Revisão bibliográfica: síntese de derivados de anti-inflamatórios não esteroides (não doadores e doadores de óxido nítrico) e seus mecanismos de ação envolvendo a ciclooxigenase (cox) como agentes antitumorais
Data
2021-12-14
Autores
Marcon, Angela Favero [UNIFESP]
Orientadores
Reis, Adriana Karla [UNIFESP]
Tipo
Trabalho de conclusão de curso de graduação
Título da Revista
ISSN da Revista
Título de Volume
Resumo
Os anti-inflamatórios não esteroides (AINEs) são uma classe de anti-inflamatórios de extrema importância no tratamento de sintomas causados por inflamações, sejam elas provocadas por bactérias ou vírus. Eles atuam na inibição da enzima ciclooxigenase (COX), encarregada de produzir prostanoides, principalmente prostaglandinas, substâncias presentes nos tecidos inflamados e que são responsáveis pelos sintomas originados no processo inflamatório. Essa enzima possui duas isoformas conhecidas, sendo uma delas a responsável pela manutenção da integridade da mucosa gastrointestinal (COX-1), enquanto a outra (COX-2) está presente nos tecidos afetados pela inflamação e é responsável pela produção das prostaglandinas presentes neles. Sabendo-se que o câncer é um processo inflamatório e que tecidos afetados por ele expressam a isoforma COX-2, a inibição de COX pode ser de grande ajuda no tratamento dessa patologia. Entretanto, os AINEs não possuem inibição específica, podendo inibir tanto a COX-2 quanto a COX-1, o que dá origem aos efeitos colaterais gastrointestinais ligados ao uso constante de anti-inflamatórios. Nesta revisão bibliográfica, daremos ênfase na busca de artigos, através das plataformas SciFinder e PubMed, que possuam diferentes métodos sintéticos de derivados de AINEs inibidores específicos de COX-2 e não de COX-1, diminuindo seus efeitos colaterais e podendo, assim, serem usados como agentes antitumorais.
Non-steroidal anti-inflammatory drugs (NSAIDs) are a class of anti-inflammatory drugs that are extremely important in the treatment of outcomes caused by inflammation, whether caused by bacteria or viruses. They act by inhibiting the cyclooxygenase (COX) enzyme, which is responsible for producing prostanoids, mainly prostaglandins, substances present in inflamed tissues and which are responsible for the symptoms originated in the inflammatory process. This enzyme has two isoforms, one of which is responsible for maintaining the integrity of the gastrointestinal mucosa (COX-1), while the other (COX-2) is present in tissues affected by inflammation and is responsible for the production of prostaglandins present in them. Knowing that cancer is an inflammatory process and that tissues affected by it express the COX-2 isoform, COX inhibition can be of great help in the treatment of this pathology. However, NSAIDs do not have specific inhibition, being able to inhibit both COX-2 and COX-1, which gives rise to gastrointestinal effects linked to the constant use of anti-inflammatory drugs. In this literature review, we will emphasize the search for articles, through the SciFinder and PubMed platforms, that have different synthetic methods for specific inhibitors of COX-2, not COX-1, reducing their side effects and, therefore, being used as antitumor agents.
Non-steroidal anti-inflammatory drugs (NSAIDs) are a class of anti-inflammatory drugs that are extremely important in the treatment of outcomes caused by inflammation, whether caused by bacteria or viruses. They act by inhibiting the cyclooxygenase (COX) enzyme, which is responsible for producing prostanoids, mainly prostaglandins, substances present in inflamed tissues and which are responsible for the symptoms originated in the inflammatory process. This enzyme has two isoforms, one of which is responsible for maintaining the integrity of the gastrointestinal mucosa (COX-1), while the other (COX-2) is present in tissues affected by inflammation and is responsible for the production of prostaglandins present in them. Knowing that cancer is an inflammatory process and that tissues affected by it express the COX-2 isoform, COX inhibition can be of great help in the treatment of this pathology. However, NSAIDs do not have specific inhibition, being able to inhibit both COX-2 and COX-1, which gives rise to gastrointestinal effects linked to the constant use of anti-inflammatory drugs. In this literature review, we will emphasize the search for articles, through the SciFinder and PubMed platforms, that have different synthetic methods for specific inhibitors of COX-2, not COX-1, reducing their side effects and, therefore, being used as antitumor agents.