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Biosci Biotechnol Biochem ; 75(8): 1472-80, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-21821954

RESUMO

The present work investigates protein tyrosine phosphatase 1B (PTP1B) and the α-glucosidase inhibitory activities of two edible brown algae, Ecklonia stolonifera and Eisenia bicyclis, as well as in their isolated phlorotannins. Since the individual extracts and fractions showed significant inhibitory activities, column chromatography was performed to isolate six phlorotannins, phloroglucinol (1), dioxinodehydroeckol (2), eckol (3), phlorofurofucoeckol-A (4), dieckol (5), and 7-phloroeckol (6). Phlorotannins 3-6 were potent and noncompetitive PTP1B inhibitors with IC(50) values ranging from 0.56 to 2.64 µM; 4-6 exhibited the most potent α-glucosidase inhibition with IC(50) values ranging from 1.37 to 6.13 µM. Interestingly, 4 and 6 were noncompetitive, while 5 exhibited competitive inhibition in an α-glucosidase assay. E. stolonifera and E. bicyclis as well as their isolated phlorotannins therefore possessed marked PTP1B and α-glucosidase inhibitory activities; this could lead to opportunities in the development of therapeutic agents to control the postprandial blood glucose level and thereby prevent diabetic complications.


Assuntos
Diabetes Mellitus/enzimologia , Inibidores Enzimáticos/farmacologia , Inibidores de Glicosídeo Hidrolases , Hiperglicemia/enzimologia , Hipoglicemiantes/farmacologia , Phaeophyceae/química , Proteína Tirosina Fosfatase não Receptora Tipo 1/antagonistas & inibidores , Taninos/farmacologia , Benzofuranos/química , Benzofuranos/farmacologia , Glicemia/análise , Misturas Complexas/química , Misturas Complexas/farmacologia , Diabetes Mellitus/tratamento farmacológico , Diabetes Mellitus/fisiopatologia , Dioxinas/química , Dioxinas/farmacologia , Inibidores Enzimáticos/química , Humanos , Hiperglicemia/tratamento farmacológico , Hiperglicemia/fisiopatologia , Hipoglicemiantes/química , Cinética , Espectroscopia de Ressonância Magnética , Floroglucinol/química , Floroglucinol/farmacologia , Proteína Tirosina Fosfatase não Receptora Tipo 1/metabolismo , Soluções , Espectrofotometria , Taninos/química , Leveduras , alfa-Glucosidases/metabolismo
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