Investigations with the selective PKC inhibitor chelerythrine on human basophils

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E von StebutH H Wolff

Abstract

Modulation of protein kinase C (PKC) activity in basophils (B) can influence IgE-mediated histamine release (HR). The present study investigated the effects of chelerythrine, which inhibits isolated PKC (IC50 0.7 microM), on different activation pathways in B. Fc epsilon RI-mediated HR was strongly inhibited by chelerythrine (86.5 +/- 5.4%, 5 microM, n = 11). TPA-induced mediator release was also suppressed: 77.1 +/- 8.5% inhibition (7.5 microM). HR due to non-immunological stimuli (A23187, FMLP) was strongly inhibited by chelerythrine. Previously, other selective PKC-inhibitors have been shown to potentiate IgE-mediated HR from B suggesting a negative modulatory role of PKC, whereas non-specific inhibitors such as staurosporine inhibited HR. Chelerythrine might therefore be less selective for PKC. This may be indicated by the fact that chelerythrine inhibits PKC at its catalytic domain, which is homologous with other protein kinases.

References

Jan 1, 1992·International Archives of Allergy and Immunology·U AmonH H Wolff
Nov 15, 1990·Biochemical and Biophysical Research Communications·J M HerbertJ P Maffrand
Mar 15, 1989·Biochemical and Biophysical Research Communications·E KobayashiT Tamaoki
Jul 18, 1986·Science·Y Nishizuka

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