In vitro human metabolism of permethrin isomers alone or as a mixture and the formation of the major metabolites in cryopreserved primary hepatocytes

Toxicology in Vitro : an International Journal Published in Association with BIBRA
M-E WilleminC Brochot

Abstract

In vitro metabolism of permethrin, a pyrethroid insecticide, was assessed in primary human hepatocytes. In vitro kinetic experiments were performed to estimate the Michaelis-Menten parameters and the clearances or formation rates of the permethrin isomers (cis- and trans-) and three metabolites, cis- and trans-3-(2,2 dichlorovinyl)-2,2-dimethyl-(1-cyclopropane) carboxylic acid (cis- and trans-DCCA) and 3-phenoxybenzoic acid (3-PBA). Non-specific binding and the activity of the enzymes involved in permethrin's metabolism (cytochromes P450 and carboxylesterases) were quantified. Trans-permethrin was cleared more rapidly than cis-permethrin with a 2.6-factor (25.7±0.6 and 10.1±0.3 μL/min/10(6) cells respectively). A 3-factor was observed between the formation rates of DCCA and 3-PBA obtained from trans- and cis-permethrin. For both isomers, the rate of formation of DCCA was higher than the one of 3-PBA. The metabolism of the isomers in mixture was also quantified. The co-incubation of isomers at different ratios showed the low inhibitory potential of cis- and trans-permethrin on each other. The estimates of the clearances and the formation rates in the co-incubation condition did not differ from the estimates obtained with a separ...Continue Reading

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Citations

Jan 24, 2016·Toxicology and Applied Pharmacology·Marie-Emilie WilleminCéline Brochot
May 18, 2016·Environmental Research·Xu WangZonghui Yuan
Apr 17, 2018·Journal of Applied Toxicology : JAT·Rachid JellaliEric Leclerc
Feb 20, 2018·Frontiers in Microbiology·Hui ZhanShaohua Chen
Oct 9, 2019·Toxicological Sciences : an Official Journal of the Society of Toxicology·Pankajini MallickMiyoung Yoon
Feb 11, 2020·Toxicological Sciences : an Official Journal of the Society of Toxicology·Miwa KondoTomoya Yamada
Mar 30, 2021·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·Rachid JellaliEric Leclerc
May 13, 2018·Toxicology and Applied Pharmacology·Keyvin DarneyVirginie Desvignes
Jul 4, 2020·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·Marie VanackerAmélie Crépet

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