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氯霉素和大环内酯类衍生抗生素在体外可抑制人血清和人肝癌细胞(HepG2)中的对氧磷酶活性。

Amphenicol and macrolide derived antibiotics inhibit paraoxonase enzyme activity in human serum and human hepatoma cells (HepG2) in vitro.

作者信息

Sinan S, Kockar F, Gencer N, Yildirim H, Arslan O

机构信息

Balikesir University, Science and Art Faculty, Department of Biology/Biochemistry Section, Balikesir, Turkey.

出版信息

Biochemistry (Mosc). 2006 Jan;71(1):46-50. doi: 10.1134/s0006297906010068.

DOI:10.1134/s0006297906010068
PMID:16457617
Abstract

Human serum paraoxonase (hPON1) was separately purified by ammonium sulfate precipitation and hydrophobic interaction chromatography. The in vitro effects of commonly used antibiotics, namely clarithromycin and chloramphenicol, on purified human serum paraoxonase enzyme activity (serum hPON1) and human hepatoma (HepG2) cell paraoxonase enzyme activity (liver hPON1) were determined. Serum hPON1 and liver hPON1 were determined using paraoxon as a substrate and IC(50) values of these drugs exhibiting inhibition effects were found from graphs of hydratase activity (%) by plotting concentration of the drugs. We determined that chloramphenicol and clarithromycin were effective inhibitors of serum hPON1.

摘要

人血清对氧磷酶(hPON1)通过硫酸铵沉淀和疏水相互作用色谱法分别进行纯化。测定了常用抗生素,即克拉霉素和氯霉素,对纯化的人血清对氧磷酶活性(血清hPON1)和人肝癌(HepG2)细胞对氧磷酶活性(肝脏hPON1)的体外作用。以对氧磷为底物测定血清hPON1和肝脏hPON1,并通过绘制药物浓度的水化酶活性(%)图,从这些具有抑制作用的药物的图中得出半数抑制浓度(IC50)值。我们确定氯霉素和克拉霉素是血清hPON1的有效抑制剂。

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