• 대한화장품학회지
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• 제40권3호
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• pp.279-287
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• 2014

폐경 이후 여성에서 발생되는 에스트로겐의 감소는 피부노화와 밀접한 관련이 있으며, 피부의 정상적 상태와 기능을 저하시키게 된다. 지난 10여 년간 보고된 많은 연구결과를 살펴보면, 에스트로겐은 폐경 이후 여성의 피부에서 콜라겐 감소를 막아주고, 탄력을 회복시키며, 건조한 피부를 개선시키는 등의 피부 안티에이징 효능을 가지는 것을 알 수 있다. 에스트로겐과 유사한 구조로 인해 파이토에스트로겐이라 알려진 이소플라본은 자외선에 의해 유도된 피부 손상을 보호하는 기작이 널리 알려져 왔으나 피부세포에서 에스트로겐과 유사한 안티에이징 효능을 가지는지에 대해서는 많은 연구가 진행되지 않았다. 이에 본 연구에서는 콩류 등에 많이 함유된 이소플라본인 다이드제인이 에스트로겐과 유사한 활성 및 효능을 가지는지 밝히고자 하였다. 먼저 에스트로겐 수용체와의 결합을 통한 transcriptional activity에 미치는 효과를 luciferase assay를 통해 살펴본 결과, 다이드제인은 대조군에 비해 농도 의존적으로 estrogen receptor-dependent transcriptional activity를 유의하게 증가시켰다. 다음으로 사람의 피부 섬유아세포를 이용하여 다이드제인이 세포외 기질단백질 성분들의 발현에 미치는 효과를 조사한 결과, 다이드제인은 콜라겐 타입 I, 콜라겐 타입 IV, 엘라스틴 및 피브릴린-1의 발현을 유의하게 증가시키는 것을 확인할 수 있었다. 모든 실험조건에서 에스트로겐 단독 효능과의 비교 분석을 통해 다이드제인은 에스트로겐과 유사한 효능을 가진다는 것을 확인할 수 있었다. 본 연구 결과를 통해 다이드제인은 기존에 알려진 이소플라본의 광보호 효능과 더불어 파이토에스트로겐 효능을 가짐으로써 갱년기 여성의 피부 안티에이징을 위해 활용할 수 있을 것이라 제안한다.

• 한국식품위생안전성학회지
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• 제22권3호
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• pp.218-222
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• 2007

에스트로젠 수용체와 리포터 유전자인 ${\beta}-galactosidase$가 도입된 효모재조합검색시험법을 이용하여 DEHP와 DBP의 내분비계 장애작용을 검색하였다. 양성대조 시험물질로 $17{\beta}-estradiol$을 설정하여 DEHP와 DBP의 에스트로젠 활성을 비교분석 하였을 때, $17{\beta}-estradiol$의 경우 $10^{-9}M$에서 가장 활성이 높게 관찰되었다. DEHP의 경우 $10^{-10}M$에서 $10^{-7}M$까지 시험하였을 때 농도의존적으로 에스트로젠활성이 증가하였으며, $10^{-7}M$의 경우 가장 강력한 에스트로젠활성을 보였다. DBP의 경우 $10^{-9}M$에서 $10^{-6}M$까지 에스트로젠활성이 관찰되었다. DEHP와 DBP의 경우 최대활성화 대비 50% 이상의 활성도를 보이기 시작하는 농도가 $10^{-9}M$로 나타나서 비슷한 농도에서 에스트로젠 활성화가 이루어지는 것으로 추측할 수 있었다. 그러나, 에스트로젠 최대활성화 시의 농도를 비교해 보면 DBP가 DEHP보다 10배 낮은 농도에서 최대활성치가 관찰되었기 때문에 DBP가 DEHP보다 에스트로젠 작용에 더 민감하게 반응하는 것으로 판단할 수 있었다. 결과적으로 본 실험에 사용되어진 시험물질인 DEHP와 DBP는 효모재조합시험법에 있어서 에스트로젠 활성을 유도하는 것으로 판단되어지며 감수성에 있어서는 DBP가 DEHP보다 높은 것으로 여겨진다.

• Biomolecules & Therapeutics
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• 제17권4호
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• pp.430-437
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• 2009

Metabolites of Soyasaponin I, a major constituent of soybean, by human intestinal microflora were investigated by LC-MS/MS analysis. We found four peaks, one parental constituent and three metabolites: m/z 941 [M-H]$^-$, m/z 795 [M-rha-H]$^-$, m/z 441 [aglycone-$H_2O$+H]$^+$, and m/z 633 [M-rha-gal-H]$^-$, which was an unknown metabolite, soyasapogenol B 3-$\beta$-D-glucuronide. When soyasaponin I was incubated with the human fecal microbial fraction from ten individuals for 48 h, soyasaponin I was metabolized to soyasapogenol B via soyasaponin III and soyasapogenol B 3-$\beta$-D-glucuronide or via soyasaponin III alone. Both soyasaponin I and its metabolite soyasapgenol B exhibited estrogenic activity. Soyasaponin I increased the proliferation, mRNA expression of c-fos and pS2, in MCF7 cells more potently than soyasapogenol B. However, soyasapogenol B showed potent cytotoxicity against A549, MCF7, HeLa and HepG2 cells, while soyasaponin I did not. The cytotoxicity of soyasapogenol B may prevent its estrogenic effect from increasing dose-dependently. These findings suggest that orally administered soyasaponin I may be metabolized to soyasapogenol B by intestinal microflora and that soyasapogenol B may express a cytotoxic effect rather than an estrogenic effect.

• Journal of Ginseng Research
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• 제43권4호
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• pp.527-538
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• 2019

Background: Ginsenoside Rg1 was shown to exert ligand-independent activation of estrogen receptor (ER) via mitogen-activated protein kinase-mediated pathway. Our study aimed to delineate the mechanisms by which Rg1 activates the rapid ER signaling pathways. Methods: ER-positive human breast cancer MCF-7 cells and ER-negative human embryonic kidney HEK293 cells were treated with Rg1 ($10^{-12}M$, $10^{-8}M$), $17{\beta}$-estradiol ($10^{-8}M$), or vehicle. Immunoprecipitation was conducted to investigate the interactions between signaling protein and ER in MCF-7 cells. To determine the roles of these signaling proteins in the actions of Rg1, small interfering RNA or their inhibitors were applied. Results: Rg1 rapidly induced $ER{\alpha}$ translocation to plasma membrane via caveolin-1 and the formation of signaling complex involving linker protein (Shc), insulin-like growth factor-I receptor, modulator of nongenomic activity of ER (MNAR), $ER{\alpha}$, and cellular nonreceptor tyrosine kinase (c-Src) in MCF-7 cells. The induction of extracellular signal-regulated protein kinase and mitogen-activated protein kinase kinase (MEK) phosphorylation in MCF-7 cells by Rg1 was suppressed by cotreatment with small interfering RNA against these signaling proteins. The stimulatory effects of Rg1 on MEK phosphorylation in these cells were suppressed by both PP2 (Src kinase inhibitor) and AG1478 [epidermal growth factor receptor (EGFR) inhibitor]. In addition, Rg1-induced estrogenic activities, EGFR and MEK phosphorylation in MCF-7 cells were abolished by cotreatment with G15 (G protein-coupled estrogen receptor-1 antagonist). The increase in intracellular cyclic AMP accumulation, but not Ca mobilization, in MCF-7 cells by Rg1 could be abolished by G15. Conclusion: Ginsenoside Rg1 exerted estrogenic actions by rapidly inducing the formation of ER containing signalosome in MCF-7 cells. Additionally, Rg1 could activate EGFR and c-Src ER-independently and exert estrogenic effects via rapid activation of membrane-associated ER and G protein-coupled estrogen receptor.

• Reproductive and Developmental Biology
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• 제35권1호
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• pp.47-54
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• 2011

Endocrine disruptors bind to hormone receptors on sperm membrane, therefore spermatozoa are potentially a useful model for examining estrogenic activities of endocrine disruptors. The objective of this study was to compare the effects of two xenoestrogenic compounds [genistein (Gen) and 4-tert-octylphenol (OP)] to those of two steroids [estrogen ($E_2$) and progesterone ($P_4$)] on boar sperm % motility and motion kinematics of in vitro. Porcine spermatozoa were incubated with various concentrations ($0.001{\sim}100\;{\mu}M$) of each chemical for 15 or 30 min, and then assessed % motility and sperm motion kinematics using computer assisted sperm analyzer (CASA). Each chemical decreased sperm % motility, and OP decreased VSL and VAP compared with untreated control(p<0.05). $E_2$ stimulated the motion kinematic changes except VCL. Moreover, Gen had effects on VCL and VAP alterations after 30 min incubation. In summary, since all chemicals studied effectively altered sperm % motility and motion kinematics, it was concluded that porcine spermatozoa could be a useful model for in vitro screening of potential endocrine disruptors.

• 한국환경독성학회:학술대회논문집
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• 한국환경독성학회 2003년도 춘계학술대회
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• pp.192-192
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• 2003

Pomegranate, a small tree originating in Orient, belongs to Punicaceae family. The seeds contain an oil of which about 80% is rare trans 18 carbon fatty acid (punicic acid), and have highest botanical concentration of a sex steroid, estrone. Pharmacological properties of pomegranate extract have been studied, with anti-microbial, anti-parasitic, ant-viral, and anti-cancer effects. We have examined the estrogenic activity of the pomegranate extracts using MCP-7-ERE cells. MCF-7-ERE cells, stably transfected with pERE-Luc were treated various amount of pomegranate extract and after overnight treatments, luciferase activity were measured. Estradiol(E2) dose dependently induced luciferase activity in this cell and maximal response is obtained at 100pM E2.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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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)

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 2001년도 추계학술대회 및 정기총회
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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.

• Toxicological Research
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• 제17권3호
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• pp.181-186
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• 2001

The estrogenic potency of bisphenol A using reverse trancriptase-PCR response of liver vitellogenin mRNA in male carp was studied. For this, six combination of primers which were synthesized on the basis of cDNA consensus region of various species, were evaluated and one pair of primers was selected as the best to show 286 bp size-transcript. By using the selected primers, vitellogenin mRNA induction in carp treated with bisphenol A was measured and the chemical showed dose-and time-dependent Induction response. From this result, it was concluded that RT-PCR technique wing the selected primers in this study can be wed to monitor the estrogenic effects exerted In carp living in Korean freshwater.

• Advances in Traditional Medicine
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• 제4권2호
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• pp.70-76
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• 2004

Petroleum ether, benzene and alcohol extracts of the seeds of C. juncea were tested for antiimplantation and pregnancy interruption activities in female albino rats. Of these three extracts, the alcohol extract was found to be the most effective in causing antiimplantation and pregnancy interruption activities. These adverse effects on fertility are reversible upon withdrawal of the extract treatments. The alcohol extract was found to possess estrogenic activity. After subjecting to preliminary phytochemical screening, the alcohol extract showed positive tests for alkaloids, steroids, glycosides, saponins, flavonoides, fixed oils, phenols and tannins.