Effect of some analgesics on Paraoxonase-1 purified from human serum

Abstract

The in vitro effects of the analgesic drugs, lornoxicam, indomethacin, tenoxicam, diclofenac sodium, ketoprofen and lincomycine, on the activity of purified human serum paraoxonase (hPON1) (EC 3.1.8.1.) were evaluated. hPON1 was purified from human serum with a final specific activity of 3840 U mg -1 and a purity of 25.3 % using simple chromatographic methods, including DEAE-Sephadex anion exchange and Sepharose 4B-L-tyrozine-1--napthylamine hydrophobic interaction chromatography. SDS-polyacrylamide gel electrophoresis indicated a single protein band corresponding to hPON1. The six analgesics dose-dependently decreased in vitro hPON1 activity, with IC 50 values for lornoxicam, indomethacin, tenoxicam, diclofenac sodium, ketoprofen and lincomycine of 0. 136, 0.195, 0.340, 1.639, 6.23 and 9.638 mM, respectively. K i constants were 0.009, 0.097, 0.306, 0.805, 13.010 and 11.116 mM, respectively. Analgesics showed different inhibition mechanisms: lornoxicam, diclofenac sodium and lincomycine were uncompetitive, indomethacin and tenoxicam were competitive, ketoprofen was noncompetitive. According to the results, inhibition potency was lornoxicam>indomethacin>tenoxicam> diclofenac sodium>ketoprofen> lincomycine.

Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols including natural products

“…CA II inhibitors are used for several purposes, in particular for the treatment of glaucoma, epilepsy, and as diuretics or antitumor agents/diagnostic tools 18,19,29 . Many chemical substances and synthesized drugs affect metabolisms by changing enzyme activities [30][31][32][33] . As CA II inhibitors are valuable molecules for therapeutical and pharmacological applications, we have synthesized novel bormophenols in the current research and evaluated their potency to be novel carbonic anhydrase inhibitors.…”

Synthesis and paroxonase activities of novel bromophenols

“…The precipitation intervals for paraoxonase were 60-80% 20 . The precipitate was collected by centrifugation at 15,000 rpm for 20 min and redissolved in 100 mM Na-phosphate buffer (pH 7.0).…”

Influence of Cobalt and Zinc Exposure on mRNA Expression Profiles of Metallothionein and Cytocrome P450 in Rainbow Trout

“…A number of studies have addressed the hazardous impacts of various chemicals, drugs, metals, and anions on enzyme and gene expression levels of different organisms, and this issue has become very popular due to the deep need for environmental safety and ecotoxicology investigations [25][26][27][28][29][30]. Thus, it is important to perform further studies with various organisms in order to characterize the hazards and to explain mechanisms of actions.…”