Isolation of arginase inhibitors from the bioactivity-guided fractionation of Byrsonima coccolobifolia leaves and stems.
J Nat Prod
; 77(2): 392-6, 2014 Feb 28.
Article
em En
| MEDLINE
| ID: mdl-24521209
Byrsonima coccolobifolia leaf and stem extracts were studied in the search for possible leishmanicidal compounds using arginase (ARG) from Leishmania amazonensis as a molecular target. Flavonoids 1b, 1e-1g, 2a, 2b, and 2d-2f showed significant inhibitory activity, with IC50 values ranging from 0.9 to 4.8 µM. The kinetics of the most active compounds were determined. Flavonoids 1e, 1f, 2a, 2b, and 2e were characterized as noncompetitive inhibitors of ARG with dissociation constants (Ki) ranging from 0.24 to 3.8 µM, demonstrating strong affinity. Structure-activity relationship studies revealed some similarities in the structural features of flavonoids related to ARG activity.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Arginase
/
Flavonoides
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Malpighiaceae
/
Leishmania
País/Região como assunto:
America do sul
/
Brasil
Idioma:
En
Revista:
J Nat Prod
Ano de publicação:
2014
Tipo de documento:
Article
País de afiliação:
Brasil
País de publicação:
Estados Unidos