4 '-Hydroxy-6,7-methylenedioxy-3-methoxyflavone: A novel flavonoid from Dulacia egleri with potential inhibitory activity against cathepsins B and L

Autor(es):Mostrar menos -

de Novais, Leice M. R. ; de Arueira, Cauane C. O. ; Ferreira, Luiz F. ; Ribeiro, Tereza A. N. ; Sousa, Paulo T., Jr. ; Jacinto, Marcos J. ; de Carvalho, Mario G. ; Judice, Wagner A. S. ; Jesus, Larissa O. P. ; de Souza, Aline A. ; Torquato, Heron F. V. ; Paredes-Gamero, Edgar J. ; Silva, Virginia C.

• Tipo de documento: Artigo Científico
• Fonte: Fitoterapia; v. 132, p. 4-pg., 2019-01-01.

Resumo

A new flavone, 4'-hydroxy-6,7-methylenedioxy-3-methoxyflavone 1, and two other nucleosides, ribavirin 2 and adenosine 3, were isolated from the leaves of Dulacia egleri. The nucleosides were identified by spectroscopic techniques (1D, 2D-NMR) while the structure of the flavonoid was established by 1D, 2D-NMR analysis, including HRESIMS data. The results obtained in the biological assays showed that the compound 1 was able to inhibit cathepsins B and L with IC50 of 14.88 +/- 0.18 mu M and 3.19 +/- 0.07 mu M, respectively. The mechanism of inhibition for both enzymes were determined showing to be competitive at cathepsin B with Ki = 12.8 +/- 0.6 mu M and non-linear non-competitive with positive cooperativity inhibition at cathepsin L with K-i = 322 +/- 33 mu M, alpha K-i= 133 +/- 15 mu M, beta K-i = 5.14 +/- 0.41 mu M and gamma K-i = 13.2 +/- 13 mu M. (AU)

• Processo FAPESP: 16/25112-4 - Avaliação de moduladores da atividade de proteases envolvidas em processos patológicos
• Beneficiário: Wagner Alves de Souza Júdice
• Modalidade de apoio: Auxílio à Pesquisa - Regular