Carbaryl, 1-naphthol and 2-naphthol inhibit the beta-1 thyroid hormone receptor-mediated transcription in vitro

Sun, Hong; Shen, Ouxi; Xu, Xiaolin; Lin, Song; Wang, Xinru

doi:10.1016/j.tox.2008.05.008

Cited by 84 publications

(41 citation statements)

References 33 publications

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“…DEGs identified in DAVID were classified by Fisher's exact test using a cut-off of p⁄0.01, to select overrepresented GO biological processes. Carbaryl changed in circulating THs in the freshwater catfish Clarias batrachus and induced thyroid dysfunction 8 . It is reported that carbaryl caused an increase in both T 3 and T 3 /T 4 ratio in C. batrachus 8 .…”

Section: Comparison Of Biological Function In Carbaryl and Vinclozolinmentioning

confidence: 99%

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Genome-wide expression profiling of carbaryl and vinclozolin in human thyroid follicular carcinoma (FTC-238) cells

et al. 2010

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Environmental chemicals have attracted attention owing to their effects on thyroid functions, because thyroid hormones (THs) play key roles in the development of mammalian organs such as the brain and heart. Carbaryl, which is used as an insecticide, is a cholinesterase inhibitor and is toxic to humans. It is classified as a likely human carcinogen by the United States Environmental Protection Agency (EPA). It induces thyroid dysfunction by acting as a thyroid receptor (TR) antagonist and altering the circulating levels of THs; it increases triiodothryonine (T 3 ) levels. Vinclozolin is a fungicide and is known as an endocrine disruptor. Vinclozolin decreases circulating thyroxine (T 4 ) levels and increases thyroid stimulating hormone (TSH) levels. We examined the changes in gene expression profiles in human thyroid follicular carcinoma FTC-238 cells that were exposed to carbaryl and vinclozolin and various chemicals by using a human oligonucleotide chip. Several genes altered by carbaryl and vinclozolin belonged to the gene ontology (GO) categories of cell cycle, apoptosis, development, and metabolism. Further, we identified 106 classifiers represent in the contrast the reaction in thyroid systems by carbaryl and vinclozolin. These classifiers are potential biomarkers of the final symptoms (i.e., hyperthyroidism and hypothyroidism) that result from disruption of THs production. In conclusion, our study suggests potential biomarkers and biological functions related to thyroid dysfunction and biological functions to be investigated in response to the exposure of environmental chemicals such as carbaryl and vinclozolin. BioChip J. (2010) 4(2): 89-98 91 157

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Section: Comparison Of Biological Function In Carbaryl and Vinclozolinmentioning

confidence: 99%

“…Carbaryl, which is one of the most important broad-spectrum carbamate insecticides, has been used since approximately 30 years for different crops and ornamental plants 8 . World Health Organization (WHO) reported that carbaryl at high doses is carcinogenic for rats 9 .…”

Section: Original Researchmentioning

confidence: 99%

Genome-wide expression profiling of carbaryl and vinclozolin in human thyroid follicular carcinoma (FTC-238) cells

et al. 2010

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“…Cell culture and exposure were conducted according to Sun et al (2008a) and Xu et al (2006). For different endocrine-disrupting activity testing systems, cells were transfected with different plasmids and transfection reagents (Table 1).…”

Section: Cell Culture and Transfectionmentioning

confidence: 99%

“…Chemicals can mimic ER and AR agonists and cause morphologic abnormalities. Research about chemicals that can interact with the AR as agonists or antagonists showed that industrial chemicals were AR antagonists (Sun et al 2008a). More recently, compounds that can interact with the thyroid hormone receptor (TR) have aroused more concern (Gaido et al 1997;Devito et al 1999).…”

Section: Introductionmentioning

confidence: 99%

Endocrine-disrupting equivalents in industrial effluents discharged into Yangtze River

Shi

Wang

et al. 2009

Ecotoxicology

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The endocrine-disrupting equivalents in effluents from three chemical industry wastewater treatment systems in the vicinity of Yangtze River were determined by several transactivation reporter gene assays. Transient transfections of African green monkey kidney cell line (CV-1) were used to determine the estrogenic, anti-androgenic and anti-thyroid equivalents in the effluents. Organic extracts of the effluents contained compounds that were potent anti-androgens and the activities measured as an equivalent concentration of flutamide were 45.53, 34.65 and 91.61 nM, respectively. The extracts also contained detectable concentrations of thyroid antagonists. Estrogenic activities, measured with the reporter gene assay, were near or below the method detection limit (0.58 pM as E2). Concentrations of some of the major constituents such as di(2-ethylhexyl)phthalate, dibutyl phthalate, 2,6-dinitrotoluene and nitrobenzene were quantified. The data suggest that the reporter gene assay is useful to predication of endocrine disrupting effects in polluted aquatic body.

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“…Exposure of carbaryl to catfish resulted in the suppression of serum level of thyroxin (Sinha et al, 1991). Sun et al (2008) have reported of the inhibitory effects of carbaryl, 1-naphthol, and 2-naphthol on the receptor-mediated transcription of thyroid hormones. Carbaryl also induces oxidative stress in snails (Leomanni et al, 2015).…”

Section: Introductionmentioning

confidence: 99%

Metabolism of methiocarb and carbaryl by rat and human livers and plasma, and effect on their PXR, CAR and PPARα activities

et al. 2016

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-The oxidative, reductive, and hydrolytic metabolism of methiocarb and the hydrolytic metabolism of carbaryl by liver microsomes and plasma of rats or humans were examined. The effects of the metabolism of methiocarb and carbaryl on their nuclear receptor activities were also examined. When methiocarb was incubated with rat liver microsomes in the presence of NADPH, methiocarb sulfoxide, and a novel metabolite, methiocarb sulfone were detected. Methiocarb sulfoxide was oxidized to the sulfone by liver microsomes and reduced back to methiocarb by liver cytosol. Thus, the interconversion between methiocarb and the sulfoxide was found to be a new metabolic pathway for methiocarb by liver microsomes. The product of methiocarb hydrolysis, which is methylthio-3,5-xylenol (MX), was also oxidized to sulfoxide form by rat liver microsomes. The oxidations were catalyzed by human flavincontaining monooxygenase isoform (FMO1). CYP2C19, which is a human cytochrome P450 (CYP) isoform, catalyzed the sulfoxidations of methiocarb and MX, while CYP1A2 also exhibited oxidase activity toward MX. Methiocarb and carbaryl were not enzymatically hydrolyzed by the liver microsomes, but they were mainly hydrolyzed by plasma and albumin to MX and 1-naphthol, respectively. Both methiocarb and carbaryl exhibited PXR and PPARα agonistic activities; however, methiocarb sulfoxide and sulfone showed markedly reduced activities. In fact, when methiocarb was incubated with liver microsomes, the receptor activities were decreased. In contrast, MX and 1-naphthol showed nuclear receptor activities equivalent to those of their parent carbamates. Thus, the hydrolysis of methiocarb and carbaryl and the oxidation of methiocarb markedly modified their nuclear receptor activities.

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Carbaryl, 1-naphthol and 2-naphthol inhibit the beta-1 thyroid hormone receptor-mediated transcription in vitro

Cited by 84 publications

References 33 publications

Genome-wide expression profiling of carbaryl and vinclozolin in human thyroid follicular carcinoma (FTC-238) cells

Genome-wide expression profiling of carbaryl and vinclozolin in human thyroid follicular carcinoma (FTC-238) cells

Endocrine-disrupting equivalents in industrial effluents discharged into Yangtze River

Metabolism of methiocarb and carbaryl by rat and human livers and plasma, and effect on their PXR, CAR and PPARα activities

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