Effect of Fluorine Atoms and Piperazine Rings on Biotoxicity of Norfloxacin Analogues: Combined Experimental and Theoretical Study.

ABSTRACT: To clarify the effect of the fluorine atom and piperazine ring on norfloxacin (NOR), NOR degradation products (NOR-DPs, P1-P8) were generated via UV combined with hydrogen peroxide (UV/H₂O₂) technology. NOR degradation did not significantly affect cytotoxicity of NOR against BV2, A549, HepG2, and Vero E6 cells. Compared with that of NOR, mutagenicity and median lethal concentration of P1-P8 in fathead minnow were increased, and bioaccumulation factor and oral median lethal dose of P1-P8 in rats were decreased. Molecular docking was used to evaluate the inhibitory effect of DNA gyrase A (gyrA) on NOR-DPs to determine the molecular-level mechanism and establish the structure-activity relationship. Results indicated that the most common amino acid residues were Ile13, Se

SUBMITTER: Yang C 

PROVIDER: S-EPMC11667292 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature