Predictive Toxicity of Conventional Triazole Pesticides by Simulating Inhibitory Effect on Human Aromatase CYP19 Enzyme

Chachibaia, Tamar; Hoskeri, Joy H.

doi:10.4018/ijkdb.2016070104

Cited by 2 publications

(1 citation statement)

References 26 publications

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“…Fard et al (2016) found a negative effect of risatriptan on hepatocytes. Hepatocyte lysosomes and mitochondria have been shown to play an important role in risatriptan-induced cell injury (Chachibaia & Hoskeri, 2016).…”

Section: Introductionmentioning

confidence: 99%

Features of experimental modeling of tuberculosis in guinea pig with the participation of N'-(2-(5-((thephylline-7' yl)methyl)-4-R-1,2,4-triazole- ylthio)acethyl)isonicotinohydrazide

Gotsulya¹,

Zazhzharskiy²,

Давиденко³

2020

Ukr J Ecol

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In this study, no toxic effects were detected after single subcutaneous injection of 40 mg/kg tadpoles. The results of macro- and microscopic examination of the internal organs 14 days after single subcutaneous administration of N'-(2-(5-((thephylline-7'-yl)methyl)-4-ethyl-1,2,4-triazole-3-ylthio)acethyl)isonicotino-hydrazide (GKP-305) at a dose of 20, 40 mg/kg showed the absence of any anatomical and morphological abnormalities in the tissue structures of the tentacles. The calculated value of the drug indicates a high degree of safety GKP-305 and its prospects for veterinary practice as an effective and safe tuberculocidal drug.

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Section: Introductionmentioning

confidence: 99%

Features of experimental modeling of tuberculosis in guinea pig with the participation of N'-(2-(5-((thephylline-7' yl)methyl)-4-R-1,2,4-triazole- ylthio)acethyl)isonicotinohydrazide

Gotsulya¹,

Zazhzharskiy²,

Давиденко³

2020

Ukr J Ecol

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In Silico, In Vitro, and In Vivo Studies Indicate the Endocrine-Disrupting Effects of Cyproconazole Stereoisomers

He,

Li,

Zhou

et al. 2024

J. Agric. Food Chem.

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The widespread use of chiral triazole fungicide cyproconazole (CPZ) in agricultural fields has led to frequent detection of CPZ in the environment. The restriction of CPZ in the EU raised wide concerns regarding its potential endocrinedisrupting effects (EDEs). The present study was conducted to evaluate EDEs of CPZ stereoisomers in vitro, in silico, and in vivo. The reporter gene assay indicated that all CPZ stereoisomers were agonists to the human estrogenic receptor α. (2S,3S)-(+)-and (2R,3S)-(−)-CPZ exhibited stronger binding capacities to ERα compared with (2R,3R)-(−)-and (2S,3R)-(+)-CPZ. Our computational studies showed consistent results with reporter gene assay, elucidating the stereoselective binding mode of CPZ to estrogen receptor. In zebrafish embryos, the 96h-lethality of CPZ stereoisomers ordered (2R,3R)-(−)-> (2R,3S)-(−)-> (2S,3S)-(+)-> Rac-> (2S,3R)-(+)-CPZ. Stereoselective developmental toxicity of CPZ was observed while (2R,3S)-(−)-CPZ is the most toxic isomer. The estrogenic hormones were significantly decreased in (2S,3R)-(+)-and (2R,3S)-(−)-CPZ groups and enhanced in (2S,3S)-(+)-and (2R,3R)-(−)-CPZ, along with the gene expression in hypothalamic−pituitary−gonad axis altered. CPZ shows no thyroid hormone activity. These data clarified that CPZ is a new-found endocrine disruptor threatening human health and each stereoisomer of CPZ showed stereoselective EDEs by regulating the nuclear receptor-mediated gene expression.

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Predictive Toxicity of Conventional Triazole Pesticides by Simulating Inhibitory Effect on Human Aromatase CYP19 Enzyme

Cited by 2 publications

References 26 publications

Features of experimental modeling of tuberculosis in guinea pig with the participation of N'-(2-(5-((thephylline-7' yl)methyl)-4-R-1,2,4-triazole- ylthio)acethyl)isonicotinohydrazide

Features of experimental modeling of tuberculosis in guinea pig with the participation of N'-(2-(5-((thephylline-7' yl)methyl)-4-R-1,2,4-triazole- ylthio)acethyl)isonicotinohydrazide

In Silico, In Vitro, and In Vivo Studies Indicate the Endocrine-Disrupting Effects of Cyproconazole Stereoisomers

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