Characteristics of activation of rat mast cells by polyethylenimines and a polyallylamine: effects on the release of histamine and of arachidonate and its metabolites.
1. Three polyethylenimines and one polyallylamine released radioactivity from rat peritoneal mast cells labeled with [1-14C]arachidonic acid and concomitantly released histamine from the cells. 2. This enhancement of the release of radioactivity was inhibited by phospholipase A2 inhibitors, quinacrine (1 mM) and p-bromophenacyl bromide (10 microM), suggesting that polyethylenimine and polyallylamine activates phospholipase A2 to generate arachidonate and its metabolites. 3. The effects of H-7 or K-252a, general kinase inhibitors for the release of histamine and of arachidonate and its metabolites induced by the polycations, were different from those of W-7, a calmodulin inhibitor. The mechanisms to generate arachidonate and its metabolites seemed to differ from those to release histamine; activation of phospholipase A2 by the polycations was calmodulin-dependent. 4. p-Bromophenacyl bromide inhibited the histamine release induced by polyethylenimines and a polyallylamine, suggesting that arachidonate production by means of phospholipase A2 activation by polycations is an important process in the release of histamine from mast cells.
Yoshino
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Y
Department of Molecular Pharmacology, Meiji College of Pharmacy, Tokyo, Japan.
Sekino
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Uchida
M K
MK
Suzuki-Nishimura
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T
D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; D000818:Animals; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000378:metabolism*; D006636:Histamine Release / Q000187:drug effects*; D007546:Isoquinolines / Q000494:pharmacology; D008297:Male; D008407:Mast Cells / Q000187:drug effects / Q000378:metabolism*; D008970:Molecular Weight; D010537:Peritoneum; D010879:Piperazines / Q000494:pharmacology; D011073:Polyamines / Q000494:pharmacology*; D011094:Polyethyleneimine / Q000031:analogs & derivatives / Q000145:classification / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains
D001095:Arachidonic Acids; D007546:Isoquinolines; D010879:Piperazines; D011073:Polyamines; D016718:Arachidonic Acid; C063994:polyallylamine; D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; D011094:Polyethyleneimine