• 대한본초학회지
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• 제35권3호
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• pp.1-8
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• 2020

Objectives : In this study, we examined the estrogenic activities and anti-osteo clastogenesis effects of PCE17, a mixture of PE (an extract of Puerariae Flos), and CE (an extract of Citri Unshius Pericarpium). Methods : The estrogenic effect of PCE17, PE and CE were examined by ER-β/ERE reporter gene assay and proliferation assay in 293 T and MCF-7 cells. The expression of estrogen-responsive gene and protein were checked by Real Time-PCR (RT-PCR) and Western blotting in MCF-7 cells. Inhibitory effect of PCE17, PE and CE on RANKL-induced osteoclast differentiation were evaluated by TRAP staining and RT-PCR in primary osteoclast precursors from rat bone marrow cells. Results : PCE17 and PE bind to ERs (estrogen receptors) and show estrogenic activities in 293T cells. They also stimulated the proliferation of MCF-7 cells and increased the expression of ER response gene, pS2. Tectorigenin, an active ingredient of PE, shows similar estrogenic activities in MCF-7 cells. PCE17 and CE inhibited RANKL-induced osteoclastogenesis in rat primary osteoclast precursor cells and down-regulated the osteoclast-specific genes of Nfatc1, Ctsk, and Acp5. Conclusions : In conclusion, PCE17 may have therapeutic potential in cases of menopause and osteoporosis.

• 대한본초학회지
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• 제37권5호
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• pp.1-8
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• 2022

Objectives : This study aimed to investigate the synergistic effect of combining Cynanchi Wilfordii Radix extract with Humuli Lupuli Flos extract on estrogenic and anti-osteoclastogenic activity. Methods : Estrogenic effect of a mixture of Cynanchi Wilfordii Radix extract and Humuli Lupuli Flos extract (CWHL), Cynanchi Wilfordii Radix extract, Humuli Lupuli Flos extract, caudatin (an active ingredient of Cynanchi wilfordii Radix extract) and 8-prenylnaringenin (an active ingredient of Humuli Lupuli Flos extract) were examined by proliferation E-screen assay and expression of estrogen inducible gene, pS2 via Real Time-PCR (RT-PCR) in MCF-7 estrogen responsive cells. And their estrogenic activities were investigated how to modulate Estrogen receptor 𝛽 by binding affinity assay. Inhibitory effect of CWHL, Cynanchi Wilfordii Radix extract, Humuli Lupuli Flos extract, caudatin and 8-prenylnaringenin on RANKL-induced osteoclast differentiation were tested by TRAP (Tartrate-resistant acid phosphatase) staining in osteoclastogenic RAW 264.7 cells. Results : CWHL, Humuli Lupuli Flos extract and 8-prenylnaringenin accelerated the proliferation of MCF-7 and the expression of pS2 in MCF-7. CWHL, Cynanchi Wilfordii Radix extract, Humuli Lupuli Flos extract, caudatin and 8-prenylnaringenin bind to estrogen receptor 𝛽. CWHL, Cynanchi Wilfordii Radix extract, Humuli Lupuli Flos extract, caudatin and 8-prenylnaringenin inhibited RANKL-induced osteoclastogenesis in osteoclastogenic RAW 264.7. CWHL is more effective for all markers than Cynanchi Wilfordii Radix extract or Humuli Lupuli Flos extract alone. Conclusions : CWHL may a potential therapeutic agent for menopause and osteoporosis as a natural food resource. CWHL as a natural food source has therapeutic potential in cases of menopause and osteoporosis.

• Molecular & Cellular Toxicology
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• 제2권2호
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• pp.106-113
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• 2006

Phthalate analogues are a plasticizer and solvent used in industry. Phthalates were classified in the category of "suspected" endocrine disruptors. The purpose of our study was to screen and elucidate the endocrine disrupting activity of seven phthalate analogues. E-screen assay was performed in MCF-7 human breast cancer cells with seven phthalate analogues. In this cell proliferation assay, benzyl butyl phthalate (BBP) and dibutyl phthalate (DBP) showed high estrogenic activity. Their relative proliferation efficiencies (RPE) were 109 and 106%, respectively. In vitro estrogen receptor (ER) binding assay, BBP, di-n-octyl phthalate (DOP) and dinonyl phthalate (DNP) showed weak relative binding affinity (RBA: 0.02%) compared to $17{\beta}-estradiol\;(E2)$ (RBA: 100%). In uterotrophic assay, E2 produced a significant increase, whereas four tested phthalate analogues had potential estrogenic effects in vitro did not increased in uterus weight in immature rats. From these results, we demonstrated that phthalate analogues exhibit weak estrogenic activity in vitro assays at high concentrations. Although phthalates induced an increase in MCF-7 cell proliferation by an estrogenic effect, they could not induce a uterus weight increase in vivo. From these, we may suggest that these phthalate analogues are easily metabolized to inactive forms in vivo. Further investigation in other in vitro and in vivo experimental systems might be required.

• Toxicological Research
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• 제18권4호
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• pp.393-396
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• 2002

This study was carried out to evaluate the ostrogenic/antiandrogenic activity of Puerariae Radix in Sprague-Dawley rats. It has known that diverse phytoestrogen were included in some Puerariae Radix, especially in Pueraria mirifica. The Uterotrophic assay and Hershberger assay were performed to evaluate the ostogenic/antiandrogenic activity of various Puerariae Radix (Pueraria thunbergiana, Pueraria mirifica and Butea superba). In Uterotrophic assay, the extracts of Puerariae Radix were administered subcutaneously to immature female SD rats from 19 to 21 days of age. The wet uterus and vaginal weighs significantly increased in the group only treated with extracts of Pueraria mirifica. But, in Hersh-berger assay, all extracts of Puerariae Radix did not show any effects in the castrated rats. These results suggest that Pueraria mirifica has not undrogenic/antiandrogenic effect but potent estrogenic effect. It is possible that components of Pueraria mirifica may act as endocrine disruptor in human body.

• 한국해양환경ㆍ에너지학회지
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• 제10권2호
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• pp.86-92
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• 2007

본 연구는 E-screen assay를 이용해서 광양만 연안해역 퇴적물의 에스트로겐 활성분포를 정량적으로 평가하고 화학분석 결과와 비교 검토하고자 하였다. 가장 높은 에스트로겐 활성을 보인 지점은 산업단지와 섬진강 유입구에 인접한 G6, G8 이었다. E-screen assay로 얻어진 이러한 결과는 다성분 동시분석 결과와도 일치하였다. 특히 GY6, GY8 지점의 RPE는 90% 이상으로 강한 에스트로겐 작용을 나타내어 full agonist 지점으로 확인되었다. 또한 이들 지점은 EEQ가 각각 35.6 ng/g, 14.6 ng/g로 타 지점에 비해 낮아 에스트로겐 활성 효능이 상대적으로 높을 것으로 판단된다. 이러한 결과로부터, 산업단지와 섬진강 유역에 인접한 지점들을 광양만 연안 해역의 내분비계 교란 물질의 유입원으로 추정할 수 있다. 한편, 에스트로겐 활성도와 화학오염물질과의 비교결과는 상관성이 없는 것으로 나타났다.

• 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 Life Science
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• 제9권2호
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• pp.19-23
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• 1999

Bisphenol-A and related conpounds recently have been reported to be estrogenic since it has been demonstrared in laboratory stuides that they mimic the effects of estrogen. Bisphenol-A refered to as "environmental estrogen" are suspected of causing health effect in living body through disruption of endocdrine system. In this review, the occurrence, environmental fate, and biological effects of bisphenol-A are presented. To provide understanding to the potential for endocrine disruption due to environmental estrogen, the physiology of bisphenol-A mammalian and fish is also reviewed. For empty can, the migrationof bisphenol-A form food conducted epoxy coating was effected by the test conditions and it increased in order to water and 4% acetic acid. Extracts from foods packed in lacquer coated can also showed estrogenic activity. Bisphenol-A was found as a contaminant not only in the liquid food cans, but also in water autoclave in can. The used of coating certain food-packaging material may require closer scrutiny to determine when bisphenol-A contribute to advert exposure of consumers to estrogenic xenobiotics. Human breast cancer MCF cell added bisphenol-A cultivated to study the ability of bisphenol-A to elicit of bisphenol-A estrogenic bioresponse in this system. Bisphenol-A, similar to estradiol, induced PR activation in transiently transfected anterior and posterior pituitary cells.

• 한국환경독성학회:학술대회논문집
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• 한국환경독성학회 2002년도 추계국제학술대회
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• pp.166-166
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• 2002

The response of environmental pollutants can be detected bioanalytically focusing on the source and matrices of concern. Cell culture bioassays are rapid and inexpensive, and thus have great potential for determination of environmental pollution. We have examined the estrogenic and dioxin-like activites of industrial wastewater using E-screen assay and EROD microbioassay. Influent and effluent wastewater were collected from four different industrial wastewater treatment plants, such as cosmetics, paints, textile producing and metal coating plant, and extracted using solid-phase extraction with Oasis＠HLB plus cartridge. Pollutants adsorbed to the cartridge were eluted with MTBE. MCF-7 cells were treated with extracts showed various estrogenic potential. The textile wastewater showed strong estrogenic activity and the others showed weak estrogenic activity, No effect was observed in the wastewater from paints producing plant. All extracts showed CYPIA inducing effects, indicating these samples contain dioxin-like chemicals. Bioanalytical results of effluents compared with influents could give us information about the incomplete wastewater treatment and biological potency caused by pollutants. [Supported by a Grant from the Korea Science and Engineering Foundation]

• 생약학회지
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• 제15권2호
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• pp.85-90
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• 1984

The whole plant of Duchesnea indica (Andr.) Focke (Rosaceae) which has been used in folklore in treating amenorrhea, inflammation, fever and traumatic injuries, in detoxifying and breaking up clots, was studied. The pharmacological test showed that the water extract had estrogenic and histaminergic actions, but no antiserotonin action. As a result of systematic separation in order to detect the active compounds revealing the estrogenic effect, the active compounds were found in the ether fraction. TLC of the ether fraction revealed 8 spots. Among them three major spots (Rf=0.54, 037, 0.31) were separated by preparative TLC. Some chemical properties of those major spots suggested that they were phenolic compounds, but that they were neither linoleic acid nor ${\beta}-sitosterol$ previously reported.

• Environmental Analysis Health and Toxicology
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• 제19권4호
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• pp.375-382
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• 2004

This study was designed to investigate potential endocrine disrupting effects of several industrial wastewater effluents discharged from cosmetic, plaiting, paint, textile industry using EROD bioassay and E-Screen assay. The results of E-screen assay showed that textile industrial wastewater could act as a full agonist and cosmetics and plaiting industrial wastewater could act as a partial agonist. On the contrary, the wastewater discharged from paint industry did not show any estrogenic effect. Estrogenic activity in the effluents of cosmetic and paint industrial wastewater was lower than that in the influents indicating that the wastewater treatment process minimized the effects of discharges on water quality. Despite of these results, it was recognized that wastewater treatment was not always minimize toxic impact. In this study, increased estrogenic effect was observed in the effluents of plating and textile wastewater, and EROD activity was increased in the effluents of cosmetic and plating wastewater.