| Full text | |
| Author(s): Show less - |
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.
Total Authors: 13
|
| Document type: | Journal article |
| Source: | Fitoterapia; v. 132, p. 4-pg., 2019-01-01. |
| Abstract | |
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 Opportunities: | Regular Research Grants |