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Chem Pharm Bull (Tokyo) ; 38(10): 2740-5, 1990 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-1963813

RESUMO

The structure of scopadulcic acid B (2, SDB), a major ingredient of the Paraguayan herb "Typychá kuratu" (Scoparia dulcis L.), was elucidated mainly by comparison of its spectral data with that of scopadulcic acid A (1). SDB inhibited both the K(+)-dependent adenosine triphosphatase (ATPase) activity of a hog gastric proton pump (H+, K(+)-ATPase) with a value of 20-30 microM for IC50 and proton transport into gastric vesicles. Pharmacokinetic studies of SDB in rats indicated that plasma SDB concentrations after i.v. injection of the sodium salt of SDB (SDB-Na) were described reasonably well by a two-compartment open model with Michaelis-Menten elimination kinetics. Plasma concentrations after oral administration of SDB-Na or SDB showed a much slower decline than what was expected following the i. v. study. It was suggested that the sustained plasma level of SDB after oral administration of SDB-Na or SDB was accounted for by relatively slow but efficient gastro-intestinal absorption in rats.


Assuntos
Adenosina Trifosfatases/antagonistas & inibidores , Antivirais/química , Diterpenos/química , Plantas Medicinais/análise , Animais , Antivirais/farmacocinética , Antivirais/farmacologia , Diterpenos/farmacocinética , Diterpenos/farmacologia , ATPase Trocadora de Hidrogênio-Potássio , Masculino , Paraguai , Ratos , Ratos Endogâmicos , Estômago/efeitos dos fármacos , Estômago/enzimologia , Suínos , Difração de Raios X
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