Metabolism-related assays and their application to agrochemical research: reactivity of pesticides with glutathione and glutathione transferases†
✍ Scribed by Clarke, Eric D.; Greenhow, Daren T.; Adams, David
- Book ID
- 101215230
- Publisher
- John Wiley and Sons
- Year
- 1998
- Tongue
- English
- Weight
- 169 KB
- Volume
- 54
- Category
- Article
- ISSN
- 1526-498X
No coin nor oath required. For personal study only.
✦ Synopsis
An HPLC-based assay system has been developed to measure the reactivity of agrochemicals with glutathione (GSH) with and without catalysis by glutathione transferases (GSTs). Metabolism-related parameters based on second-order related rate constants from non-enzymatic GSH and enzymatic GSH ] GST assays have been derived for use in structureÈactivity and structureÈreactivity relationship studies of exploratory agrochemicals. The versatility and sensitivity of the assay system has been established using a diverse range of agrochemicals and model compounds, e.g. 4-nitrobenzyl chloride, 1chloro-2,4-dinitrobenzene, atrazine, acetochlor, Ñuorodifen, Ñuazifop-butyl, tridiphane, Ñuazinam, chlorothalonil and diazinon. For the enzymatic GSH ] GST assay, second-order related rate constants, ratioed to the assay standard, 4nitrobenzyl chloride to provide a parameter independent of assay conditions, spanned Ðve orders of magnitude, Ñuazinam being the most reactive and atrazine the least. Within chemical classes signiÐcant variations in reactivity were observed, alachlor being c.15-fold more reactive than pretilachlor. Applications of this assay system based on comparative measures of reactivity across and within chemical classes are discussed.