Title
4′-Hydroxy-6,7-methylenedioxy-3-methoxyflavone: A novel flavonoid from Dulacia egleri with potential inhibitory activity against cathepsins B and L
Date Issued
01 January 2019
Access level
metadata only access
Resource Type
journal article
Author(s)
de Novais L.M.R.
de Arueira C.C.O.
Ferreira L.F.
Ribeiro T.A.N.
Sousa P.T.
Jacinto M.J.
de Carvalho M.G.
Judice W.A.S.
Jesus L.O.P.
de Souza A.A.
Torquato H.F.V.
Silva V.C.
Universidade de Mogi das Cruzes
Publisher(s)
Elsevier B.V.
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 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.
Start page
26
End page
29
Volume
132
Language
English
OCDE Knowledge area
Bioquímica, Biología molecular
Subjects
Scopus EID
2-s2.0-85057192622
PubMed ID
Source
Fitoterapia
ISSN of the container
0367326X
Sponsor(s)
The authors are grateful to the Instituto Nacional de Ciência e Tecnologia em Áreas Úmidas (INAU) and the Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) for scholarships and financial support. This research was supported by the FAPEMAT (TANR, 214599/2015) and FAPESP GRANT (WASJ, 2016/25112-4).
Sources of information:
Directorio de Producción Científica
Scopus