Stearic acid potently modulates the activity of cyclooxygenase-1, but not cyclooxygenase-2, in the form of its CoA ester.
The effects of palmitic acid (PA), stearic acid (SA) and oleic acid (OA), and their respective CoA esters, PA-CoA, SA-CoA and OA-CoA, on the activities of cyclooxygenase (COX)-1 and -2 were examined. Ten units of purified COX-1 or -2 were preincubated with drugs in the presence of hematin (0.1 microM) and phenol (2 mM) as cofactors for 10 min at 37 degrees C, and then incubated with 100 microM arachidonic acid for 2 min at 37 degrees C. The amounts of prostaglandins formed were measured by HPLC. PA, SA and OA had no effect on the COX-1 and -2 activities, but their respective CoA esters, PA-CoA, SA-CoA and OA-CoA, suppressed COX-1 activity with no significant effect on COX-2 activity. The inhibitory effect of SA-CoA was much stronger than that of PA-CoA and OA-CoA. These results suggest that SA has the potential to inhibit COX-1 activity, but not COX-2 activity, in the form of their CoA ester.
Fujimoto
Yohko
Y
Department of Physiological Chemistry, Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka, Japan. fujimoto@gly.oups.ac.jp
Yonemura
Toshimitsu
T
Sakuma
Satoru
S
D000214:Acyl Coenzyme A / Q000494:pharmacology*; D000818:Animals; D016718:Arachidonic Acid / Q000378:metabolism; D002417:Cattle; D051545:Cyclooxygenase 1 / Q000378:metabolism*; D051546:Cyclooxygenase 2 / Q000378:metabolism*; D019301:Oleic Acid / Q000494:pharmacology; D019308:Palmitic Acid / Q000494:pharmacology; D011453:Prostaglandins / Q000378:metabolism; D013229:Stearic Acids / Q000494:pharmacology*
D000214:Acyl Coenzyme A; D011453:Prostaglandins; D013229:Stearic Acids; D016718:Arachidonic Acid; D019301:Oleic Acid; D019308:Palmitic Acid; C031183:stearic acid; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2