Distribution and tissue elimination in rats during and after prolonged dietary exposure to a highly fluorinated sulfonamide pesticide

Grossman, Mark R.; Mispagel, Michael E.; Bowen, John M.

doi:10.1021/jf00024a033

Cited by 21 publications

(24 citation statements)

References 10 publications

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“…No evidence is available about the in vivo autoactivation of UGT. The FOSA concentrations used in the current study were much higher than the blood concentrations of FOSA in experimental animals given FOSA (Manning et al, 1991;Grossman et al, 1992). The concentrations of FOSA in human sera have been reported (Olsen et al, 2003(Olsen et al, , 2005.…”

Section: Kinetic Parameters Of Fosa N-glucuronide Formation In Liver mentioning

confidence: 63%

“…In rats given 50 mg/kg N-ethylperfluorooctanesulfonamide p.o., the metabolically formed FOSA had a long elimination half-life (5 days) in blood and was present at a concentration of 25 M for 2 days in the elimination phase (Manning et al, 1991;Grossman et al, 1992). N-Glucuronidation of FOSA could be a major metabolic pathway to eliminate FOSA, although the hydrolysis of FOSA, which occurs at a slow rate, may also contribute to its elimination.…”

Section: Discussionmentioning

confidence: 99%

“…Perfluorooctanesulfonamide (FOSA) (Fig. 1) is a major metabolite of N-alkylperfluorooctanesulfonamides and has a long half-life in animals and in the environment (Manning et al, 1991;Grossman et al, 1992). FOSA is biotransformed to perfluorooctanesulfonic acid and FOSA N-glucuronide ( Fig.…”

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confidence: 99%

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N-GLUCURONIDATION OF PERFLUOROOCTANESULFONAMIDE BY HUMAN, RAT, DOG, AND MONKEY LIVER MICROSOMES AND BY EXPRESSED RAT AND HUMAN UDP-GLUCURONOSYLTRANSFERASES

Xu¹,

Krenitsky²,

Seacat³

et al. 2006

Drug Metab Dispos

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ABSTRACT:N-Alkylperfluorooctanesulfonamides have been used in a range of industrial and commercial applications. Perfluorooctanesulfonamide (FOSA) is a major metabolite of N-alkylperfluorooctanesulfonamides and has a long half-life in animals and in the environment and is biotransformed to FOSA N-glucuronide. The objective of this study was to identify and characterize the human and experimental animal liver UDP-glucuronosyltransferases (UGTs) that catalyze the N-glucuronidation of FOSA. The results showed that pooled human liver and rat liver microsomes had high Nglucuronidation activities. Expressed rat UGT1.1, UGT2B1, and UGT2B12 in HK293 cells catalyzed the N-glucuronidation of FOSA but at rates that were lower than those observed in rat liver microsomes. Of the 10 expressed human UGTs (1A1, 1A3, 1A4, 1A6, 1A9, 2B4, 2B7, 2B15, and 2B17) studied, only hUGT2B4 and hUGT2B7 catalyzed the N-glucuronidation of FOSA. The kinetics of N-glucuronidation of FOSA by rat liver microsomes and by hUGT2B4/7 was consistent with a single-enzyme Michaelis-Menten model, whereas human liver microsomes showed sigmoidal kinetics. These data show that rat liver UGT1.1, UGT2B1, and UGT2B12 catalyze the N-glucuronidation of FOSA, albeit at low rates, and that hUGT2B4 and hUGT2B7 catalyze the N-glucuronidation of FOSA.

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Section: Kinetic Parameters Of Fosa N-glucuronide Formation In Liver mentioning

confidence: 63%

Section: Discussionmentioning

confidence: 99%

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N-GLUCURONIDATION OF PERFLUOROOCTANESULFONAMIDE BY HUMAN, RAT, DOG, AND MONKEY LIVER MICROSOMES AND BY EXPRESSED RAT AND HUMAN UDP-GLUCURONOSYLTRANSFERASES

Xu¹,

Krenitsky²,

Seacat³

et al. 2006

Drug Metab Dispos

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“…7 A tissue sample weighing 0.5 g was cut into small pieces that were transferred to a 16 Â 100 mm culture test tube. An enzyme mixture containing 6 mg ml À1 collagenase and 4 mg ml À1 protease was prepared.…”

Section: Tissue Analysesmentioning

confidence: 99%

“…Prolonged exposure of young rats to sul¯uramid in their diet resulted in a transitory reduction in rate of weight gain. 7 In rabbit renal proximal tubule suspensions and isolated renal cortical mitochondria, sul¯uramid and desethylsul¯uramid uncoupled oxidative phosphorylation, which may provide a mechanism for mammalian toxicity. 8,9 Interest in the large-scale application of sul¯uramid to agricultural lands in a bait such as corn grits for control of the red imported ®re ant 10 requires knowledge of its potential for toxicity to exposed grazing animals and occurrence of residues in food products derived from these animals.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of sulfluramid and its metabolite desethylsulfluramid after intravenous and intraruminal administration of sulfluramid to sheep

Vitayavirasuk

Bowen

1999

Pestic. Sci.

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Pharmacokinetic properties and tissue residues of the insecticide sul¯uramid (I) and its major metabolite desethylsul¯uramid (II) were determined in healthy sheep after bolus intravenous (IV) administration (5 and 15 mg kg À1; n = 10) and bolus intraruminal (IR) administration (100 and 400 mg kg À1 ; n = 12) of I. Depression, lethargy, and dyspnea were noted for 4 h after the higher IV dose, but not after the other IV or IR doses. The time courses of the mean blood concentrations of I and II were best described by a two-compartment open model with rapid distribution and slow elimination phases. The blood-to-plasma concentration ratios for I and II were 1.43 (AE 0.50) and 26.7 (AE 9.41), respectively, suggesting binding of II to red blood cells. The T 1/2b values for I and II for the higher IV dose of I were 15.3 (AE 4.68) h and 63.4 (AE 4.75) h and for the higher IR dose of I, 31.5 (AE 5.41) h and 74.9 (AE 7.49) h, respectively. Bioavailability was 28.6 (AE 2.96)% for the lower IR dose and 19.5 (AE 0.99)% for the higher IR dose. C max values for II were higher in female than male sheep after IR administration of I. Only II was found in tissue samples, with the highest concentration being in liver (9.4 (AE 5.2) mg g À1 ).

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A rapid quantitative method for the analysis of sulfluramid and its isomers in ant bait by capillary column gas chromatography

Bastos¹,

Freitas

Pagliarussi

et al. 2001

J. Sep. Science

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Distribution and tissue elimination in rats during and after prolonged dietary exposure to a highly fluorinated sulfonamide pesticide

Cited by 21 publications

References 10 publications

N-GLUCURONIDATION OF PERFLUOROOCTANESULFONAMIDE BY HUMAN, RAT, DOG, AND MONKEY LIVER MICROSOMES AND BY EXPRESSED RAT AND HUMAN UDP-GLUCURONOSYLTRANSFERASES

N-GLUCURONIDATION OF PERFLUOROOCTANESULFONAMIDE BY HUMAN, RAT, DOG, AND MONKEY LIVER MICROSOMES AND BY EXPRESSED RAT AND HUMAN UDP-GLUCURONOSYLTRANSFERASES

Pharmacokinetics of sulfluramid and its metabolite desethylsulfluramid after intravenous and intraruminal administration of sulfluramid to sheep

A rapid quantitative method for the analysis of sulfluramid and its isomers in ant bait by capillary column gas chromatography

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