Indomethacin inhibition of glutathione S-transferases |
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| Authors: | C Wu K P Mathews |
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| Affiliation: | 1. Department of Biological Chemistry The University of Michigan Medical School, Ann Arbor, Michigan 48109, U.S.A.;2. the Montgomery Allergy Research Laboratory, Department of Internal Medicine, The University of Michigan Medical School, Ann Arbor, Michigan 48109, U.S.A. |
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| Abstract: | Indomethacin inhibited rat liver glutathione S-transferases (EC 2.5.1.18). Its inhibition was non-competitive with respect to 3,4-dichloronitrobenzene with an apparent Ki of 5.3 X 10(-5) M and uncompetitive with respect to glutathione with an apparent Ki of 4.0 X 10(-5) M. 4-Chlorobenzoic acid and 5-methoxy-2-methylindole-3-acetic acid, two metabolites of indomethacin, were weak inhibitors of the enzymes. On the other hand, meclofenamic acid was a competitive inhibitor of the enzymes with an apparent Ki of 3.0 X 10(-4) M. Possible significance of these findings in arachidonic acid metabolism is discussed. |
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| Keywords: | CBA 4-chlorobenzoic acid DCNB 3,4-dichloronitrobenzene DTNB 5,5′-dithiobis-(2-nitrobenzoic acid) GSH reduced glutathione 12-HPETE 12-hydroperoxy-5,8,10,14-eicosatetraenoic acid MMIA 5-methoxy-2-methylindole-3-acetic acid SRS slow reacting substance (of anaphylaxis) |
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