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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

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

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de Novais, Leice M. R. [1] ; de Arueira, Cauane C. O. [1] ; Ferreira, Luiz F. [1] ; Ribeiro, Tereza A. N. [1] ; Sousa, Jr., Paulo T. [1] ; Jacinto, Marcos J. [1] ; de Carvalho, Mario G. [2] ; Judice, Wagner A. S. [3] ; Jesus, Larissa O. P. [3] ; de Souza, Aline A. [3] ; Torquato, Heron F. V. [4] ; Paredes-Gamero, Edgar J. [3] ; Silva, Virginia C. [1]
Total Authors: 13
[1] Univ Fed Mato Grosso, Dept Quim, Cuiaba, MT - Brazil
[2] Univ Fed Rural Rio de Janeiro, Dept Quim, Seropedica, RJ - Brazil
[3] Univ Mogi das Cruzes, Ctr Interdisciplinar Invest Bioquim, BR-08780911 Mogi Das Cruzes, SP - Brazil
[4] Univ Fed Sao Paulo, Dept Bioquim, Campus Sao Paulo, Sao Paulo - Brazil
Total Affiliations: 4
Document type: Journal article
Source: Fitoterapia; v. 132, p. 26-29, JAN 2019.
Web of Science Citations: 1

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)

FAPESP's process: 16/25112-4 - Evaluation of modulators of the activity of proteases involved in pathological processes
Grantee:Wagner Alves de Souza Júdice
Support type: Regular Research Grants