In vitro screening of 200 pesticides for agonistic activity via mouse peroxisome proliferator-activated receptor (PPAR)α and PPARγ and quantitative analysis of in vivo induction pathway
In vitro screening of 200 pesticides for agonistic activity via mouse peroxisome proliferator-activated receptor (PPAR)α and PPARγ and quantitative analysis of in vivo induction pathway
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DOI：
10.1016/j.taap.2006.08.011
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发表时间：
2006-12-15
影响因子：
3.8
通讯作者：
Kojima, Hiroyuki
中科院分区：
文献类型：
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作者：
Takeuchi, Shinji;Matsuda, Tadashi;Kojima, Hiroyuki
过氧化物酶体增殖激活受体（PPARs）是依赖配体的转录因子，是脂质代谢和细胞分化的关键调节因子。然而，很少有研究报道各种环境化学物质可能与这些受体相互作用。在本研究中，我们利用CV-1猴肾细胞，通过体外报告基因测定了200种农药（29种有机氯、1种二苯醚、56种有机磷农药、12种拟除虫菊酯、22种氨基甲酸酯、1种酸酰胺、7种三嗪类、8种脲类和44种其他农药）对小鼠PPAR α和PPAR γ的拮抗活性。在200种农药中，具有不同化学结构的双氯灭、除虫菊酯和吡唑啉显示出PPAR α介导的转录活性，且呈剂量依赖性。另一方面，200种农药均未表现出一定浓度的PPAR γ拮抗活性
Peroxisome proliferator-activated receptors (PPARs) are ligand-dependent transcription factors and key regulators of lipid metabolism and cell differentiation. However, there have been few studies reporting on a variety of environmental chemicals, which may interact with these receptors. In the present study, we characterized mouse PPAR alpha and PPAR gamma agonistic activities of 200 pesticides (29 organochlorines, I I diphenyl ethers, 56 organophosphorus pesticides, 12 pyrethroids, 22 carbamates, I I acid amides, 7 triazines, 8 ureas and 44 others) by in vitro reporter gene assays using CV-1 monkey kidney cells. Three of the 200 pesticides, diclofop-methyl, pyrethrins and imazalil, which have different chemical structures, showed PPAR alpha-mediated transcriptional activities in a dose-dependent manner. On the other hand, none of the 200 pesticides showed PPAR gamma agonistic activity at concentrations