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BIBTEX RIS

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

2018; Elsevier BV; Volume: 132; Linguagem: Inglês

10.1016/j.fitote.2018.08.005

1873-6971

Leice Milla Ribeiro de Novais, Cauane C.O. de Arueira, Luiz Felipe Ferreira, Tereza Auxiliadora Nascimento Ribeiro, Paulo Teixeira de Sousa, Marcos J. Jacinto, Mário Geraldo de Carvalho, Wagner Alves de Souza Júdice, Larissa O.P. Jesus, Aline Aparecida de Souza, Heron Fernandes Vieira Torquato, Edgar Julian Paredes‐Gamero, Virgínia Cláudia da Silva,

Protease and Inhibitor Mechanisms

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 μM and 3.19 ± 0.07 μM, respectively. The mechanism of inhibition for both enzymes were determined showing to be competitive at cathepsin B with Ki = 12.8 ± 0.6 μM and non-linear non-competitive with positive cooperativity inhibition at cathepsin L with Ki = 322 ± 33 μM, αKi = 133 ± 15 μM, βKi = 5.14 ± 0.41 μM and γKi = 13.2 ± 13 μM.