Inhibition of phospholipid methylation by an anti-allergic agent, NCO-650, during histamine release.
Antigen, anti-IgE and concanavalin A (Con A) induced an increase in both the incorporation of the 3H-methyl moiety into phospholipids and histamine release. Maximal incorporation of the 3H-methyl moiety into the lipid fraction of the cells was observed within 15 sec and 1 min after being challenged with antigen (100 micrograms/mL) and anti-IgE (200 micrograms/mL) respectively. However, the methylated phospholipid decreased rapidly. The addition of Con A (10 micrograms/mL) also increased phospholipid methylation, which reached a maximum at 5 min after challenge. Trans-4-guanidinomethylcyclohexanecarboxylic acid p-tert-butylphenyl ester hydrochloride (NCO-650; 27 microM) strongly inhibited the incorporation of the 3H-methyl moiety into phospholipid by antigen, anti-IgE and Con A. The IC50 values of NCO-650 for phospholipid methylation in response to antigen, anti-IgE and Con A were 1.5, 4.7 and 1.1 microM respectively. Although the Ca2(+)-ionophore A23187 did not induce phospholipid methylation, it caused histamine release.
Takei
M
M
Department of Pharmacology, Tokushima Bunri University, Japan.
Matumoto
T
T
Endo
K
K
Muramatu
M
M
D000818:Animals; D002478:Cells, Cultured / Q000187:drug effects; D003208:Concanavalin A / Q000037:antagonists & inhibitors / Q000494:pharmacology; D003509:Cyclohexanecarboxylic Acids / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006632:Histamine / Q000378:metabolism; D006634:Histamine H1 Antagonists / Q000494:pharmacology; D007116:Immunization, Passive; D007073:Immunoglobulin E / Q000037:antagonists & inhibitors / Q000494:pharmacology; D007700:Kinetics; D008407:Mast Cells / Q000187:drug effects* / Q000378:metabolism; D008745:Methylation; D010537:Peritoneum; D010743:Phospholipids / Q000378:metabolism*; D051381:Rats
D003509:Cyclohexanecarboxylic Acids; D006634:Histamine H1 Antagonists; D010743:Phospholipids; D003208:Concanavalin A; D007073:Immunoglobulin E; C038303:NCO 650; D006632:Histamine