Enantioselective metabolism of quizalofop-ethyl in rat

Yiran Liang; Peng Wang; Donghui Liu; Zhigang Shen; Hui Liu; Zhixin Jia; Zhiqiang Zhou

doi:10.1371/journal.pone.0101052

Enantioselective metabolism of quizalofop-ethyl in rat

PLoS One. 2014 Jun 25;9(6):e101052. doi: 10.1371/journal.pone.0101052. eCollection 2014.

Authors

Yiran Liang¹, Peng Wang¹, Donghui Liu¹, Zhigang Shen¹, Hui Liu¹, Zhixin Jia², Zhiqiang Zhou¹

Affiliations

¹ Department of Applied Chemistry, China Agricultural University, Beijing, PR China.
² Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, PR China.

Abstract

The pharmacokinetic and distribution of the enantiomers of quizalofop-ethyl and its metabolite quizalofop-acid were studied in Sprague-Dawley male rats. The two pairs of enantiomers were determined using a validated chiral high-performance liquid chromatography method. Animals were administered quizalofop-ethyl at 10 mg kg(-1) orally and intravenously. It was found high concentration of quizalofop-acid in the blood and tissues by both intragastric and intravenous administration, and quizalofop-ethyl could not be detected through the whole study which indicated a quick metabolism of quizalofop-ethyl to quizalofop-acid in vivo. In almost all the samples, the concentrations of (+)-quizalofop-acid exceeded those of (-)-quizalofop-acid. Quizalofop-acid could still be detected in the samples even at 120 h except in brain due to the function of blood-brain barrier. Based on a rough calculation, about 8.77% and 2.16% of quizalofop-acid were excreted through urine and feces after intragastric administration. The oral bioavailability of (+)-quizalofop-acid and (-)-quizalofop-acid were 72.8% and 83.6%.

Publication types

Comparative Study
Research Support, Non-U.S. Gov't

MeSH terms

Administration, Oral
Animals
Area Under Curve
Biological Availability
Chromatography, High Pressure Liquid
Male
Propionates / administration & dosage
Propionates / chemistry
Propionates / pharmacokinetics*
Quinoxalines / administration & dosage
Quinoxalines / chemistry
Quinoxalines / pharmacokinetics*
Rats
Rats, Sprague-Dawley
Stereoisomerism
Substrate Specificity
Tissue Distribution

Substances

Propionates
Quinoxalines
quizalofop
quizalofop-ethyl

Grants and funding

Supported by A Foundation for the Author of National Excellent Doctoral Dissertation of PR China, Program for New Century Excellent Talents in University (NCET09-0738), the National Natural Science Foundation of China (21277171, 21307155), the New-Star of Science and Technology supported by Beijing Metropolis, Program for New Century Excellent Talents in University and Program for Changjiang Scholars and Innovative Research Team in University. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.