In vitro assessment of corticosteroid effects of eight chiral herbicides
In vitro assessment of corticosteroid effects of eight chiral herbicides
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八种手性除草剂皮质类固醇作用的体外评估
DOI：
10.1080/03601234.2019.1665408
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发表时间：
2020-02
影响因子：
2
通讯作者：
Liu Jing
中科院分区：
文献类型：
--
作者：
Shen Yuqing;Zhang Jianyun;Xie Jingqian;Liu Jing
关于手性除草剂的对映选择性内分泌干扰的信息很少。这项研究评估了八种典型的手性除草剂对皮质类固醇(包括糖皮质激素和矿物皮质激素)的干扰作用。用报告基因法研究了8种手性除草剂对CHOK1细胞糖皮质激素受体(GR)和盐皮质激素受体(MR)的对映选择性。采用酶联免疫吸附试验(EL ISA)进一步研究它们对H295R细胞分泌皮质类固醇激素的影响。在非细胞毒性浓度下，8种手性除草剂的外消旋体或对映体均未表现出GR或MR激动剂活性。在1.0×10~(-7)M和1.0×10~(-6)M时，R-异丙胺显著抑制醛固酮诱导的MR反式激活68.78%；1.0×10~(-6)M时，R-异丙胺和RAC-/R-异丙胺显著抑制皮质醇的分泌26.49%。1.0×10~(-5)M敌敌畏及其两个对映体在1.0×10~(-5)M浓度下对糖皮质激素的诱导率分别为75.60%、100.1%和68.78%。RAc-丙异氯(1.0×10(-6)M)、S-三氯杀灭(1.0×10(-5)M)或Rac-/S-/R-乙草胺(1.0×10(-6)M)和Rac-/S-/R-乳酸(1.0×10(-6)M)可抑制约40%的醛固酮分泌。我们的发现表明，手性除草剂以对映体选择性的方式破坏皮质类固醇的动态平衡。因此，需要进行更全面的筛查，以更好地了解手性农药的生态和健康风险。
Information regarding the enantioselective endocrine disruption of chiral herbicides is scarce. This study assessed the disrupting effects of eight typical chiral herbicides on corticosteroids (including glucocorticoids and mineralocorticoids). Enantioselectivity of eight chiral herbicides were evaluated for their agonistic/antagonistic effects on glucocorticoid receptor (GR) and mineralocorticoid receptor (MR) with CHOK1 cell line using reporter gene assay. Their influence on the production of corticosteroids were further investigated in H295R cell line using enzyme-linked immunosorbent assay (ELISA). None of the racemates or enantiomers of eight chiral herbicides exhibited GR or MR agonistic activity at non-cytotoxic concentrations. However, rac-propisochlor and S-imazamox antagonized cortisol-induced transactivation of GR by 21.79% and 38.73% at the concentration of 1.0 x 10(-7) M and 1.0 x 10(-6) M, respectively, and R-napropamide remarkably attenuated aldosterone-induced MR transactivation by 68.78% at 1.0 x 10(-6) M. The secretion of cortisol was significantly restrained after treated with 1.0 x 10(-6) M rac-propisochlor and rac-/R-napropamide at the concentration of 1.0 x 10(-6) M by 26.49%, 30.10% and 35.27%, respectively, while this glucocorticoid was remarkably induced by 1.0 x 10(-5) M rac-diclofop-methyl and its two enantiomers at the concentration of 1.0 x 10(-5) M by 75.60%, 100.1% and 68.78%, respectively. Exposure to rac-propisochlor (1.0 x 10(-6) M), S-diclofop-methyl (1.0 x 10(-5) M) or rac-/S-/R- acetochlor (1.0 x 10(-6) M) and rac-/S-/R-lactofen (1.0 x 10(-6) M) inhibited the secretion of aldosterone by approximately 40%. Our findings suggested that chiral herbicides disrupted corticosteroid homeostasis in an enantioselective way. Therefore, more comprehensive screening is required to better understand the ecological and health risks of chiral pesticides.
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DOI：
10.1161/hypertensionaha.116.07094
发表时间：
2016-09
期刊：
Hypertension (Dallas, Tex. : 1979)
影响因子：
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期刊：
The Science of the total environment
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影响因子：
8.8
作者：
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