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Influence of Pesticides on UDP-glucuronosyltransferase in Rat Liver Microsomes

✍ Scribed by Naydenova, Zlatina; Urshev, Zoltan; Golovinsky, Evgeny; Grancharov, Konstantin

Publisher
John Wiley and Sons
Year
1996
Tongue
English
Weight
542 KB
Volume
47
Category
Article
ISSN
1526-498X

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✦ Synopsis

Fifteen pesticides, representatives of different chemical groups, were tested for their inhibitory effect on the glucuronidation of 4-nitrophenol (4-NP) and phenolphthalein (PPh) by rat liver microsomes. Three herbicides (simazine, chlorsulfuron, tribenuron-methyl), two insecticides (dioxacarb, carbaryl) and one fungicide (zineb) significantly decreased the UDP-glucuronosyltransferase (UDPGT) activity. The carbamate insecticide dioxacarb was found to be the most potent inhibitor, at 1 mM concentration suppressing 4-NP-UDPGT activity completely, and reducing by 55% the activity associated with the conjugation of PPh. One millimole simazine and carbaryl affected only 4-NP glucuronidation, while chlorsulfuron and zineb exerted a marked inhibition of both 4-NP and PPh conversion. Concentrations of 0-1 m M carbaryl, dioxacarb and zineb were still inhibitory against 4-NP-UDPGT, with zineb producing 40% inhibition of PPh glucuronidation. As a whole, UDPGT isoforms conjugating PPh were less sensitive to the agrochemicals tested. Kinetic studies with dioxacarb, chlorsulfuron and carbaryl revealed a mixed type of inhibition with respect to the acceptor substrate 4-NP, with apparent Ki values of 70 PM, 120 PM and 160 PM, respectively.

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