• Journal of the Korean Society of Food Science and Nutrition
• /
• v.45 no.10
• /
• pp.1430-1437
• /
• 2016

This study was performed to investigate the changes in isoflavone composition, estrogenic activity and antiestrogenic activity of soybean cultivars of different isoflavone content (Aga 8, Uram, Cheongja 3, and Dawon) with germination. Total isoflavone contents of Aga 8, Dawon and Cheongja 3 was increased from 2,671.74, 261.08 and 2,240.08 to 2,977.50, 966.13 and $2,354.11{\mu}g/g$, respectively after germination except for Uram cultivars, and highest contents of total isoflavone showed $2,977.50{\mu}g/g$ and $2,354.11{\mu}g/g$, respectively in Aga 8 and Cheongja 3 after germination. MTT cell proliferation assay using MCF-7 cells revealed that germinated soybean of Aga 8 and Cheonja 3 obtained not only contained a high content of isoflavone but also had estrogenic activity. Estrogenic activity of Aga 8 and Cheongja 3 soybean extracts increased from 116.21% and 101.60% to 135.34% and 121.05% after germination. These results suggest that germinated soybean of Aga 8 and Cheongja 3 might have a potential preventive effect on estrogen-deficient diseases.

• Toxicological Research
• /
• v.27 no.3
• /
• pp.181-184
• /
• 2011

Screening of estrogenic activity on dichloro diphenyl trichloroethane (DDT), dichloro diphenyl dichloro ethylene (DDE), dieldrin, heptachlor, aldrin, chlordane, lindane, polybrominated diphenyl ethers (PBDE) and parabens was compared using Organization for Economic Cooperation and Development (OECD) test guideline 455 (TG455). The estrogenic activity of DDT was 58,000-fold ($PC_{50}$, $1.67{\times}10^{-6}$ M) less than $17{\beta}$-estradiol($E_2$) ($PC_{50}$, $2.88{\times}10^{-11}$ M) but DDE, dieldrin, heptachlor, aldrin, chlordane, lindane and PBDE did not show any estrogenic activity in this assay system. In the case of paraben compounds, the rank of relative transcriptional activation (logRTA) was butyl paraben -1.63752 ($PC_{50}$, $1.25{\times}10^{-7}$ M) > isobutyl paraben -2.34008 ($PC_{50}$, $6.3{\times}10^{-7}$ M) > ethyl paraben -2.64016 ($PC_{50}$, $1.26{\times}10^{-6}$ M) > isopropyl paraben -2.73993 ($PC_{50}$, $1.58{\times}10^{-6}$ M) > propyl paraben -2.84164 ($PC_{50}$, $2.0{\times}10^{-6}$ M). Our data suggest that OECD test guideline TG455 may be useful as a screening tool for potential endocrine disruptors.

• Asian Pacific Journal of Cancer Prevention
• /
• v.13 no.2
• /
• pp.427-436
• /
• 2012

Targeted therapy has been a very promising strategy of drug development research. Many molecular mechanims of diseases have been known to be regulated by abundance of proteins, such as receptors and hormones. Chemoprevention for treatment and prevention of diseases are continuously developed. Pre-clinical and clinical studies in chemoprevention field yielded many valuable data in preventing the onset of disease and suppressing the progress of their growth, making chemoprevention a challenging and a very rational strategy in future researches. Natural products being rich of flavonoids are those fruits belong to the genus citrus. Ethanolic extract of Citrus reticulata and Citrus aurantiifolia peels showed anticarcinogenic, antiproliferative, co-chemotherapeutic and estrogenic effects. Several examples of citrus flavonoids that are potential as chemotherapeutic agents are tangeretin, nobiletin, hesperetin, hesperidin, naringenin, and naringin. Those flavonoids have been shown to possess inhibition activity on certain cancer cells' growth through various mechanisms. Moreover, citrus flavonoids also perform promising effect in combination with several chemotherapeutic agents against the growth of cancer cells. Some mechanisms involved in those activities are through cell cycle modulation, antiangiogenic effect, and apoptosis induction.Previous studies showed that tangeretin suppressed the growth of T47D breast cancer cells by inhibiting ERK phosphorylation. While in combination with tamoxifen, doxorubicin, and 5-FU, respectively, it was proven to be synergist on several cancer cells. Hesperidin and naringenin increased cytotoxicitity of doxorubicin on MCF-7 cells and HeLa cells. Besides, citrus flavonoids also performed estrogenic effect in vivo. One example is hesperidin having the ability to decrease the concentration of serum and hepatic lipid and reduce osteoporosis of ovariectomized rats. Those studies showed the great potential of citrus fruits as natural product to be developed as not only the source of co-chemotherapeutic agents, but also phyto-estrogens. Therefore, further study needs to be conducted to explore the potential of citrus fruits in overcoming cancer.

• Reproductive and Developmental Biology
• /
• v.35 no.1
• /
• pp.47-54
• /
• 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.

• Proceedings of the Korea Society of Environmental Toocicology Conference
• /
• 2001.05a
• /
• pp.126-126
• /
• 2001

Over the last few years, an increased awareness of endocrine disrupting chemicals (EDCs) and their potential to affect wildlife and humans has produced a demand for practical screening methods to identify endocrine activity in a wild range of environmental and industrial chemicals. It is clear that in vivo methods will be required to identify adverse effects produced by these chemicals. (omitted)

• Journal of the East Asian Society of Dietary Life
• /
• v.15 no.3
• /
• pp.315-322
• /
• 2005

In this study we report on the estrogen activity of silkworm pupa and herb extracts in vitro. The estrogenic activity of these resources was investigated by competition binding assays with estrogen receptor $\alpha(ER{\alpha})\;or\;ER{\beta}$, and viability of MCF-7 cells, a human breast cancer cell line. Saturation ligand-binding analysis of $ER{\alpha}\;and\;ER{\beta}$ revealed that all plant extracts competed with estrogen ligand for binding to both ER subtypes with a similar preference and degree and competed stronger with ligand for binding to $ER{\beta}\;than\;to\;ER{\alpha}$. The highest $ER{\alpha}-binding$ sample was silkworm pupa aqueous extract The highest $ER{\beta}-binding$ sample was silkworm pupa oil. These samples were further tested for bioactivity based on their ability to regulate cell growth rate in ER(+) breast cancer cell line, MCF-7 cells. Our studies showed that silkworm pupa, soritae, sesame, yam, pueraria, malt, ginseng, Polygonum multiflorum, and Curcuma longa significantly stimulated the growth of MCF-7 cells (P<0.05). In summary, these results suggested that silkworm pupa and herbs might be useful as potential phytoestrogens.

• Environmental Mutagens and Carcinogens
• /
• v.22 no.4
• /
• pp.259-265
• /
• 2002

Phthalate analogues are a plasticizer and solvent used in industry. Phthalates were reported to be a potential carcinogen classified in the category of suspected endocrine disruptors. Most common human exposure to these compounds may occur with contaminated food. They may migrate into food from plastic wrap or may enter food from general environmental contamination. Since these substances are not limited to the original products, and enter the environment, they have become widespread environmental pollutants, thus leading to a variety of phthalates that possibly threaten the public health. Concern about their use has been mounting. To screen and elucidate the endocrine disrupting activity and their mechanism of phthalate analogues, first of all, E-screen assay was performed in MCF7 human breast cancer cells with seven phthalate analogues. In this cell proliferation assay, only dibutyl phthalate (DBP) showed weak estrogenic activity. Also the yeast-based transcription assay to assess the interactions of DBP with the estrogen, androgen, and progesterone receptors was conducted. DBP in the concentration ranges from 10$^{-16}$ to 10$^{-11}$ M was active in the estrogen transcriptional assay, but it did not show the effect on $\beta$-galactosidase activity in the progesterone and androgen transcriptional assays. These data indicate that DBP shows estrogenic potential and can be classified as weak and/or suspected endocrine disrupting chemicals.

• Korean Journal of Food Science and Technology
• /
• v.37 no.4
• /
• pp.549-556
• /
• 2005

Estrogenic and antioxidant activities of ethanol extracts of 45 edible and medicinal plants were evaluated by ${\beta}-galactosidase$ assay, and DPPH radical scavenging assay, and TBARS inhibition rate, respectively. Total polyphenol contents were in the range of 8.6 (Panax notoginseng Buck F.H. Chen.)-594.7 (Amomum globosum Loureiro) mg/g. Direct correlation between the DPPH radical scavenging activity and polyphenol content $(r^2=0.61)$ was established through simple regression analysis, whereas no correlation was observed between TBARS inhibition rate or ${\beta}-galactosidase$ activity and polyphenol content. Among medicinal plants screened, Glycyrrhiza glabra L. and Rheum undulatum L. showed strong antioxidant and estrogenic activities. Results of this study could be used as fundamental data for selecting potential phytoestrogen candidates.

• Proceedings of the Korea Society of Environmental Toocicology Conference
• /
• 2003.10a
• /
• pp.57-69
• /
• 2003

It is well known that many pesticides possess hormonal activity, and affect the developments of wildlife and mammals including human. Currently, pyrethroid insecticides are in worldwide use to control in and outdoor pests, providing potential far environmental exposure. Hormonal activities of these pyrethroid insecticides, however, have been little studied, and the developmental effects of them were no reported. Therefore, we firstly examined the potential estrogenic activities of some pyrethroid insecticides (permethrin, cypermethrin, tetramethrin, deltamethrin, sumithrin, fenvalerate and bioallethrin) by immature rat uterotrophic assay, luciferase reporter gene assay and Calbindin-D$\sub$9k/ (CaBP-9k) gene expression assay. Uterine wet weights were increased by permethrin and the permethrin-induced weights were inhibited by ICI 182780 in the uterolrophic assay. On the other hand tetramethrin significantly reduced uterine and vaginal wet weights, and also inhibited the E2-induced weight increases at all doses tested. Cypermethrin and sumithrin had a tendency to increase uterine weights, although not statistically significant. Permethrin and cypermethrin dose-dependently increased the luciferase activity in reporter gene assay. Northern blot analysis showed that permethrin induced CaBP-9k mRNA expression whereas tetramethrin inhibted. Subsequent studies were conducted to investigate the possible developmental effects of four pyrethroid insecricides (permethrin, cypermethrin, sumithrin and teramethrin). Either diethlbestrol (DES) or 17${\beta}$ -estradiol (E2) was used as a reference control in this study. Pyrethroid insecticides were administered to Sprague Dawley rats via subcutaneous injection at 6 to 18 days of gestation or 1 to 5 days after birth. In utero treatment of permethrin (10mg/kg/day) in female rat resulted in significant increases in uterine and ovarian weights while significant decreases in serum E2 concentration, uterine and ovarian ER${\alpha}$ mRNA levels. Sumithrin and permethrin led to acceleration in vaginal opening of female rat, while delay in preputial separation of male after neonatal treatment. Anogenital distances of PND 18 were significantly reduced in sumthrin-treated, and permerhrin-treated male rats after neonatal treatment. All the pyrethroid insecticides tested caused significant increases in uterine weights on PND 18, while significant reductions in the first diestrus phase when neonataly treated. In addition, exposure to pyrethroids in neonatal period led to significant reduction in relative brain weight in female rat on PND 18, but its weight was recovered in diestrus phase. In summary, Our experimental data demonstrate the possibilities of developmental effects of pyrethroid insecticides via estrogenic or antiestrogenic activity.

• Proceedings of the PSK Conference
• /
• 2003.04a
• /
• pp.173.2-174
• /
• 2003

Many pesticides possess hormonal activity and have been thus classified as endocrine disruptors. Bioallethrin is one of the pyrethroids. synthetic derivatives of naturally occurring pyrethrins. These pyrethroids including bioallethrin have been developed as insectides due to their high insecticidal potency and low mammalian toxicity. Currently, bioallethrin is used to eradicate pests and insects in Korea, providing potential for human exposure. (omitted)