共 50 条
The endocrine-disrupting potential of four chlorophenols by in vitro and in silico assay
被引:19
|作者:
Yu, Chang
[1
]
Wang, Chi
[2
]
Lu, Zhengbiao
[1
]
Zhang, Chen
[3
]
Dai, Wei
[1
]
Yu, Shuqing
[1
]
Lin, Shu
[1
]
Zhang, Quan
[1
]
机构:
[1] Zhejiang Univ Technol, Key Lab Microbial Technol Ind Pollut Control Zhej, Coll Environm, Hangzhou 310032, Zhejiang, Peoples R China
[2] Longyou Huashui Drinking Water Ind Co, Quzhou 324400, Zhejiang, Peoples R China
[3] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China
来源:
基金:
中国国家自然科学基金;
关键词:
Chlorophenols;
Endocrine-disrupting effects;
Molecular docking;
H295R;
RELATIVE BINDING AFFINITIES;
ALPHA-ESTROGEN-RECEPTOR;
PENTACHLOROPHENOL PCP;
FRESH-WATER;
VIVO;
ENVIRONMENT;
PESTICIDES;
HUMANS;
DIVERSITY;
CHEMICALS;
D O I:
10.1016/j.chemosphere.2018.11.199
中图分类号:
X [环境科学、安全科学];
学科分类号:
08 ;
0830 ;
摘要:
Chlorophenols (CPs) have mainly been used as a biocide, wood treatment agent and a byproduct of bleaching in paper mills. They have been a topic of concern due to their wide spread and potential effects on human and wildlife. However, data on the thresholds and effects of the number of chlorine atoms on the endocrine-disrupting potential of CPs remain scarce. In this study, we adopted two in vitro models (reporter gene assays and H295R cell line) to investigate the endocrine-disrupting effects of four CPs (pentachlorophenol (PCP), 2,4,6-trichlorophenol (2,4,6-TCP), 2,4-dichlorophenol (2,4-DCP) and 2-chlorophenol (2-CP)). The molecular docking platform was adopted to further confirm the results of the in vitro assessment. Our results revealed that PCP exhibited oestrogen receptor alpha (ER alpha) agonistic activity at the concentration of 10(-5) M and the value of REC20 was 1.9 x 10(-6) M. PCP and 2, 4, 6-TCP showed anti-oestrogenic activities with a RIC20 value of 2.8 x 10(-7) and 2.9 x 10(-6) M, respectively. Notably, only PCP exhibited thyroid hormone receptor beta (TR beta) antagonistic activity occurred at the concentration of 10(-5) M, with a RIC(20 )value of 1.3 x 10(-6) M. The oestrogenic and thyroid hormone effects of CPs may be dependent on the number of chlorine atoms. A higher number of chlorine atoms indicated the higher effect of four CPs. The results of molecular docking were consistent with the reporter gene assay. For H295R cell line assay, PCP induced the StAR upregulation, while CYP17 was downregulated in a concentration-dependent manner by PCP and 2, 4, 6-TCP. (C) 2018 Elsevier Ltd. All rights reserved.
引用
下载
收藏
页码:941 / 947
页数:7
相关论文