☆ 4.3 Article

Some indazoles reduced the activity of human serum paraoxonase 1, an antioxidant enzyme: in vitro inhibition and molecular modeling studies

ARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRY (2019)

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ARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRY
卷 125, 期 5, 页码 387-395

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TAYLOR & FRANCIS LTD
DOI: 10.1080/13813455.2018.1470646

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Enzyme inhibition; molecular modeling; paraoxonase 1; purification; indazole

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Biochemistry & Molecular Biology Biophysics Endocrinology & Metabolism Physiology

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Background: Paraoxonase 1 (PON1: EC 3.1.8.1) is a vital antioxidant enzyme against mainly atherosclerosis and many other diseases associated with oxidative stress. Thus, studies related to PON1 have an important place in the pharmacology. In this study, we aimed to evaluate the in vitro inhibition effects of some indazoles on the activity of human PON1. Methods: PON1 was purified from human serum with a specific activity of 5000?U/mg and 13.50% yield by using simple chromatographic methods. Results: The indazoles showed K-i values in a range of 26.0???3.00?111???31.0??M against hPON1. All these indazoles exhibited competitive inhibition. In addition, molecular docking studies were performed in order to assess the probable binding mechanisms into the active site of hPON1. Molecular modeling studies confirmed our results. Conclusions: Inhibition of PON1 by indazoles supplies a verification to further consideration of limitation dosage of indazole molecule groups as drug.

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