• Title/Summary/Keyword: Estrogenic Activity

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Estrogenic Activity Assessment of Alkylphenolic chemicals using in vitro assays : I. E-Screen Assay

  • Park, Hyo-Joung;Lee, Ho-Sa;Na, Jin-Gyun;Ryu, Jae-Chun
    • Proceedings of the Korea Society of Environmental Toocicology Conference
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    • 2001.05a
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    • pp.125-125
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    • 2001
  • It has been hypothesized that environmental estrogens may play roles in the increasing incidence of breast and testicular cancers and another problems of the reproductive systems. Alkylphenols which are widely used as plastic additives and surfactants have been shown to induce estrogenic responses. The E-screen assay was developed to assess the estrogenedity of environmental chemicals using the profiferation effect of estrogens on their target cells as an end point. (omitted)

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Estrouenic/antiestrogenic potencies in crude and fractionated extracts of diesel exhaust particulate matter(PM) on human breast cancer cell

  • Ryu, Byung-Taek;Kim, Yun-Hee;Han, Kyu-Tae;Oh, Seung-Min;Chung, Kyu-Hyuck
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.165.2-166
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    • 2003
  • Diesel exhaust is suspected to cause acute and chronic adverse effects on health. In recent. the effect of estrogenic endocrine disruptor in diesel particulate matter was little studied. Therefore, we examined the estrogenic activity of respirable diesel exhaust particulate matter derived from diesel engine motor. PM2.5 diesel exhaust of vehicle was collected using a high volume samples equipped with a cascade impactor. (omitted)

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STUDY OF RESVERATROL AND ITS DERIVATIVES ON THE REGULATION OG GENE EXPRESSION IN MCF-7 CELLS TRANSFECTED WITH EITHER pERE-LUC OR phCYP1A1-LUC

  • Joung, Ki-Eun;Kim, Yeo-Woon;Sheen, Yhun-Yhong
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2001.11a
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    • pp.111-111
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    • 2001
  • Resveratrol (trans-3,4',5-trihydroxystilbene), which is a polyphenolic compound found in a variety of plants such as grapes and wine, has been reported to have a variety of anti-inflammatory, anti-platelet, and anti-carcinogenic effects. Recently resveratrol of was reported to serve as an estrogen agonist in MCF-7 cells Based on its structural similarity to diethylstilbestrol, a synthetic estrogen, we examined whether resveratrol and its derivatives might be estrogenic using stable MCF-7-ERE cells. Resveratrol functioned as a superagonist at high concentrations (i.e., produced a greater maximal transcriptional response than estradiol) Among the resveratrol derivatives, 10 compounds showed significant estrogenic activity.

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Ginsenoside-Rb1 Acts as a Weak Estrogen Receptor Agonist Independent of Ligand Binding.

  • Park, Wan-Kyu;Jungyoon Cho;Lee, Young-Joo
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2003.11a
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    • pp.114-114
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    • 2003
  • Ginseng is a medicinal herb widely used in Asian countries, and its pharmacological effects has been demonstrated in various systems such as cardiovascular, central nervous, and endocrine systems. Its effects are mainly attributed to the ginsenosides. We hypothesize that a component of Panax ginseng, ginsenoside-Rbl, acts by binding to estrogen receptor. We have investigated the estrogenic activity of ginsenoside-Rbl in a transient transfection system using estrogen receptors ${\alpha}$ or ${\beta}$ with estrogen -responsive luciferase plasmids in COS monkey kidney cells. Ginsenoside-Rbl activated both estrogen receptors ${\alpha}$ and ${\beta}$ in a dose-dependent manner (0.5 -100 M ). Activation was inhibited by the specific estrogen receptor antagonist ICI 182,780, indicating that the estrogenic effect of ginsenoside-Rbl is estrogen receptor dependent. Next, we evaluated the ability of ginsenoside-Rbl to induce estrogen-responsive progesterone receptor gene by semi-quantitative RT-PCR assays. MCF-7 cells treated with l7${\beta}$-estradiol or ginsenoside- Rb1 exhibited an increased expression of progesterone receptor mRNA. However, ginsenoside-Rbl failed to displace the specific binding of [3H]17${\beta}$-estradiol to estrogen receptor in MCF-7 cells as examined by whole cell ligand binding assays, suggesting that there is no direct interaction of ginsenoside-Rbl with estrogen receptor. Our results indicate that estrogen-like activity of ginsenoside-Rbl is independent of direct estrogen receptor association.

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REQUIREMENT OF METABOLIC ACTIVATION OF PUERARIA MIRIFICA FOR ESTROGENIC ACTIVITY

  • Yang, Se-Ran;Cho, Sung-Dae;Park, Ki-Soo;Hong, In-Sun;Jo, Eun-Hye;Seo, Min-Soo;Lee, Yong-Soon;Kang, Kyung-Sun
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2002.05a
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    • pp.105-105
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    • 2002
  • A wide range of chemicals derived from plant and human-made xenobiotics are reported to have hormonal activity. The present studies were performed to examine the estrogenic effect of Kwao Keur, Pueraria mirifica (PM), that has been used a rejuvenating folk medicine from Thailand, using recombinant yeast, MCF-7 cell proliferation and HepG2 cell transient transfection assay.(omitted)

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Modification of Estrogenic Effect of Nonylphenol Combined with DEHP in Yeast-based Bioassay (형질전환효모를 이용한 내분비계장애물질검색과 Nonylphenol의 Estrogen 유사작용에 대한 DEHP의 상협작용)

  • 박미선;정해관;박현신;한의식;김종원;엄미옥;정상희;오혜영
    • Toxicological Research
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    • v.17 no.1
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    • pp.65-71
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    • 2001
  • The key targets of endocrine disruptors are nuclear hormone receptors, which bind to steroid hormones and regulate their gene transcription. A yeast-based steroid hormone receptor gene trascription assay was previously developed for the evaluation of chemicals with endocrine modulating activity. The yeast transformants used in this assay contain the human estrogen receptor along with the appropriate steroid response elements upstream of the $\beta$-galactosidase reporter gene. We tried to evaluate several natural and synthetic steroids of their potential to interact directly with the steroid receptor. Some putative endocrine disruptors, including nonylphenol, are weakly estrogenic. But the combined treatment oj these chemicals with di-(2-ethylhexyl)phthalate (DEHP) significantly increased the $\beta$-galactosidase activity in the yeast transformant. These results suggest that we also have to consider the synergistic effects of endocrine disruptors. In this study, we showed that yeast-based bioassay is a valuable tool for screening potential endocrine disruptors and quantitative determination of estrogenicity. And the possibility that the estrogen receptor binds multiple environmental chemicals adds another level of complexity to the interaction between the endocrine disruptors and the human hormone system.

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Peripubertal Administration of Icariin and Icaritin Advances Pubertal Development in Female Rats

  • Kang, Hyun-Ku;Lee, Sang-Bum;Kwon, Hyo-Suk;Sung, Chung-Ki;Park, Young-In;Dong, Mi-Sook
    • Biomolecules & Therapeutics
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    • v.20 no.2
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    • pp.189-195
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    • 2012
  • Epimedii Herba is a traditional medicinal herb used in Korea and China and exerts estrogenic activity. In this study, we investigated the effect of peripubertal administration of Epimedii Herba on pubertal development in female rats using a modified protocol of the rodent 20-day pubertal female assay. Female Sprague-Dawley rats (21 days old after weaning, 10 rats per group) were divided into five groups: saline (Con), ethinyl estradiol (E2), Epimedii Herba ext (Ext), icariin (ICI), and icaritin (ICT), which were administered by oral gavage (E2 by subcutaneous injection) from postnatal day (PND) 21 through PND40. The time to vaginal opening (VO) was shorter for the Epimedii groups, particularly for the ICT group (p<0.05). Treatment with ICI and ICT significantly increased the duration of the estrus cycle (ICI, 2.78 days; ICT, 4.0 days; control, 1.78 days). Ovary weight was reduced by E2 treatment and increased by the Ext, ICI, and ICT treatments while the weight of the uterus and pituitary glands increased significantly only in the E2 and ICT groups. Although Epimedii Herba displayed relatively weak estrogenic activity, its repeated administration could affect pubertal development in female rats.

Improvement of the Biosensor for Detection of Endocrine Disruptors by Combination of Human Estrogen Receptorα and Co-Activator (Human Estrogen Receptor α와 Co-activator로 구성된 바이오센서를 이용한 내분비계장애물질의 검출)

  • Lee, Haeng-Seog
    • Journal of Korean Society of Water and Wastewater
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    • v.20 no.6
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    • pp.893-904
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    • 2006
  • To improve sensitivity of biosensor as yeast two-hybrid detection system for estrogenic activity of suspected chemicals, we tested effects of several combinations of the bait and fish components in the two-hybrid system on Saccharomyces cerevisiae inducted a chromosome-integrated lacZ reporter gene that was under the control of CYC1 promoter and the upstream Gal4p-binding element $UAS_{GAL}$. The bait components that were fused with the Gal4p DNA binding domain are full-length human estrogen receptor ${\alpha}$ and its ligand-binding domain. The fish components that were fused with the Gal4p transcriptional activation domain were nuclear receptor-binding domains of co-activators SRC1 and TIF2. We found that the combination of the full-length human estrogen receptor ${\alpha}$ with the nuclear receptor-binding domain of co-activator SRC1 was most effective for the estrogen-dependent induction of reporter activity among the two-hybrid systems so far reported. The relative strength of transcriptional activation by representative natural and xenobiotic chemicals was well correlated with their estrogenic potency that had been reported with other assay systems.