeito inibitório no burst oxidativo produzido por monócitos humanos e ainda o estudo da relação estrutura-atividade (SARS). Por fim, são descritos os métodos mais utilizados para a síntese de (E)-2-estirilcromonas contendo grupos substituintes relevantes para a sua atividade antioxidante e antiinflamatória, nomeadamente grupos hidroxilo e halogéneos, assim como os métodos utilizados nos ensaios in chemico e in vitro.2023-12-26T00:00:00Z2021-12-14T00:00:00Z2021-12-14info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfhttp://hdl.handle.net/10773/33584engCorreia, Catarina Marçalinfo:eu-repo/semantics/embargoedAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2024-02-22T12:04:39Zoai:ria.ua.pt:10773/33584Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-20T03:04:59.939287Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse |
dc.title.none.fl_str_mv |
(E)-2-styrylchromones: synthesis and evaluation of the inhibitory effects on the oxidative burst produced by human monocytes |
title |
(E)-2-styrylchromones: synthesis and evaluation of the inhibitory effects on the oxidative burst produced by human monocytes |
spellingShingle |
(E)-2-styrylchromones: synthesis and evaluation of the inhibitory effects on the oxidative burst produced by human monocytes Correia, Catarina Marçal Oxidative stress Inflammation Human monocytes Polyphenols (E)-2-styrylchromones Antioxidant activity Anti-inflammatory activity Oxidative burst Flow cytometry |
title_short |
(E)-2-styrylchromones: synthesis and evaluation of the inhibitory effects on the oxidative burst produced by human monocytes |
title_full |
(E)-2-styrylchromones: synthesis and evaluation of the inhibitory effects on the oxidative burst produced by human monocytes |
title_fullStr |
(E)-2-styrylchromones: synthesis and evaluation of the inhibitory effects on the oxidative burst produced by human monocytes |
title_full_unstemmed |
(E)-2-styrylchromones: synthesis and evaluation of the inhibitory effects on the oxidative burst produced by human monocytes |
title_sort |
(E)-2-styrylchromones: synthesis and evaluation of the inhibitory effects on the oxidative burst produced by human monocytes |
author |
Correia, Catarina Marçal |
author_facet |
Correia, Catarina Marçal |
author_role |
author |
dc.contributor.author.fl_str_mv |
Correia, Catarina Marçal |
dc.subject.por.fl_str_mv |
Oxidative stress Inflammation Human monocytes Polyphenols (E)-2-styrylchromones Antioxidant activity Anti-inflammatory activity Oxidative burst Flow cytometry |
topic |
Oxidative stress Inflammation Human monocytes Polyphenols (E)-2-styrylchromones Antioxidant activity Anti-inflammatory activity Oxidative burst Flow cytometry |
description |
Several studies have attributed the onset and progression of several diseases, including degenerative and cardiovascular diseases, cell aging and cancer, to the production of free radicals and inflammatory processes. Consequently, a large number of investigations have been carried out in order to find new, safer and potent antioxidant and anti-inflammatory drugs, and to elucidate their corresponding mechanisms of action. The evaluation of antioxidant vs antiradicalar and anti-inflammatory activity of phenolic compounds, either of natural or synthetic origin, is nowadays an important area of research in the field of medicinal chemistry. This work presents a brief introduction about oxidative stress and the origin of reactive oxygen and nitrogen species, and about inflammation and the cells involved in this process, specifically monocytes. The relationship between the inflammatory process and the oxidative burst produced by human monocytes is addressed. Polyphenols, secondary metabolites of several plants, are recognized as an important source of flavonoids, including 2-styrylchromones, which have demonstrated important biological activities. Thus, several examples of (E)-2- styrylchromones of natural and synthetic origin and the biological activities associated with them are presented herein, with emphasis on antioxidant and anti-inflammatory activities. The major goal of this work relies on the design and synthesis of a library of nine (E)-2-styrylchromones and their inhibitory effects on the oxidative burst produced by human monocytes and the establishment of structure-activity relationship studies (SARS). At last, the most used methods for the synthesis of (E)-2-styrylchromones containing relevant substituent groups to their antioxidant and anti-inflammatory activity, namely hydroxyl and halogen groups, as well as the procedures for the in chemico and in vitro biological assays, are described. |
publishDate |
2021 |
dc.date.none.fl_str_mv |
2021-12-14T00:00:00Z 2021-12-14 2023-12-26T00:00:00Z |
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 |
http://hdl.handle.net/10773/33584 |
url |
http://hdl.handle.net/10773/33584 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
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info:eu-repo/semantics/embargoedAccess |
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application/pdf |
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Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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RCAAP |
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RCAAP |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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