4'-Hydroxy-6,7-methylenedioxy-3-methoxyflavone: A novel flavonoid from Dulacia egleri with potential inhibitory activity against cathepsins B and L.
Fitoterapia
; 132: 26-29, 2019 Jan.
Article
en En
| MEDLINE
| ID: mdl-30114470
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⯱â¯0.18⯵M and 3.19⯱â¯0.07⯵M, respectively. The mechanism of inhibition for both enzymes were determined showing to be competitive at cathepsin B with Kiâ¯=â¯12.8⯱â¯0.6⯵M and non-linear non-competitive with positive cooperativity inhibition at cathepsin L with Kiâ¯=â¯322⯱â¯33⯵M, αKiâ¯=â¯133⯱â¯15⯵M, ßKiâ¯=â¯5.14⯱â¯0.41⯵M and γKiâ¯=â¯13.2⯱â¯13⯵M.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Flavonoides
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Catepsina B
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Olacaceae
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Inhibidores Enzimáticos
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Catepsina L
País/Región como asunto:
America do sul
/
Brasil
Idioma:
En
Revista:
Fitoterapia
Año:
2019
Tipo del documento:
Article
País de afiliación:
Brasil