Inhibition of Bovine Leukocyte Thioltransferase by Anti-inflammatory Drugs and Anti-histaminic Drugs

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Thioltransferase was partially purified from bovine leukocyte using sonication, heat treatment at pH 5.1,Sephadex G-50 gel filtration and isoelectric focusing techniques. Isoelectric point (pI) of 8.3 for leukocyte thioltransferase was quite different from pI of 6.5 for erythrocyte enzyme. Bovine leukocyte thioltransferase was employed in a study on the influence of 12 anti-inflammatory drugs and 7 anti-histaminic drugs. Piroxicam which is a well-known anti-inflammatory drug demonstrated the most powerful inhibitory effect on enzyme activity. Inhibition of piroxicam was noncompetitive, and the K_i value measured 55.0 μM in the experiment involving bovine leukocyte enzyme. Tranilast which is a typical anti-histaminic drug most strongly inhibited the enzyme activity and the K_i value of the medicine was 20.3 μM (noncompetitive). Bovine liver and erythrocyte thioltransferases also were effectively inhibited by both medicines similar to leukocyte enzyme.
1993-09-15