Prostaglandin biosynthesis in rabbit kidney: Mepacrine inhibits renomedullary cyclooxygenase

Arie Erman*, Ruth Azuri, Amiram Raz

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

Abstract

Mepacrine was found to exert a dose-dependent inhibition of prostaglandin E2 synthesis in rabbit kidney medulla slices and in medullary microsomes. Mepacrine at 0.5 mM produced 90% inhibition of microsomal prostaglandin E2 biosynthesis from added arachidonic acid. This effect results from inhibition of medullary cyclooxygenase; the activities of the prostaglandin G2 hydroperoxidase and the prostaglandin H2 isomerases are unaffected. In experiments with medulla slices prelabelled with [14C]arachidonate, the effect of mepacrine on the inhibition of [14C]prostaglandin generation was significantly higher (2.5 to 3.5-fold) than its inhibition of [14C]arachidonate release. Hence, although mepacrine reduces prostaglandin production by decreasing the lipolytic release of arachidonate from medullary lipids, its inhibitory effect on prostaglandin cyclooxygenase activity is substantial and appears to contribute significantly to its overall inhibition of prostaglandin generation in kidney medulla. Mepacrine is thus not only a non-selective antilipolytic agent but also a potent cyclooxygenase inhibitor.

Original languageEnglish
Pages (from-to)79-82
Number of pages4
JournalBiochemical Pharmacology
Volume33
Issue number1
DOIs
StatePublished - 1 Jan 1984

Funding

FundersFunder number
United States-Israel Binational Science Foundation

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