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. 2019 Oct;71(10):1576-1583.
doi: 10.1111/jphp.13144. Epub 2019 Jul 26.

The behaviour of some antihypertension drugs on human serum paraoxonase-1: an important protector enzyme against atherosclerosis

Yeliz Demir  1   2
Affiliations

The behaviour of some antihypertension drugs on human serum paraoxonase-1: an important protector enzyme against atherosclerosis

Yeliz Demir. J Pharm Pharmacol. 2019 Oct.

Abstract

Objectives: Paraoxonase-1 (PON1) enzyme is related to high-density lipoprotein (HDL), which is calcium dependent. It has essential roles such as protecting LDL against oxidation and detoxification of highly toxic substances. It is a significant risk to reduce the levels of this enzyme in patients with diabetes mellitus, cardiovascular diseases, hyperthyroidism and chronic renal failure.

Methods: Here, it was reported that the purification of human serum PON1 using straightforward methods and determination of the interactions between some antihypertension drugs and the enzyme.

Key finding: It was found that these drugs exhibit potential inhibitor properties for human serum PON1 with IC50 values in the range of 131.40-369.40 μm and Ki values in the range of 56.24 ± 6.75-286.74 ± 28.28 μm. These drugs showed different inhibition mechanisms. It was determined that midodrine and nadolol were exhibited competitive inhibition, but atenolol and pindolol were exhibited non-competitive inhibition.

Conclusion: Usage of these drugs would be hazardous in some cases.

Keywords: enzyme purification; hypertension; inhibition; paraoxonase; β-adrenoceptor blocking drugs.

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