4-Bromophenacyl bromide induces Ca2+ influx in human gingival fibroblasts.
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.
Ogata
Yorimasa
Y
Department of Periodontology, Nihon University School of Dentistry at Matsudo, Matsudo, Chiba 271-8587, Japan.
Sakurai
Takeshi
T
Nakao
Sumi
S
Kuboyama
Noboru
N
Moriwaki
Kazunari
K
Furuyama
Shunsuke
S
Sugiya
Hiroshi
H
D000098:Acetophenones / Q000494:pharmacology*; D000814:Aniline Compounds; D001095:Arachidonic Acids / Q000494:pharmacology; D001920:Bradykinin / Q000494:pharmacology; D002118:Calcium / Q000378:metabolism*; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000494:pharmacology; D005347:Fibroblasts / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D005456:Fluorescent Dyes; D005881:Gingiva / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D006632:Histamine / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D010741:Phospholipases A / Q000037:antagonists & inhibitors; D054467:Phospholipases A2; D011796:Quinacrine / Q000494:pharmacology; D013050:Spectrometry, Fluorescence; D013329:Structure-Activity Relationship; D013729:Terpenes / Q000494:pharmacology; D014966:Xanthenes
D000098:Acetophenones; D000814:Aniline Compounds; D001095:Arachidonic Acids; D004791:Enzyme Inhibitors; D005456:Fluorescent Dyes; D013729:Terpenes; D014966:Xanthenes; C081565:arachidonyltrifluoromethane; C059715:Fluo-3; D006632:Histamine; C045673:manoalide; D010741:Phospholipases A; D054467:Phospholipases A2; D011796:Quinacrine; C006821:4-bromophenacyl bromide; D001920:Bradykinin; D002118:Calcium