• Journal of Life Science
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• v.13 no.6
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• pp.799-804
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• 2003

In order to verify the occurrence of an estrogenic compound in natural products, the estrogenic activity was measured using an in vitro detection system. For this system, human breast cancer cell line MCF7 was transfected using an estrogen responsive CAT reporter plasmid. Estrogenic activities of photosynthetic algae spirulina and sea lettuce were evaluated using this system. Estrogenic activities of a $500\mug/ml\; and\; 50 \mug/ml$ ethanol extracts of spirulina were as much as that of $10^{-8}$M standard solution (17$\beta$-estradiol) and activity of $5\mug/ml$ ethanol extract of spirulina was as much as that of $10^{-10}$ M standard solution. However, no significant estrogenic activity was observed using sea lettuce extract. Estrogenic activities of marine animals, such as star fish and shrimp, were also evaluated using this system, however, no significant estrogenic activity was observed in these extracts. In this result, it is confirmed that spirulina extract possesses estrogenic compound.

• Archives of Pharmacal Research
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• v.28 no.2
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• pp.186-189
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• 2005

Anti-estrogenic activity of (-)-sesamin (1), helioxanthin (2), savinin (3), taiwanin C (4), and 3­(3,4-dimethoxybenzyl)-2-(3,4-methylenedioxybenzyl)butyrolactone (5) isolated from the root of Acanthopanax chiisanensis was tested using Ishikawa cells. Among them, compound 3 exhibited anti-estrogenic activity ($IC_{50}\;=\;4.86\;{\mu}M$).

• Korean Journal of Pharmacognosy
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• v.52 no.2
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• pp.118-125
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• 2021

Leguminosae plants are known for its phytoestrogen constituents which play a major role in the prevention of osteoporosis, cancer and heart disease. In this study, the estrogenic activity of 158 samples from 58 species, 3 subspecies and 10 varieties of Leguminosae plants growing in Korea was evaluated. An estrogen, 17β-estradiol was used as a reference compound, and the potency of each sample was expressed in relative efficacy (%) compared to that of the reference by a reporter gene assay using MCF-7 cells. As results, the estrogenic activity of methanolic extracts of Phaseolus vulgaris var. humilis, Sophora flavescens, Lespedeza × robusta, Indigofera pseudotinctoria, Maackia amurensis, Glycine soja, Wisteria floribunda, Robinia pseudoacacia, Astragalus sinicus, Pueraria lobata, Lespedeza maximowiczii var. tomentella, Trifolium repens and Crotalaria sessiliflora showed similar to or higher at 100 ㎍/ml than the positive control at 10 nM. These findings can be a potential evidence for developing estrogen alternatives resolving various types of menopause symptoms with information on proper harvest season and usage plant part. To the best of our knowledge, the estrogenic activity of Lespedeza × robusta, Indigofera pseudotinctoria, Wisteria floribunda, Robinia pseudoacacia and Lespedeza maximowiczii var. tomentella is reported for the first time in this study.

• 한국생물공학회:학술대회논문집
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• 2005.04a
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• pp.368-372
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• 2005

Phytoestrogens are non-steroidal compounds found in a variety of plants, which exert estrogenic effects in animals. In this study, the useful compounds of pomegranate as preliminarily research for the developing of natural estrogen supplement were determined. The estrogenic activity of phytoestrogens in the pomegranate was estimated by using the Yeast Estrogen Receptor and E-screen assay. Estrogenic activity of all pomegranate extracts in the Yest Estrogen Receptor assay were not significant difference at all concentration. Whereas peel extracts of Iranian and domestic red pomegranate are significantly enhanced in the E-screen assay. When various pomegranate extracts enzyme and acid hydrolyzed, three aglycones of phytoestrogen, kaempferol, quercetin and catechin were detected. Peel extract of domestic red pomegranste contained more than kaempferol(87.0 mg%), quercetin(172.8 mg%)) and catechin(956.8 mg%) than other extracts. These differences in concentrations of key phytoestrogens among various extracts seemed to be responsible for their differences in estrogenic activities. Among these three compound, kaempferol showed the highest MCF-7 cell enhancing efface.

• Korean Journal of Veterinary Research
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• v.46 no.1
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• pp.35-41
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• 2006

Vitellogenin (Vtg), a phospholipoglycoprotein precursor of egg yolk is synthesized and secreted from the liver in response to estrogens in female fish. Vtg is normally undetectable in the blood of male fish, but can be induced by exposure to chemicals possessing estrogenic activity. Thus, the presence of Vtg in blood of male fish can serve as a useful biomarker for assessing previous exposure to estrogenic compounds. In the present study, Vtg was abnormally expressed in Rhynchocypris oxycephalus using estradiol benzoate ($E_2$). As the result, it was found that the level of Vtg in blood from R. oxycephalus was increased by treated quantity of $E_2$ with dose-effect manner. Monoclonal antibodies were generated against Vtg of R. oxycephalus. The hybridoma were screened with an enzyme immunoassay for the production of specific anti-Vtg antibodies. Five positive cell lines with a high specificity were selected. Monoclonal antibodies against vtg of R. oxycephalus that was developed in this study, may be a useful bio-indicator for the detection of estrogenic contamination in the aquatic ecosystem.

• 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.

• Clinical and Experimental Pediatrics
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• v.55 no.8
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• pp.265-271
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• 2012

Phytoestrogen is an estrogenic compound that occurs naturally in plants. The most common sources of phytoestrogen are soybean products, which contain high levels of isoflavones. This compound, which has structural similarity with estrogen, can act as an estrogen receptor agonist or antagonist. Animal studies provide evidence of the significant effects of phytoestrogen on sexual development, including altered pubertal timing, impaired estrous cycling and ovarian function, and altered hypothalamus and pituitary functions. Although human studies examining the effects of phytoestrogen on sexual development are extremely limited, the results of some studies agree with those of the animal studies. In this paper, we review the possible mechanism of phytoestrogen action and the evidence showing the effects of phytoestrogen on sexual development in animal and human studies.

• Development and Reproduction
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• v.20 no.4
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• pp.349-357
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• 2016

The present research was chiefly designed to determine the effect of the treatment of estrogenic agonist, estradiol benzoate (EB), or antiandrogenic compound, flutamide (Flu), at the weaning age on the expression of connexin (Cx) isoforms in the caudal epididymis of adult male rat. Animals were subcutaneously administrated with a single shot of either EB at a low-dose ($0.015{\mu}g$ of EB/kg body weight (BW)) or a high-dose ($1.5{\mu}g$ of EB/kg BW) or Flu at a low-dose ($500{\mu}g$ of EB/kg BW) or a high-dose (5 mg of EB/kg BW). Expressional changes of Cx isoforms in the adult caudal epididymis were examined by quantitative real-time PCR analysis. The treatment of a low-dose EB caused significant increases of Cx30.3, Cx31, Cx32, and Cx43 transcript levels but reduction of Cx31.1, Cx37, and Cx45 expression. Exposure to a high-dose EB resulted in very close responses observed in a low-dose EB treatment, except no significant expressional change of Cx37 and a significant induction of Cx40. Expression of all Cx isoforms, except Cx45, was significantly increased by a low-dose Flu treatment. Expressional increases of all Cx isoforms were detected by a high-dose Flu treatment. The current study demonstrates that a single exposure to estrogenic or antiandrogenic compound during the early postnatal developmental period is sufficient to disrupt normal expression of Cx isoforms in the adult caudal epididymis.

• Toxicological Research
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• v.16 no.3
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• pp.201-209
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• 2000

In association with the international validation program to establish a rodent uterotrophic assay, we conducted preliminary uterotrophic assay proposed by GECD using immature female rats. In the present study, oral and subcutaneous routes were chosen to compare the effects of estrogenic com-pounds in the two dosing regimens. The reference compound ethinyl estradiol (EE) and the antagonist ZM189154(ZM) were administered by gavage or subcutaneously (s.c.) to immature female SD rats from 20 to 22 days of age. For each study, sixty-six female rats were randomly assigned to eleven groups: Untreated control, EE 0,0.01, 0.03, 0.1, 0.3, 1.0,3.0 and 10.0 $\mu\textrm{g}$/kg, EE 3.0 $\mu\textrm{g}$/kg(gavage)/0.3 $\mu\textrm{g}$/kg(s.c) & ZM 0.1 mg/kg, and EE 3.0 $\mu\textrm{g}$/kg(gavage)/0.3 $\mu\textrm{g}$/kg (s.c) & ZM 1.0 mg/kg. There were no treatment-related changes in clinical signs, body weights, food consumption, and necropsy findings in any groups of two studies. The wet and blotted uterus weights increased dose-dependently. Histopathological examination revealed that diameter of uterine duct, height of uterine luminal epithelium. and height oj vaginal epithelium increased dose-dependently. The proliferating cell nuclear antigen (PCNA) immunoreactive cells were increased in number dose-dependently. The estrogenic effects observed in the present studies occurred at $\geq$ 0.3 $\mu\textrm{g}$/kg of oral dose and $\geq$ 0.1 $\mu\textrm{g}$/kg of s.c. dose. An antagonistic effect of ZM against EE was found in both uterus weight and histopathological parameters. From the results obtained, it can be concluded that dose-dependence of the uterotrophic assay using EE and ZM was well demonstrated by gavage and subcutaneous administration and that the estrogenic effects of EE by s.c. dose were higher than those by gavage administration. In addition, blotted uterus weight was more sensitive than wet uterus weight and vaginal epithelial height was found to be the most sensitive parameter among the parameters examined.

• YAKHAK HOEJI
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• v.45 no.6
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• pp.694-700
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• 2001

Synthetic pyrethroids are analysis of a natural chemical moiety, pyrethrin derived from the pyrethrum plant Chrysanthemum. The natural pyrethrin structure has been modified to be highly lipophilic and photostable, creating an effective pesticide and resulting in an increased presence in the environment. Worldwide, they are commonly used insecticides against ticks, mites, mosquitoes, and as treatment for human head lice and scabies. Therefore, human exposure to their compounds in extensive. Several studies on the effects of pyrethroids on thyroid hormone regulation, estrogen and androgen function have been reported and yet little has been done try assess their potential hormonal activities. Among humans, a pyrethroid compound was suggested to be the causal agent for gynecomastia in a group of Haitian men. The reports suggest that some pyrethroid compounds are capable of disrupting endocrine function. Therefore, we examined estrogenic/antiestrogenic potential of three pyrethroid insecticides, that is permethrin, allethrin and fenvalerate in human breast cancer cell and action mechanism mediated by the estrogen receptor. Fenvalerate showed weak estrogenic activity but aallethrin and permethrin showed no effect. In combination with high levels (10$^{-10}$ M, 10$^{-11}$ M) of 17$\beta$-estradiol and three synthetic pyrethroids inhibited cert proliferations in MCF7-BUS cell by 17$\beta$-estradiol. Whereas, fenvalerate increased cell proliferative activity at lower level of estradiol (10$^{-12}$ M, 10$^{-13}$ M). The relative affinities to the estrogen receptor were observed by allethrin and permethrin treatment, but not by fenvalerate. These results indicated that some of pyrethroid insecticides may modulate estrogen functions in human breast cancer cell. The action mechanisms of estrogen receptor mediated antiestrogenicity by allethrin and permethrin were postulated.