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J Nat Prod ; 77(2): 392-6, 2014 Feb 28.
Artigo em Inglês | 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.

Arginase/antagonistas & inibidores , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Leishmania/efeitos dos fármacos , Malpighiaceae/química , Brasil , Flavonoides/química , Concentração Inibidora 50 , Estrutura Molecular , Folhas de Planta/química , Caules de Planta/química , Relação Estrutura-Atividade
Chem Biodivers ; 10(11): 1999-2006, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24243608


A series of chalcone derivatives, 1-15, were prepared by Claisen-Schmidt condensation and evaluated for their cytotoxicities on tumor cell lines and also against proteolytic enzymes such as cathepsins B and K. Of the compounds synthesized, (E)-3-(3,4-dimethoxyphenyl)-1-phenylprop-2-en-1-one (12), (E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-one (13), (E)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-one (14), and (E)-3-(4-nitrophenyl)-1-phenylprop-2-en-1-one (15) showed significant cytotoxicities. The most effective compound was 15, which showed high cytotoxic activity with an IC50 value lower than 1 µg/ml, and no selectivity on the tumor cells evaluated. Substituents at C(4) of ring B were found to be essential for cytotoxicity. In addition, it was also demonstrated that some of these chalcones are moderate inhibitors of cathepsin K and have no activity against cathepsin B.

Antineoplásicos/química , Antineoplásicos/farmacologia , Catepsina B/antagonistas & inibidores , Catepsina K/antagonistas & inibidores , Chalcona/análogos & derivados , Chalcona/farmacologia , Catepsina B/metabolismo , Catepsina K/metabolismo , Linhagem Celular Tumoral , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Humanos , Neoplasias/tratamento farmacológico , Neoplasias/enzimologia