In situ screening of 3-arylcoumarin derivatives reveals new inhibitors of mast cell degranulation

Autor(es)

Santos, Marcela de Souza ^{[1, 2]} ; Freire de Morais Del Lama, Maria Perpetua ^{[1, 2]} ; Deliberto, Laila Aparecida ^{[1, 2]} ; Emery, Flavio da Silva ^[3] ; Pupo, Monica Tallarico ^[3] ; Zumstein Georgetto Naal, Rose Mary ^{[1, 2]}

Afiliação do(s) autor(es)

^[1] Univ Sao Paulo, Dept Fis & Quim, Fac Ciencias Farmaceut Ribeirao Preto, BR-14040903 Ribeirao Preto, SP - Brazil

^[2] Inst Ciencia & Tecnol Bioanalit, Campinas, SP - Brazil

^[3] Univ Sao Paulo, Dept Ciencias Farmaceut, Fac Ciencias Farmaceut Ribeirao Preto, BR-14040903 Ribeirao Preto, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: ARCHIVES OF PHARMACAL RESEARCH; v. 36, n. 6, p. 731-738, JUN 2013.
• Citações Web of Science: 8

Resumo

Due to the severity and high prevalence of allergic diseases, there is growing interest in the development of inhibitors of such conditions. 3-Arylcoumarin derivatives emerge as promising compounds for the treatment of allergic disorders, in particular due to their close structural similarity to flavonoids, whose anti-allergic activity has been extensively reported. The aim of this work was to perform a screening of a set of 3-arylcoumarins as potential inhibitors of mast cell degranulation, a key event for the development of allergic reactions. For that purpose, it was utilized a biosensor model based on mast cells, whose in vitro assay allows for such screening, in a high throughput fashion, and also permits bringing to attention some coumarin structural features that are important for their biological activity. The mast cell-based biosensor was shown to discriminate, with high sensitivity and reproducibility, between coumarins that did not affect or caused different degrees of inhibition of degranulation. Among active coumarins, some substituents could be accounted for their inhibitory activity, such as the hydroxylation of positions 6 and 2' of 3-phenylcoumarins, in addition to catechol, amino and thiophene moieties. In summary, 3-arylcoumarins could be suggested as potential candidates for the development of new anti-allergic drugs. (AU)

• Processo FAPESP: 08/01712-6 - Estudo da atividade antialérgica de cumarinas naturais e sintéticas: aplicação do biossensor baseado em mastócitos
• Beneficiário: Marcela de Souza Santos
• Modalidade de apoio: Bolsas no Brasil - Doutorado Direto