Evaluation of antimicrobial and anti-inflammatory effects of furoxan and benzofuroxan derivatives as an alternative for acne vulgaris treatment

Autor: Delgado, Ivone Leila Lima [UNESP]
Přispěvatelé: Universidade Estadual Paulista (Unesp), Santos, Jean Leandro dos [UNESP]
Jazyk: portugalština
Rok vydání: 2017
Předmět:
Zdroj: Repositório Institucional da UNESP
Universidade Estadual Paulista (UNESP)
instacron:UNESP
Popis: Submitted by Ivone Leila Lima Delgado null (leilavone@gmail.com) on 2017-06-23T19:11:39Z No. of bitstreams: 1 Dissertação repos..pdf: 2133288 bytes, checksum: ec58ee4f471950dfade8804f338e05f4 (MD5) Approved for entry into archive by Luiz Galeffi (luizgaleffi@gmail.com) on 2017-06-28T16:32:25Z (GMT) No. of bitstreams: 1 delgado_ill_me_arafcf.pdf: 2133288 bytes, checksum: ec58ee4f471950dfade8804f338e05f4 (MD5) Made available in DSpace on 2017-06-28T16:32:25Z (GMT). No. of bitstreams: 1 delgado_ill_me_arafcf.pdf: 2133288 bytes, checksum: ec58ee4f471950dfade8804f338e05f4 (MD5) Previous issue date: 2017-05-23 Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) A acne é uma doença autolimitada de componente multifatorial, caracterizada pela presença de inflamação e colonização bacteriana pelo microrganismo Propionibacterium acnes. Atualmente, o tratamento tópico e/ou oral, inclui fármacos com propriedades anti-inflamatórias, antimicrobianas e queratolíticas. Apesar dos efeitos benéficos no tratamento da acne, a terapia atual apresenta limitações que justificam a busca de novos fármacos. Furoxanos e benzofuroxanos são compostos heterocíclicos contendo a função N-óxido e que apresentam uma grande diversidade de propriedades farmacológicas, incluindo antimicrobiana. Neste trabalho investigouse o efeito antimicrobiano de compostos furoxanos e benzofuroxanos pertencentes à biblioteca de moléculas do laboratório de Química Farmacêutica e Medicinal da Faculdade de Ciências Farmacêuticas. Para fins de caracterização do espectro de ação, além do P. acnes foi realizado screening do perfil de atividade antimicrobiana frente às cepas fúngicas, bactérias Gram positivas e Gram negativas usando as técnicas de microdiluição. Os furoxanos e benzofuroxanos foram testados em concentrações que variaram de 0.03 a 100 μg/mL. Foram usados controles como a cefazolina (0.39 μg/mL) para P. acnes, o imipenen (65 μg/mL) for species of Candida and Cryptococcus, respectively. After incubation, visual readings were performed with and without revealing reassuring (0.01%) to determine the MIC value. Over 20 compounds evaluated, 14 were able to inhibit the growth of at least one microorganism.The compound (E) -4- (3 - ((2- (3-hydroxybenzoyl) hydrazone) methyl) phenoxy) -3- (phenylsulfonyl) -1,2,5-oxadiazole-2-oxidewas the most active molecule against Propionobacterium acnes, presenting MIC value of 0.19 μg/mL. In vitro studies showed that this compound was able to release nitric oxide, which should be one of the modes of action for this compound. There was also inhibition of NO production in macrophage at the concentration of 0.78 ug/mL.The cellular viability against macrophage cells and the anti-inflammatory effect characterized by the inhibition of IL1-β e a TNF-α were performed. It was characterized in murine macrophages that the limit of 100% of viability is found at concentrations inferior to 0.09 μg/mL; however, it was not observed inhibition ability of these cytokines in the concentration used. The in vivo assay did not show anti-inflammatory activity of the tested compound. As conclusion, we identified the compound (E) -4- (3 - ((2- (3- hydroxybenzoyl) hydrazone) methyl) phenoxy) -3- (phenylsulfonyl) -1,2,5-oxadiazole- 2-oxideas a new drug antimicrobial active against Propionobacterium acnes. This compound could be used as a new alternative to treat acne.
Databáze: OpenAIRE
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