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.
journal_name
Fitoterapiajournal_title
Fitoterapiaauthors
de Novais LMR,de Arueira CCO,Ferreira LF,Ribeiro TAN,Sousa PT Jr,Jacinto MJ,de Carvalho MG,Judice WAS,Jesus LOP,de Souza AA,Torquato HFV,Paredes-Gamero EJ,Silva VCdoi
10.1016/j.fitote.2018.08.005subject
Has Abstractpub_date
2019-01-01 00:00:00pages
26-29eissn
0367-326Xissn
1873-6971pii
S0367-326X(18)30745-7journal_volume
132pub_type
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