OUT-OF-MIND INHIBITORS OF HUMAN SERUM PARAOXONASE 1 (PON1): AN IN VITRO STUDY

4-(dimethylamino)benzaldehyde, 3,5-dinitrosalicylic acid, berylliumsulfate tetrahydrate, urea, sodium azide, iron(II)sulfateheptahydrate, 2-thiobarbituric acid, benzidine, and hydrazinium sulfate, which are commonly used in the pharmaceutical industry and medical studies, have been examined as novel type of inhibitors of PON1. PON1 was purified by hydrophobic column of Sepharose-4B-coupled L-tyrosine- 1-naphthylamine. PON1 enzyme activity towards paraoxon substrate was quantified spectrophotometrically. A critical overview of the effects of these nine reagents on PON1 which associated with cardiovascular diseases has been given. The IC50 values were between 1.26×10-4 M and 2.31×10-4 M and benzidine showed the best inhibitory effect (IC50 = 1.26×10-4M) for PON1 enzyme activity.

Keywords:

Cardiovascular disease, PON1, Antioxidant activity, Inhibition, HDL-C LDL-C,

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