4-Bromophenacyl bromide induces Ca2+ influx in human gingival fibroblasts

Add time:09/05/2019    Source:sciencedirect.com

4-Bromophenacyl bromide (BPB) is generally used as a phospholipase A2 (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.

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