• Toxicological Research
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• v.18 no.4
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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.

• Advances in Traditional Medicine
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• v.3 no.3
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• pp.133-140
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• 2003

Petroleum ether, chloroform and ethanol extracts of the seeds of Melia azedarach Linn. administered orally to male rats at the dose level of 25 mg/100 g body weight for 48 days showed antispermatogenic activity, as the number of spermatocytes, spermatids and spermatozoa was decreased. The total cholesterol content was increased while protein and glycogen contents were decreased. The acid phosphatase content was also decreased while that of alkaline phosphatase increased. At the same time the weight of caput and cauda epididymis, prostate gland, seminal vesicle and Levator Ani muscle was decreased indicating its antiandrogenic property. Of the three extracts, the petroleum ether extract was more potent in its antispermatogenic and antiandrogenic activities and did not produce any sings of toxicity upto a dose of 25 mg/100 g body weight oral administration. After subjecting it to preliminary phytochemical screening the petroleum ether extract showed positive tests for steroids and saponins.

• Advances in Traditional Medicine
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• v.6 no.2
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• pp.86-95
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• 2006

The ethanol extract of the Crotalaria juncea seeds, which showed promising antispermatogenic and antiandrogenic activities in albino mice, was taken up further for the isolation of the active fractions present in it. Two fractions that were obtained from thin layer chromatography were subjected for testing to know their antispermatogenic and antiandrogenic activities. After preliminary trials the fraction I showed maximum antifertility activity at the dose level of 200 mg/kg body weight when administered orally to the rats for 50 days. The fraction I was found to affect spermatogenesis as well as the endocrine functions of the testis as indicated by gravimetric, histopathological and biochemical changes. Further this fraction has caused degenerative changes in the seminiferous tubules and Leydig cells of the testis. The accessory reproductive organs like epididymis, seminal vesicles, vas deferens, prostrate, Cowper's gland and Levator Ani muscle showed significant malfunction. Cauda epididymal sperm count and sperm motility were reduced significantly. The treatment has also resulted in increase in the cholesterol level and alkaline phosphatase activity, and decrease in protein, glycogen, sialic acid contents and acid phosphatase activity in testis. It is noteworthy that RIA studies have shown significant reduction in serum FSH, LH and testosterone. Scanning electron microscopic observations revealed abnormalities in sperm structure.

• Proceedings of the Korean Society of Toxicology Conference
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• 2005.05a
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• pp.107-107
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• 2005

• Proceedings of the PSK Conference
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• 2000.10a
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• pp.169.2-170
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• 2000

• Korean Journal of Food Science and Technology
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• v.31 no.2
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• pp.535-539
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• 1999

Soybean has drawn much attention mainly due to its chemopreventive action as well as antiestrogenic effect. Although suppression of breast and prostate cancers were believed to be exerted via antiestrogenic or antiandrogenic activity of genistein, its mechanism of prevention against other cancers has not been clearly demonstrated. We proposed that prevention by soybean from other cancers than sex hormone -related cancers was achieved via modulation of drug-metabolizing enzymes. Addition of acid hydrolysate of 80% methanol extract of soyflour to diet caused a significant induction of quinone reductase, an anticarcinogenic marker enzyme and one of drug-metabolizing enzymes, in mouse lung while it suppressed arylhydrocarbon hydroxylase, involved in bioactivation of procarcinogens, in kidney and small intestine. It is likely that active components exist in a conjugated form and released by acid hydrolysis to be able to affect drug-metabolizing enzyme and exert chemopreventive activity. Benzo(a)pyrene-induced tumor development in mouse lung was greatly reduced by soybean extract supplementation, which is consistent with the extract's capability to modulate favorably arylhydrocarbon hydroxylase and quinone reductase towards chemoprevention.

• Development and Reproduction
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• v.21 no.4
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• pp.441-448
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• 2017

Bisphenol-A(BPA) is a member of alkylphenol family, and shows adverse effects including reduced fertility, reproductive tract abnormalities, metabolic disorder, cancer induction, neurotoxicity and immunotoxicity. In the present study, we conducted Hershberger assay to evaluate whether the two candidates to replace BPA have androgenic or antiandrogenic activity. The assay was carried out using immature castrated Sprague-Dawley male rats. After 7 days of the surgery, testosterone propionate (TP, 0.4 mg/kg/day) and test materials (low dose, 40 mg/kg/day; high dose, 400 mg/kg/day) were administered for 10 consecutive days by subcutaneous (s.c.) injection and oral gavage, respectively. Test materials were BPA, isosorbide (ISO) and cyclohexanedimethanol (CHDM). The rats were necropsied, and then the weights of five androgen-dependent tissues [ventral prostate, seminal vesicle, levator ani-bulbocavernosus (LABC) muscle, paired Cowper's glands, and glans penis] and three androgen-insensitive tissues (kidney, spleen and liver) were measured. All test materials including BPA did not exhibit any androgenic activity in the assay. On the contrary, antiandrogen-like activities were found in all test groups, and the order of the intensity was CHDM > BPA > ISO in the five androgen-sensitive tissues. There was no statistical difference between low dose treatment and high dose treatment of BPA group as well as ISO group. In CHDM group, high dose treatment exhibited most severe weight reduction in all measured tissues. There was no statistical difference in androgen-insensitive tissue measurements, except BPA groups. Since the effects of ISO treatment on the accessory sex organs were much less or not present at all when compared to those of BPA, ISO could be a strong candidate to replace BPA. CHDM treatment brought most severe weight reduction in all of androgen-sensitive tissues, so this material should be excluded for further screening of BPA substitute selection.

• Development and Reproduction
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• v.22 no.1
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• pp.19-27
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• 2018

In the present study, we employed Hershberger assay to determine possible androgenic or antiandrogenic activities of three di-2-ethylhexyl phthalate (DEHP) substitute candidates. The assay was carried out using immature castrated Sprague-Dawley male rats. After 7 days of the surgery, testosterone propionate (TP, 0.4 mg/kg/day) and test materials (low dose, 40 mg/kg/day; high dose, 400 mg/kg/day) were administered for 10 consecutive days by subcutaneous (s.c.) injection and oral gavage, respectively. Test materials were DEHP, 2-ethylhexyl oleate (IOO), 2-ethylhexyl stearate (IOS) and triethyl 2-acetylcitrate (ATEC). The rats were necropsied, and then the weights of five androgen-dependent tissues [ventral prostate, seminal vesicle, coagulating glands, levator ani-bulbocavernosus (LABC) muscle, paired Cowper's glands, and glans penis] and four androgen-insensitive tissues (kidney, adrenal glands, spleen and liver) were measured. All test materials including DEHP did not exhibit any androgenic activity in the assay. On the contrary, antiandrogen-like activities were found in all test groups, and the order of the intensity was ATEC < DEHP < ISO < IOO in the five androgen-sensitive tissues. There was no statistical difference between low dose treatment and high dose treatment of all replacement candidate groups. In DEHP groups, high dose treatment exhibited significant weight gains in LABC and Glan Penis. There was no statistical difference in androgen-insensitive tissue measurements. Since the effects of ATEC treatment on the accessory sex organs were much less or not present at all when compared to those of DEHP, ATEC could be a strong candidate to replace DEHP. IOO treatment brought most severe weight reduction in all of androgen-sensitive tissues, so this material should be excluded for further screening of DEHP substitute selection.

• Korean Journal of Environmental Biology
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• v.27 no.4
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• pp.323-333
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• 2009

Parabens are alkyl esters of p-hydroxybenzoic acid, which are widely used in foods, cosmetics, and pharmaceutic products as preservatives. Absorbed parabens are metabolized fastly and excreted. Actually human body is exposed to complex mixture of parabens. Safety assessment at various toxicological end points revealed parabens have a little acute, subacute and chronic toxicities. Some reports have argued that as parabens have estrogenic activity, they are associated with the incidence of breast cancer through dermal absorption by cosmetics. There is an inference that antiandrogenic activity of parabens may give rise to a lesion of male reproductive system, but also there is an contrary. At cellular level, parabens may inhibit mitochondrial function of sperms and androgen production in testis, but also there is an contrary. Parabens seem to have little or no toxicity in embryonic development. Parabens can cause hemolysis, membrane permeability change in mitochondria and apoptosis, suggesting cellular toxicity of parabens. Parabens evoked endocrine disruption in several fish species and have toxic effect on small invertebrates and microbes. Therefore, the toxicity of parabens should be considered as a potentially toxic chemical in the freshwater environment. In conclusion, though parabens may be considered as a low toxic chemical, more definite data are required concerning the endocrine disrupting effect of parabens on human body and aquatic animals according to route and term of exposure as well as the residual concentration of parabens.