Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, Turkey.
Department of Pharmacy Services, Nihat Delibalta Göle Vocational High School, Ardahan University, Ardahan, Turkey.
J Pharm Pharmacol. 2019 Oct;71(10):1576-1583. doi: 10.1111/jphp.13144. Epub 2019 Jul 26.
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.
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.
It was found that these drugs exhibit potential inhibitor properties for human serum PON1 with IC values in the range of 131.40-369.40 μm and K 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.
Usage of these drugs would be hazardous in some cases.
对氧磷酶-1（PON1）酶与高密度脂蛋白（HDL）有关，而后者依赖于钙。它具有保护 LDL 免受氧化和解毒高毒性物质等重要作用。在糖尿病、心血管疾病、甲状腺功能亢进和慢性肾衰竭患者中，这种酶的水平降低是一个重大风险。
本研究采用简单的方法对人血清 PON1 进行了纯化，并测定了一些抗高血压药物与该酶之间的相互作用。
结果发现这些药物对人血清 PON1 具有潜在的抑制特性，IC50 值范围为 131.40-369.40μm，K 值范围为 56.24±6.75-286.74±28.28μm。这些药物显示出不同的抑制机制。确定米多君和纳多洛尔表现出竞争性抑制，而阿替洛尔和吲哚洛尔表现出非竞争性抑制。
在某些情况下，这些药物的使用可能会有危险。
