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Comp Biochem Physiol C Toxicol Pharmacol ; 131(3): 315-22, 2002 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-11912056

RESUMO

4-Bromophenacyl bromide (BPB) is generally used as a phospholipase A(2) (PLA2) inhibitor. In the present study, we demonstrate that BPB induces Ca2+ influx in human gingival fibroblasts. In fura-2-loaded human gingival fibroblasts, BPB evoked a transient increase in intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner. The BPB-induced Ca2+ mobilization was also shown in a single fluo-3-loaded-fibroblast. The BPB-induced increase in [Ca2+]i was completely abolished by the elimination of the external Ca2+. Ca2+ influx induced by the Ca2+-mobilizing agonist histamine was markedly enhanced in the presence of BPB. These suggest that the BPB-induced Ca2+ mobilization is due to the influx of extracellular Ca2+. However, it is unlikely that the effect of BPB is dependent on the inhibition of PLA2 activity, because other PLA2 inhibitors, such as AACOCF3, quinacrine dihydrochloride and manoalide, failed to induce Ca2+ mobilization. Chemical compounds similar to BPB, but which have no -CH2-Br at position 1 in the benzene ring failed to evoke Ca2+ mobilization, indicating that the position of -CH2--Br in BPB is important for causing the Ca2+ influx.


Assuntos
Acetofenonas/farmacologia , Cálcio/metabolismo , Fibroblastos/efeitos dos fármacos , Gengiva/efeitos dos fármacos , Compostos de Anilina , Ácidos Araquidônicos/farmacologia , Bradicinina/farmacologia , Células Cultivadas , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/farmacologia , Fibroblastos/citologia , Fibroblastos/metabolismo , Corantes Fluorescentes , Gengiva/citologia , Gengiva/metabolismo , Histamina/farmacologia , Humanos , Cinética , Fosfolipases A/antagonistas & inibidores , Fosfolipases A2 , Quinacrina/farmacologia , Espectrometria de Fluorescência , Relação Estrutura-Atividade , Terpenos/farmacologia , Xantenos
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