title: Impacts of some antibiotics on human serum paraoxonase 1 activity.
abstract: Some enzymes are known to be drug target inhibitions of which can be critical for organisms. PON has a critical role to prevent atherogenesis by inhibiting lipid peroxidation. It is well known that paraoxonase 1 (PON1) plays an important function on high-density lipoprotein (HDL) structure to prevent lipid oxidation not only of low-density lipoprotein, but also of HDL itself. We investigated in vitro effects of some medical drugs on PON1 activity from human serum. Ki constants for oxytetracycline hydrochloride, netilmycin sulfate, lincomycin hydrochloride, clindamycin phosphate, and streptomycin sulfate were found as 0.2, 3.73, 18.30, 35.80, and 56.30 mM, respectively. Our results indicate that these commonly used drugs inhibit the activity of the enzyme at very low doses with different inhibition mechanisms.
authors.affiliation: Department of Chemistry, Division of Biochemistry, Science Faculty, Atatürk University, Erzurum, Turkey.
authors.forename: Esra Bayram
authors.initials: EB
authors.lastname: Dilek
authors.forename: Ömer İrfan
authors.initials: Öİ
authors.lastname: Küfrevioğlu
authors.forename: Şükrü
authors.initials: Ş
authors.lastname: Beydemir
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D043303:Aryldialkylphosphatase / Q000037:antagonists & inhibitors* / Q000097:blood / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008968:Molecular Conformation; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D043303:Aryldialkylphosphatase; C468406:PON1 protein, human