title: Inhibition of lysoPAF acetyltransferase activity by flavonoids.
abstract: OBJECTIVE
  Several kinds of flavonoids, widely distributed natural products of the vegetable kingdom which possess anti-inflammatory activity, were examined for inhibitory effects on the acetyl-CoA: 1-alkyl-2-lyso-sn-glycero-3-phosphocholine (lysoPAF) acetyltransferase activity.
  
  
  METHODS
  Acetyl-CoA:lysoPAF acetyltransferase activity was determined using homogenates of a rat mucosal-type mastocytoma cell line, RBL-2H3 as an enzyme source. The production of platelet-activating factor (PAF) in rat peripheral white blood cells stimulated with the calcium ionophore A23187 was studied.
  
  
  RESULTS
  Of the flavonoids tested, luteolin and quercetin exhibited significant inhibitory effects (IC50, 45 microM and 80 microM, respectively), whereas other structurally-related flavonoids failed to affect the lysoPAF acetyltransferase activity. Luteolin did not suppress the activity of choline acetyltransferase, suggesting that the inhibition observed here was specific. Luteolin also inhibited the production of PAF in rat peripheral white blood cells.
  
  
  CONCLUSIONS
  These results indicate that luteolin could become a leading compound for developing a novel type of anti-inflammatory, anti-allergic drugs that target lysoPAF acetyltransferase.
authors.affiliation: Institute of Medicinal Chemistry, Hoshi University, Tokyo, Japan.
authors.forename: R
authors.initials: R
authors.lastname: Yanoshita
authors.forename: H W
authors.initials: HW
authors.lastname: Chang
authors.forename: K H
authors.initials: KH
authors.lastname: Son
authors.forename: I
authors.initials: I
authors.lastname: Kudo
authors.forename: Y
authors.initials: Y
authors.lastname: Samejima
mesh_terms: D000123:Acetyltransferases / Q000037:antagonists & inhibitors* / Q000097:blood*; D000818:Animals; D002474:Cell-Free System / Q000187:drug effects; D002795:Choline O-Acetyltransferase / Q000037:antagonists & inhibitors; D005419:Flavonoids / Q000494:pharmacology*; D047311:Luteolin; D012515:Mast-Cell Sarcoma / Q000201:enzymology; D010972:Platelet Activating Factor / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D051381:Rats; D014407:Tumor Cells, Cultured
chemical_list: D005419:Flavonoids; D010972:Platelet Activating Factor; D000123:Acetyltransferases; D002795:Choline O-Acetyltransferase; C046035:1-alkylglycerophosphocholine acetyltransferase; D047311:Luteolin