Histamine release from human basophils by pepstatin A.
Pepstatin A, a pentapeptide isolated from cultures of actinomycetes, induced histamine secretion from human basophils in the concentration range of 3 X 10(-7) to 10(-4) M. The characteristics of this reaction were similar to those of f-met-peptide-induced histamine release: pepstatin A-induced release required Ca2+ and the release reaction was complete within 2 min at 22 or 37 degrees C, but did not occur at 4 degrees C. Release by both pepstatin A and f-met-peptide was reversibly inhibited by two non-releasing analogs of f-met-peptide, CBZ-Phe-Met and BOC-Met-Leu-Phe. Further, there was complete cross-desensitization between pepstatin A and f-met-peptide, while cells desensitized to pepstatin A released normally with anti-IgE and vice versa. A variety of pharmacological agents had similar effects on both pepstatin A and f-met-peptide-induced release (e.g., no enhancement with D2O; marked enhancement with cytochalasin B). We suggest that pepstatin A induces histamine release from human basophils by activating a cell surface receptor(s), also activated by the synthetic tripeptide f-met-peptide.
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G
Marone
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M
Columbo
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L
Soppelsa
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M
Condorelli
D001491:Basophils / Q000187:drug effects / Q000378:metabolism*; D003571:Cytochalasin B / Q000494:pharmacology; D003903:Deuterium / Q000494:pharmacology; D004151:Dipeptides / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006636:Histamine Release / Q000187:drug effects*; D006801:Humans; D007073:Immunoglobulin E / Q000502:physiology; D009240:N-Formylmethionine Leucyl-Phenylalanine / Q000494:pharmacology; D009842:Oligopeptides / Q000494:pharmacology*; D010436:Pepstatins / Q000494:pharmacology*
D004151:Dipeptides; D009842:Oligopeptides; D010436:Pepstatins; C014195:Streptomyces pepsin inhibitor; C035192:carbobenzoxyphenylalanylmethionine; D007073:Immunoglobulin E; D003571:Cytochalasin B; D009240:N-Formylmethionine Leucyl-Phenylalanine; C046832:t-butyloxycarbonyl-methionyl-leucyl-phenylalanine; D003903:Deuterium; C031375:pepstatin