PMID: 2123476Oct 1, 1990Paper

Retinoids inhibit phospholipase A2 in human synovial fluid and arachidonic acid release from rat peritoneal macrophages

Inflammation
W C HopeB H Wittreich

Abstract

Retinoids have demonstrated antiinflammatory activity in certain animal models and human disease states. The mechanism by which retinoids elicit this activity is unknown. Some retinoids are known to inhibit arachidonic acid (AA) release and metabolism in intact cells in vitro. Retinoids may exert their antiinflammatory effects by inhibiting phospholipase A2 (PLA2) and the resultant production of inflammatory AA metabolites. Retinoids were evaluated in vitro as inhibitors of the PLA2 activity in human synovial fluid (HSF-PLA2). Of the naturally occurring, nonaromatic retinoids tested, all-trans-retinal, all-trans-retinoic acid (all-trans-RA) and 13-cis-RA were the most potent inhibitors (IC50 S 6-15 microM), whereas all-trans-retinol was much less potent. Of the synthetic aromatic retinoids and arotinoids examined, the free carboxylic, sulfonic, and sulfinic acid forms were more than 15-fold more potent inhibitors of HSF-PLA2 than their corresponding ethyl esters. These retinoids also were evaluated as inhibitors of calcium ionophore A23187-induced AA release from rat peritoneal macrophages. All-trans-RA and 13-cis-RA were potent inhibitors of AA release from these cells (IC50 S 4 microM), while the other natural retinoids were ...Continue Reading

References

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Citations

Sep 1, 1991·Agents and Actions·W C HopeD R Bolin
Aug 4, 1992·Biochemical Pharmacology·F CabréG Carganico
Jul 8, 2000·International Journal of Immunopharmacology·J S Mathew, R P Sharma
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Mar 1, 1997·Expert Opinion on Investigational Drugs·U Tibes, W G Friebe
Nov 7, 2008·The Journal of Investigative Dermatology·Amanda M NelsonDiane M Thiboutot
Oct 16, 2015·Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology·Kai Kristoffer LieMari Moren
Feb 9, 1993·Biochemical Pharmacology·A CarabazaG Carganico
Apr 30, 1992·Biochemical and Biophysical Research Communications·K I HulkowerD W Morgan
Mar 22, 2000·Clinical and Applied Thrombosis/hemostasis : Official Journal of the International Academy of Clinical and Applied Thrombosis/Hemostasis·T W Stief, J Fareed
Aug 10, 2002·American Journal of Physiology. Endocrinology and Metabolism·Carole Seguin-DevauxDan Longrois
Oct 29, 2000·American Journal of Physiology. Endocrinology and Metabolism·Y DevauxD Ungureanu-Longrois
Jul 22, 2017·Archivum Immunologiae Et Therapiae Experimentalis·Danuta NowickaJacek Roliński
Jun 4, 2020·Heliyon·Xu-Yan YangShuai-Nan Zhang
Apr 22, 2010·Journal of Medicinal Chemistry·Palle J PedersenMads H Clausen

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