Effects of mono and dinuclear copper(II) complexes derived from non-steroidal anti-inflammatory drug naproxen on human serum paraoxanase1 (PON1) activity


Esra Dilek, Sema Caglar




The inhibition of human paraoxonase 1 (PON1, EC enzyme, with two Cu(II) complexes derived from naproxen was investigated by using the paraoxonase activity method with diethyl 4-nitrophenyl phosphate as substrate. The complexes [Cu2(µ-nap)4(3-pic)2] (1) and [Cu(nap)2(H2O)(4-pic)2] (2) decreased the in vitro PON1 activity with different inhibition mechanisms. The inhibition mechanism of complex 1 was uncompetitive whereas complex 2 was noncompetitive inhibitors. In this study, complexes mentioned above showed effective inhibitory activity on PON1.  IC50 values for [Cu2(µ-nap)4(3-pic)2] (1) and [Cu(nap)2(H2O)(4-pic)2] (2) were of 0.109 mM and 0.103 mM for PON1, respectively. Ki values for complex 1 and complex 2 were of 0.116 mM and 0.121 mM for PON1, respectively.




paraoxonase1; inhibition; copper(II) complexes; enzyme; inhibitor


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DOI: http://dx.doi.org/10.7439/ijpc.v5i6.2094

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