Characterization of estrogen receptor α activities in polychlorinated biphenyls by in vitro dual-luciferase reporter gene assay.

Polychlorinated biphenyls (PCBs) are thought to cause adverse health effects, particularly endocrine disruption. However, results on the estrogenic activities of a large set of PCB congeners through hormone receptors have not been fully studied. In this study, we evaluated the anti/estrogenic effects of 20 PCBs using an in vitro dual-luciferase reporter gene assay. PCB 18, 28, 49, 52, 99, 101, 103, 110, and 128 exhibited estrogenic effects, whereas PCB 118, 138, 163, 170, 180, 187, 194, 199 and 203 behaved as anti-estrogens. In particular, PCB 30 and 44 exhibited both agonistic and antagonistic activities in the dual-luciferase reporter gene assay. The results obtained from the dual-luciferase reporter gene assay, yeast two-hybrid assay and E-SCREEN were compared, suggesting that the dual-luciferase reporter gene assay is a useful approach for high-throughput screening. We also predicted the possible relationship between the chemical structures and the estrogenic effects of PCBs.

[1]  M. van den Berg,et al.  Impact of Polychlorinated Biphenyls Contamination on Estrogenic Activity in Human Male Serum , 2005, Environmental health perspectives.

[2]  B. Pinto,et al.  Estrogen-like activity of seafood related to environmental chemical contaminants , 2006, Environmental health : a global access science source.

[3]  B. Ozenberger,et al.  Selective uptake of estrogenic compounds by Saccharomyces cerevisiae: a mechanism for antiestrogen resistance in yeast expressing the mammalian estrogen receptor. , 1995, Endocrinology.

[4]  S. Takeuchi,et al.  Nuclear Hormone Receptor Activity of Polybrominated Diphenyl Ethers and Their Hydroxylated and Methoxylated Metabolites in Transactivation Assays Using Chinese Hamster Ovary Cells , 2009, Environmental health perspectives.

[5]  J. Sumpter.  Endocrine Disrupters in the Aquatic Environment: An Overview , 2005 .

[6]  Åke Bergman,et al.  State of the Science of Endocrine Disrupting Chemicals - 2012 , 2012 .

[7]  V. Ceja-Moreno,et al.  Organochlorine Pesticides and Polychlorinated Biphenyls Levels in Human Milk from Chelem, Yucatán, México , 2008, Bulletin of environmental contamination and toxicology.

[8]  Zhiyan Pan,et al.  Enantioselectivity in estrogenic potential and uptake of bifenthrin. , 2007, Environmental science & technology.

[9]  C. Portier,et al.  Evaluation of chemicals with endocrine modulating activity in a yeast-based steroid hormone receptor gene transcription assay. , 1997, Toxicology and applied pharmacology.

[10]  John D Spengler,et al.  Estrogenic activity of polychlorinated biphenyls present in human tissue and the environment. , 2006, Environmental science & technology.

[11]  K. Arcaro,et al.  2,2',6,6'‐tetrachlorobiphenyl is estrogenic in vitro and in vivo , 1999, Journal of cellular biochemistry.

[12]  G. Jiang,et al.  The in Vitro Estrogenic Activities of Polyfluorinated Iodine Alkanes , 2011, Environmental health perspectives.

[13]  Eiji Katsura,et al.  Screening for estrogen and androgen receptor activities in 200 pesticides by in vitro reporter gene assays using Chinese hamster ovary cells. , 2004, Environmental health perspectives.

[14]  P. Pomeroy,et al.  Effects of polychlorobiphenyls, polybromodiphenylethers, organochlorine pesticides and their metabolites on vitamin A status in lactating grey seals. , 2013, Environmental research.

[15]  T. Cajthaml,et al.  New in vitro reporter gene bioassays for screening of hormonal active compounds in the environment , 2010, Applied Microbiology and Biotechnology.

[16]  R. Cooper,et al.  Environmental endocrine disruption: an effects assessment and analysis. , 1998, Environmental health perspectives.

[17]  A M Vinggaard,et al.  Effect of highly bioaccumulated polychlorinated biphenyl congeners on estrogen and androgen receptor activity. , 2001, Toxicology.

[18]  E. Budtz-Jørgensen,et al.  Reproductive hormone profile and pubertal development in 14-year-old boys prenatally exposed to polychlorinated biphenyls. , 2012, Reproductive toxicology.

[19]  A. Trocino,et al.  PCBs contamination in farmed European sea bass from different Italian rearing systems. , 2009, Chemosphere.

[20]  V. J. Moreno,et al.  Polychlorinated biphenyls in different trophic levels from a shallow lake in Argentina. , 2002, Chemosphere.

[21]  S. Shiau,et al.  Activation of the human estrogen receptor by estrogenic and antiestrogenic compounds in Saccharomyces cerevisiae: a positive selection system. , 1995, Gene.

[22]  E. Zeng,et al.  Short-range transport of contaminants released from e-waste recycling site in South China. , 2011, Journal of Environmental Monitoring.

[23]  M. Perry,et al.  Environmental Exposure to Polychlorinated Biphenyls and p,p´-DDE and Sperm Sex-Chromosome Disomy , 2011, Environmental health perspectives.

[24]  Weiping Liu,et al.  Understanding the endocrine disruption of chiral pesticides: The enantioselectivity in estrogenic activity of synthetic pyrethroids , 2010 .

[25]  P.R.S. Kodavanti.  Polychlorinated Biphenyls (PCBs) , 2014 .

[26]  Yankai Xia,et al.  Assessing hormone receptor activities of pyrethroid insecticides and their metabolites in reporter gene assays. , 2010, Toxicological sciences : an official journal of the Society of Toxicology.

[27]  P. K. Lam,et al.  Polychlorinated biphenyls (PCBs) in marine fishes from China: levels, distribution and risk assessment. , 2012, Chemosphere.

[28]  W. Karasov,et al.  Effect of mono-ortho and di-ortho substituted polychlorinated biphenyl (PCB) congeners on leopard frog survival and sexual development. , 2008, Chemosphere.

[29]  S. Radice,et al.  Different effects of PCB101, PCB118, PCB138 and PCB153 alone or mixed in MCF-7 breast cancer cells. , 2008, Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association.

[30]  Lisa A. Rodenburg,et al.  Source apportionment of polychlorinated biphenyls in Chicago air from 1996 to 2007. , 2013, Environmental science & technology.

[31]  Xiaoping Zhou,et al.  Polychlorinated dibenzo-p-dioxins/furans (PCDD/Fs), polychlorinated biphenyls (PCBs), and polybrominated diphenyl ethers (PBDEs) in breast milk from Zhejiang, China. , 2012, Environment international.

[32]  A. di Domenico,et al.  Serum levels of PCDDs, PCDFs and PCBs in non-occupationally exposed population groups living near two incineration plants in Tuscany, Italy. , 2008, Chemosphere.

[33]  R. Kocan,et al.  Possible effects of polychlorinated biphenyls on sex determination in rainbow trout , 1998 .