Effects of non-steroidal anti-inflammatory drugs on cyclo-oxygenase and lipoxygenase activity in whole blood from aspirin-sensitive asthmatics vs healthy donors

Br J Pharmacol. 2002 Dec;137(7):1031-8. doi: 10.1038/sj.bjp.0704927.

Abstract

1. Cyclo-oxygenase (COX) and lipoxygenase (LO) share a common substrate, arachidonic acid. Aspirin and related drugs inhibit COX activity. In a subset of patients with asthma aspirin induces clinical symptoms associated with increased levels of certain LO products, a phenomenon known as aspirin-sensitive asthma. The pharmacological pathways regulating such responses are not known. 2. Here COX-1 and LO activity were measured respectively by the formation of thromboxane B(2) (TXB(2)) or leukotrienes (LT) C(4), D(4) and E(4) in whole blood stimulated with A23187. COX-2 activity was measured by the formation of prostaglandin E(2) (PGE(2)) in blood stimulated with lipopolysaccharide (LPS) for 18 h. 3. No differences in the levels of COX-1, COX-2 or LO products or the potency of drugs were found in blood from aspirin sensitive vs aspirin tolerant patients. Aspirin, indomethacin and nimesulide inhibited COX-1 activity, without altering LO activity. Indomethacin, nimesulide and the COX-2 selective inhibitor DFP [5,5-dimethyl-3-(2-isopropoxy)-4-(4-methanesulfonylphenyl)-2(5H)-furanone] inhibited COX-2 activity. NO-aspirin, like aspirin inhibited COX-1 activity in blood from both groups. However, NO-aspirin also reduced LO activity in the blood from both patient groups. Sodium salicylate was an ineffective inhibitor of COX-1, COX-2 or LO activity in blood from both aspirin-sensitive and tolerant patients. 4. Thus, when COX activity in the blood of aspirin-sensitive asthmatics is blocked there is no associated increase in LO products. Moreover, NO-aspirin, unlike other NSAIDs tested, inhibited LO activity in the blood from both aspirin sensitive and aspirin tolerant individuals. This suggests that NO-aspirin may be better tolerated than aspirin by aspirin-sensitive asthmatics.

Publication types

  • Comparative Study

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Aspirin / administration & dosage
  • Asthma / blood*
  • Asthma / chemically induced
  • Asthma / enzymology
  • Benzene Derivatives / pharmacology
  • Calcimycin / pharmacology
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / pharmacology
  • Dinoprostone / blood
  • Dose-Response Relationship, Drug
  • Furans / pharmacology
  • Humans
  • Indomethacin / pharmacology
  • Ionophores / pharmacology
  • Isoenzymes / blood
  • Isoenzymes / drug effects
  • Leukotrienes / blood
  • Lipopolysaccharides / pharmacology
  • Lipoxygenase / blood
  • Lipoxygenase / drug effects*
  • Membrane Proteins
  • Prostaglandin-Endoperoxide Synthases / blood
  • Prostaglandin-Endoperoxide Synthases / drug effects*
  • Sulfonamides / pharmacology
  • Thromboxane B2 / blood

Substances

  • 3-2(-propyloxy)-(4-methylsulfonylphenyl)-(5,5-dimethyl)furanone
  • Anti-Inflammatory Agents, Non-Steroidal
  • Benzene Derivatives
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Furans
  • Ionophores
  • Isoenzymes
  • Leukotrienes
  • Lipopolysaccharides
  • Membrane Proteins
  • Sulfonamides
  • Calcimycin
  • Thromboxane B2
  • Lipoxygenase
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • PTGS1 protein, human
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases
  • Dinoprostone
  • Aspirin
  • nimesulide
  • Indomethacin