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Steroid Hormone Receptor/Reporter Gene Transcription Assay for Food Additives and Contaminants
Sang-Hee Jeong,Joon-Hyoung Cho,Jong-Myung Park 한국독성학회 2006 Toxicological Research Vol.22 No.1
Many of endocrine disrupting chemicals induce effects via interaction with hormone receptors and responsive elements in target cells. We investigated endocrine disrupting effects of some food additives and contaminants including BHA, BHT, ethoxyquin, propionic acid, sorbic acid, benzoic acid, CPM, aflatoxin B1, cadmium chloride, genistein, TCDD and PCBs in yeast transformants expressing human steroid hormone receptors along with steroid responsive elements. The response limit of genetically recombinant yeast to 17β-estradiol, testosterone and progesterone was 1 × 10<SUP>-16</SUP>, 1 × 10<SUP>-12</SUP> and 1 × 10<SUP>-13</SUP> M, respectively. BHT induced weak transcriptional activity in estrogen sensitive yeast, while BHA and sorbic acid interacted weakly with androgen receptor/responsive element. CPM induced transcriptional activities in all types of yeasts sensitive to steroid hormones. Zearalenone and genistein induced high transcriptional activation in estrogen sensitive yeast with relative potencies almost 108 folds lower than 17β-estradiol. TCDD induced transcriptional activation weakly in estrogen- and progesterone- sensitive yeasts. This study elucidated that recombinant yeast is a sensitive and high-throughput system and can be used for the direct assessment on chemical interactions with steroid receptors and responsive elements. Also, the present study raises the requirement of evaluation on the endocrine disrupting effects of BHT, BHA, sorbic acid, CPM and TCDD for their transcription activity in yeast screening system though weak in intensity
Thyroid Hormones Receptor/Reporter Gene Transcription Assay for Food Additives and Contaminants
Jeong Sang-Hee,Cho Joon-Hyoung Korean Society of ToxicologyKorea Environmental Mu 2005 Toxicological Research Vol.21 No.4
Many of thyroid hormones disrupting chemicals induce effects via interaction with thyroid hormone and retinoic acid receptors and responsive elements intrinsic in target cells. We studied thyroid hormones disrupting effects of food additives and contaminants including BHA, BHT, ethoxyquin, propionic acid, sorbic acid, benzoic acid, CPM, aflatoxin B1, cadmium chloride, genistein, TCDD, PCBs and TDBE in recombinant HeLa cells containing plasmid construct for thyroxin responsive elements. The limit of response of the recombinant cells to T3 and T4 was $1\times10^{-12}\;M$. BHA. genistein, cadmium and TBDE were interacted with thyroid receptors with dose-responsive pattern. In addition, BHA, BHT, ethoxyquin, propionic acid, benzoic acid, sorbic acid, and TBDE showed synergism while cadmium chloride antagonism for T3-induced activity. This study elucidates that recombinant HeLa cell is sensitive and high-throughput system for the detection of chemicals that induce thyroid hormonal disruption via thyroid hormone receptors and responsive elements. Also this study raised suspect of BHA. BHT, ethoxyquin, propionic acid, benzoic acid, sorbic acid, TBDE, genisteine and cadmium chloride as thyroid hormonal system disruptors.
Steroid Hormone Receptor/Reporter Gene Transcription Assay for Food Additives and Contaminants
Jeong Sang-Hee,Cho Joon-Hyoung,Park Jong-Myung Korean Society of ToxicologyKorea Environmental Mu 2006 Toxicological Research Vol.22 No.1
Many of endocrine disrupting chemicals induce effects via interaction with hormone receptors and responsive elements in target cells. We investigated endocrine disrupting effects of some food additives and contaminants including BHA, BHT, ethoxyquin, propionic acid, sorbic acid, benzoic acid, CPM, aflatoxin B1, cadmium chloride, genistein, TCDD and PCBs in yeast transformants expressing human steroid hormone receptors along with steroid responsive elements. The response limit of genetically recombinant yeast to $17{\beta}$-estradiol, testosterone and progesterone was $1{\times}10^{-16},\;1{\times}10^{-12}\;and\;1{\times}10^{-13}M$, respectively. BHT induced weak transcriptional activity in estrogen sensitive yeast, while BHA and sorbic acid interacted weakly with androgen receptor/responsive element. CPM induced transcriptional activities in all types of yeasts sensitive to steroid hormones. Zearalenone and genistein induced high transcriptional activation in estrogen sensitive yeast with relative potencies almost $10^8$ folds lower than $17{\beta}$-estradiol. TCDD induced transcriptional activation weakly in estrogen- and progesterone- sensitive yeasts. This study elucidated that recombinant yeast is a sensitive and high-throughput system and can be used for the direct assessment on chemical interactions with steroid receptors and responsive elements. Also, the present study raises the requirement of evaluation on the endocrine disrupting effects of BHT, BHA, sorbic acid, CPM and TCDD for their transcription activity in yeast screening system though weak in intensity.
Steroid Hormone Receptor/Reporter Gene Transactivation Assay for Food Additives and Contaminants
Sang-Hee Jeong,Joon-Hyoung Cho,Jong-Myung Park 한국독성학회 2006 Toxicological Research Vol.22 No.1
Many of endocrine disrupting chemicals induce effects via interaction with hormone receptors and responsive elements in target cells. We investigated endocrine disrupting effects of some food additives and contaminants including BHA, BHT, ethoxyquin, propionic acid, sorbic acid, benzoic acid, CPM, aflatoxin B1, cadmium chloride, genistein, TCDD and PCBs in yeast transformants expressing human steroid hormone receptors along with steroid responsive elements. The response limit of genetically recombinant yeast to 17b-estradiol, testosterone and progesterone was 1 ? 10-16, 1 ? 10-12 and 1 ? 10-13 M, respectively. BHT induced weak transcriptional activity in estrogen sensitive yeast, while BHA and sorbic acid interacted weakly with androgen receptor/responsive element. CPM induced transcriptional activities in all types of yeasts sensitive to steroid hormones. Zearalenone and genistein induced high transcriptional activation in estrogen sensitive yeast with relative potencies almost 108 folds lower than 17b-estradiol. TCDD induced transcriptional activation weakly in estrogen- and progesterone- sensitive yeasts. This study elucidated that recombinant yeast is a sensitive and high-throughput system and can be used for the direct assessment on chemical interactions with steroid receptors and responsive elements. Also, the present study raises the requirement of evaluation on the endocrine disrupting effects of BHT, BHA, sorbic acid, CPM and TCDD for their transcription activity in yeast screening system though weak in intensity.
SAFB1, an RBMX-binding protein, is a newly identified regulator of hepatic SREBP-1c gene
( Yasushi Omura ),( Yoshihiko Nishio ),( Tadashi Takemoto ),( Chikako Ikeuchi ),( Osamu Sekine ),( Katsutaro Morino ),( Yasuhiro Maeno ),( Toshiyuki Obata ),( Satoshi Ugi ),( Hiroshi Maegawa ),( Hiros 생화학분자생물학회 2009 BMB Reports Vol.42 No.4
Hye Lim Yeo,송윤선,류재하,김희두 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.9
We have designed the cyclopropane analog ofstilbene as subtype-selective ligands for estrogen receptorbased on the bioisosterism that cyclopropane could act asalkene bioisoster. Three cyclopropane analogs were preparedefficiently starting from 4-benzyloxybenzaldehyde,and evaluated for their binding to estrogen receptors ERaand ERb. These cyclopropane analogs were also found tobe full agonists in estrogen receptor-mediated gene transcriptionassay. Compared to the stilbene analogs such astamoxifen and raloxifene, the three cyclopropane analogsshowed lower binding affinity for estrogen receptor, buthigher subtype selectivity for ERa. The structure–activityrelationship revealed from this study might provide cluesfor improving subtype selectivity for ERa.