(E)-2-styrylchromones: synthesis and evaluation of the inhibitory effects on the oxidative burst produced by human monocytes

• Autor(a) principal: Correia, Catarina Marçal
• 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
• topic: Oxidative stress; Inflammation; Human monocytes; Polyphenols; (E)-2-styrylchromones; Antioxidant activity; Anti-inflammatory activity; Oxidative burst; Flow cytometry

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.