• Natural Product Sciences
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• 제6권1호
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• pp.25-30
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• 2000

To analyse scientifically the fundamental formulation theory and drug interaction of Chungpegagan-tang, the extraction level of puerarin and daidzin, the transforming activity of puerarin and daidzin to daidzein by human intestinal bacteria and in vitro cytotoxicity against tumor cell lines of Chungpesagan-tang were investigated. When Puerariae Radix was extracted with Chungpesagan-tang composing herbal medicines, the puerarin extraction level from these polyprescriptions was decreased by the extraction with Raphani Semen or Cimicifugae Rhizoma, but the other herbal medicines increased it. The activity transforming puerarin and daidzin to daidzein by human intestinal bacteria was increased by Raphani Semen, Cimicifugae Rhizoma and Angelicae Tenuissimae Radix, but decreased by Scutellariae Radix and Rhei Rhizoma. Puerariae Radix did not showed in vitro cytotoxicity against tumor cell lines. However, by its anaerobic incubation with human intestinal bacteria, it showed a potent cytotoxicity. When the main components, puerarin and daidzin, of Puerariae Radix were incubated with human intestinal bacteria, the main metabolites were daidzein and calycosin. These metabolites had the most potent cytotoxicity, compared to those of puerarin and daidzin. Raphani Semen, Rhei Rhizoma and Chungpesagan-tang had also the potent cytotoxicity against tumor cell lines by the anaerobic incubation with human intestinal bacteria.

• Asian Pacific Journal of Cancer Prevention
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• 제14권1호
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• pp.1-4
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• 2013

Background: The age-adjusted incidence rate of prostate cancer (PCa) has been reported to be lower among Asians than Western populations. A traditional Japanese meal, high in soybean products or isoflavones, may be associated with a decreased risk of PCa. Equol, which is converted from daidzein by human intestinal flora, is biologically more active than any other isoflavone aglycone. Materials and Methods: We reviewed not only recent epidemiological studies on association of isoflavones with PCa risk, but also recent research on human intestinal bacteria responsible for converting daidzein into equol. Studies were systematically searched from the database published within the last 5 years of from 2008-2012. Results: Five out of 6 articles showed significant association of isoflavones with a decreased risk of PCa, and two of them consistently showed that equol-producers carry a significantly reduced risk of PCa. Furthermore, 5 human intestinal bacteria that can convert daidzein into equol were identified in the last 5 years. Conclusions: If equol can reduce risk of PCa, a possible strategy for reducing the risk of PCa may be to increase the proportion of equol-producers by changing the intestinal flora to carrying an equol-producing bacterium with dietary alteration or probiotic technology.

• Asian-Australasian Journal of Animal Sciences
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• 제19권2호
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• pp.236-244
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• 2006

This study was designed to determine the effects of daidzein (DE) on hepatic lipid metabolism in chicks fed with low protein (LP) diet based on casein. In experiment 1, the male chicks were fed with one of the three levels of dietary protein containing 10.95%, 21.9% and 43.8% protein content for 2 days. In experiment 2, the chicks were fed one of the three levels of protein with or without DE at 1,000 mg/kg diet for 2 days. Experiment 3 was conducted to compare DE (LP+DE) with estradiol (LP+E2) in chicks fed with LP diet for 7 days. Plasma lipid profiles, hepatic lipid profiles, activities of hepatic malic enzyme and isocitrate dehydrogenase (ICDH) were measured. Transcriptions of hepatic fatty acid synthase, apolipoprotein-B (APO-B), and fructose bisphosphatase mRNA were measured by RT-PCR. Increasing dietary protein levels markedly decreased the concentrations of plasma triglycerides, hepatic total lipids, hepatic TG, and the mRNA transcriptions while the increased dietary protein levels increased hepatic ICDH activities in experiment 1. In experiment 2, the effects of dietary protein levels on blood and hepatic lipid content were more prominent than those of the additional DE. Interestingly, plasma TG levels were affected by DE supplementation (p<0.05). In experiment 3, DE inhibited APO-B mRNA expressions and stimulated the accumulation of lipid in the liver through mechanisms different from E2. In this study, we demonstrate that DE has beneficial effects on blood lipid profiles, but that it inhibits APO-B mRNA transcription and aggravates the fatty liver induced by LP diet in chicks.

• 한국식품과학회지
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• 제34권5호
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• pp.916-918
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• 2002

산가수분해시 산의 농도가 탈지대두박의 isoflavone 양에 미치는 영향을 조사하였다. 측정한 isoflavone은 daidzin, genistin 등 glucosides와 daidzein, genistein 등 aglycons이었다. 산가수분해는 탈지대두박 분말에 0.25 N-3.00 N HCl을 가하고 $95^{\circ}C$에서 4시간 가열하였다. 그 결과 총 isoflavone은 0.25 N-1.0 N HCl의 범위에서 가열이 진행되면서 증가하여 2시간 후에는 약 40% 증가함을 보였다. 그러나 그 이상의 농도에서는 현저한 감소가 있어 4시간 후에는 52%의 감소가 있었다. 이 결과는 낮은 HCl 농도에서의 증가는 isoflavone isomer가 isoflavone으로 전환되었음을 보여주고 높은 농도에서의 감소는 isoflavone이 분해됨을 보여주고 있다. 가열 중 각각의 isoflavone의 변화는 전체적으로 glucosides는 감소하고 aglycons는 증가하는 경향이었다. 특히 2 N HCl에서의 60분 반응시 daidzin과 genistin, glycitin 등 glucosides는 검출되지 않았다.

• Biomolecules & Therapeutics
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• 제27권4호
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• pp.363-372
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• 2019

Daidzein isolated from soybean (Glycine max) has been widely studied for its antioxidant and anti-inflammatory activities. However, the protective effects of 7,8,4'-trihydroxyisoflavone (THIF), a major metabolite of daidzein, on 6-hydroxydopamine (OHDA)-induced neurotoxicity are not well understood. In the current study, 7,8,4'-THIF significantly inhibited neuronal cell death and lactate dehydrogenase (LDH) release induced by 6-OHDA in SH-SY5Y cells, which were used as an in vitro model of Parkinson's disease (PD). Moreover, pretreatment with 7,8,4'-THIF significantly increased the levels of superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH) and decreased malondialdehyde (MDA) activity in 6-OHDA-induced SH-SY5Y cells. In addition, 7,8,4'-THIF significantly recovered 6-OHDA-induced cleaved caspase-3, cleaved caspase-9, cleaved poly-ADP-ribose polymerase (PARP), increased Bax, and decreased Bcl-2 levels. Additionally, 7,8,4'-THIF significantly restored the expression levels of phosphorylated c-Jun N-terminal kinase (JNK), p38 mitogen-activated protein kinase (MAPK), extracellular signal-regulated kinase 1/2 (ERK 1/2), phosphatidylinositol 3-kinases (PI3K)/Akt, and glycogen synthase kinase-3 beta ($GSK-3{\beta}$) in 6-OHDA-induced SH-SY5Y cells. Further, 7,8,4'-THIF significantly increased the reduced tyrosine hydroxylase (TH) level induced by 6-OHDA in SH-SY5Y cells. Collectively, these results suggest that 7,8,4'-THIF protects against 6-OHDA-induced neuronal cell death in cellular PD models. Also, these effects are mediated partly by inhibiting activation of the MAPK and PI3K/Akt/$GSK-3{\beta}$ pathways.

• 한국식품과학회지
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• 제34권4호
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• pp.710-718
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• 2002

콩과 식물인 갈근에는 genistein과 daidzein이 함유된 것으로 알려졌으므로 본 연구는 갈근(PR), 갈화(PF) 및 어린순인 갈용(PL)에 함유된 phytoestrogen의 함량을 HPLC법으로 정량 분석하였다. 동시에 phytoestrogen의 골다공증 치료제에 대한 효능 검색의 일환으로 조골세포의 증식작용(MTT법 및 ALP분석)과 피골세포의 활성(TRAP법)을 측정하였고 난소절제 흰쥐에 PR 1 g/kg/day(PR-1) 및 PR 5 g/kg/day(PR-5)을 9주 동안 투여한 후 혈액분석, 혈장 Alkaline phospatase(ALP), 칼슘, 무기성 인산염, 총콜레스테롤, LDL- 및 HDL-콜레스테롤을 측정하였고 적출된 경골 및 요추골의 소주골면적을 측정하였다. PR과 PF의 총 daidzein의 함량은 $10436{\pm}2144\;mg/kg$와 $1003{\pm}206\;mg/kg$이었고 genistein과 formononetin은 PR에만 존재하고 PF 및 PL에는 함유되어 있지 않았다. 인간 유사 조골 세포주인 Saos-2에 PR은 대조군의 158% 정도(5 mg/mL)의 세포증식효과와 ALP 활성을 증가시켰으나 전처리한 PR, PF 및 PL의 세포증식효과는 없었고 PL만이 ALP 활성을 증가시켰다. 파골세포의 증식억제실험에서 genistein의 $IC_{50}$는 $1.57{\times}10^{-4}\;mg/mL$ $(5.81{\times}10^{-7}\;M)$이었고, daidzein과 PR은 효과가 없었다. 난소절제 흰쥐에 대한 in vivo 실험에서 대조군이 sham군보다 난소적출 1주 후부터 체중의 증가가 급격하게 나타났으나 PR의 투여로 둔화되었다. PR 투약에 의한 자궁의 무게는 PR-5군은 대조군에 비해 증가되었고(p<0.05), PR-1군은 대조군과 유의성이 없었다. 혈장 ALP의 활성은 주령의 증가에 EK라 감소하는 경향을 보였고, HDL-콜레스테롤의 농도는 모든 군에서 주령에 따라 감소되었으나(p<0.01), PR-5군의 LDL-콜레스테롤의 농도는 대조군에 비해 감소되었다(p<0.01). 대조군에 비해 sham군의 경골 및 요추골의 면적은 증가되었고(p<0.01), PR 투여군(PR-1 및 PR-5)도 sham보다 적으나 대조군에 비해 소주골 면적이 증가되었다(각 p<0.01). 특히 고용량의 PR 투여는 PR의 골다공증 치료효과가 우수함을 증명하였으며(p<0.01), PL과 PF는 효능이 미비하나 PR은 골다공증의 예방 및 치료제로는 상당히 우수한 한약재임이 확인되었다.

• Asian-Australasian Journal of Animal Sciences
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• 제15권7호
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• pp.1066-1070
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• 2002

10 male piglets at 5-6 weeks old with similar body weight (BW) were randomly assigned into the experimental (EXP) and control (CON) groups. The animals in EXP received intro-muscular injection with daidzein (DA) at the dose of 0.5 mg DA per kg start BW on day 1. The same procedures were repeated once every 3 days for eight times. The animals in CON received the injection only with same volume of control peanut oil. The animals were weighted on day 14 and 28 and the blood samples were obtained at different stages of the treatment for determining IGF-I levels and blood parameters. At the end of the experiment, the thymus and spleen from all the animals were surgically taken out and weighted. The results showed that BW and average daily gain (ADG) were not significantly different between the groups in term of the whole period, but ADG between days 14-28 was higher in EXP than in CON (p<0.05). On days 18, 21 and 25, IGF-I levels in EXP group were 20.53% (p<0.05), 15.92% (p>0.05) and 23.46% (p<0.05), respectively, higher than those in CON. The weights of thymus and spleen, the ratios of their weights to BW and red blood count (RBC) did not significantly differ between the groups at all stages. White blood count (WBC) in EXP steadily increased from day 22, reached its apex on day 24, which was higher than in CON (p<0.05) and its own levels on day 20 and 22 (p<0.01 or p<0.05), and remained higher on the later time (p=0.058). The results of percentage of T-Lymphocytes also demonstrated similar trend to WBC, but TLymphocyte transformation rate (%) appeared no significant change between the groups. In conclusion, Daidzein could stimulate male piglet growth and elevate serum IGF-I levels at certain stages of the treatment. It could also increase WBC and T-Lymphocyte rates, but had no significant impacts on RBC and T-Lymphocyte transformation rate.

• 대한의생명과학회지
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• 제11권2호
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• pp.175-183
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• 2005

The two major isoflavones in soy, genistein and daidzein, are well known to prevent hormone-dependent cancers by their anti estrogenic activity. The exact molecular mechanisms for the protective action are, however, not provided yet. It has been reported that genistein and daidzein have a potential anticancer activity through their antiproliferative effect in many hormone-dependent cancer cell lines. Transforming growth $factor-\beta1(TGF-\beta1)$ has also been found to have cell growth inhibitory effect, especially in mammary epithelial cells. This knowledge led to a hypothetical mechanism that the soy isoflavones-induced growth inhibitory effect can be derived from the regulation of $TGF-\beta1$ and $TGF-\beta$ receptors. In order to test this hypothesis, the effects of the soy isoflavones at various concentrations and periods on the expression of $TGF-\beta1$and $TGF-\beta$ receptors were investigated by using Northern blot analysis in human breast carcinoma epithelial cell lines, an estrogen receptor positive cell line (MCF-7) and an estrogen receptor negative cell line (MDA-MB-231). As a result, only genistein has shown a profound dose-dependent effect on $TGF-\beta1$ expression in the $ER^+$ cell line within the range of doses tested, and the expression levels are correspondent to their inhibitory activities of cell growth. Moreover, daidzein showed down-regulated $TGF-\beta1$ expression at a low dose, the cell growth proliferation was promoted at the same condition. Therefore, antiproliferative activity of the soy isoflavones can be mediated by $TGF-\beta1$ expression, and the effects are mainly, if not all, occurred by ER dependent pathway. The expression of $TGF-\beta$ receptors was induced at a lower dose than the one for $TGF-{\beta}1$ induction regardless of the presence of ER, and the expression patterns are similar to those of the cell growth inhibition. These results indicated that the regulation of $TGF-\beta$ receptor expression as well, prior to $TGF-\beta1$ expression, may be involved in the antiproliferative activity of soy isoflavones. Little or no expression of $TGF-\beta$ receptors was found in the MCF-7 and MDA-MB-231 cells, suggesting refractory properties of the cells to growth inhibitory effect of the $TGF-\beta$. The soy isoflavones can seemingly restore the sensitivity of growth inhibitory responses to $TGF-\beta1$ by re-inducing $TGF-\beta$ receptors expression. In conclusions, our findings presented in this study show that the antitumorigenic activity of the soy isoflavones could be mediated by not only $TGF-\beta1$induction but $TGF-\beta$ receptor restoration. Thus, soy isoflavones could be good model molecules to develop new nonsteroidal antiestrogenic chemopreventive agents, associated with, regulation of $TGF-\beta$ and its receptors.

• 한국식품영양과학회지
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• 제30권4호
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• pp.662-667
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• 2001

Bacillus 균주를 이용하여 42$^{\circ}C$에서 72시간동안 발효된 검정콩 청국장의 몇 가지 생리활성 및 sioflavone(daidzein, genistein) 함량을 조사하였다. B. subtilis 보다는 분리균주 Bacillus megaterium SMY-212 균주를 첨가한 청국장이 항균활성이 매우 높았고, 대립 검정콩의 메탄올 추출물이 소립 검정콩의 것보다 항균 효과가 우수하였다. 청국장의 수소공여능은 대립 및 소립 검정콩 청국장에서 각각 76.4 및 75.5%를 나타내었으며, B. subtilis 및 SMY-212 를 첨가한 것은 무첨가보다 약간 높게 나타났다. 아질산염 소거능은 대립 검정콩이 소립 검정콩보다 그 효과가 크게 나타났으나, 균종간에는 차이가 나타나지 않았다. Linoleic acid 에 대한 과산화물가 및 흰쥐의 liver homogenate에 의한 TBARS 함량으로부터 볼 때 검정콩 청국장의 메탄올 추출물은 상당한 항산화효과가 있었다. 그 효과는 소립 검정콩의 청국장 추출물이 대립 검정콩의 청국장 추출물보다, 균주 첨가 청국장 추출물이 균주 무첨가 청국장 추출물보다 크게 나타났다. 청국장의 daidzein 및 genisteing함량은 발효 중 증가하였으며, 대립 검정콩 청국장이 소립 검정콩 청국장에 비하여 약간 높았다.

• 한국작물학회지
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• 제51권1호
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• pp.81-88
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• 2006

The 117 soybean cultivars were collected from nine provinces in Korea, and various seed quality traits along with isoflavone contents were evaluated to elucidate their relationship. The 100-seed weight of the black soybean (31.2 g) was significantly higher (p<0.05) than yellow soybeans (28.6 g). The composition of genistein, daidzein, and glycitein accounted for 75.8, 22.8, and 1.4 % of total isoflavone in yellow soybean cultivars, while their compositions in black soybeans were 58.5, 39.7, and 1.8%, respectively. The mean contents of total isoflavone in yellow and black soybean were $l,561.6{\mu}g\;g^{-1}\;and\;l,018.3{\mu}g\;g^{-1}$. The isofalvone content showed significant variation among cultivars when classified by the seed size. In the yellow soybeans, total isoflavone content was higher in small size soybean cultivars $(1,776.0{\mu}g\;g^{-1})$ and medium size soybean cultivars $(1,714.3{\mu}g\;g^{-1})$ compared to large size ones $(1,518.5{\mu}g\;g^{-1})$. Genistein content was proved as the major factor determining the relationship between isoflavone content and 100-seed weights (r =-0.206*). Daidzein and glycitein, however, showed no significant relationship with the 100-seed weights. Isoflavone content was not significantly correlated with color parameters L (lightness) and a (redness) values, but color parameter b (yellowness) was positively correlated with glycitein (r=0.264*) in the yellow soybeans, while its negative correlation between daidzein (r=-0.245*) and total isoflavone (r=-0.256*) were observed in black soybeans. However, these findings suggested that the seed color value may not serve as an effective parameter for estimating the isoflavone intensity of the soybeans. Variation of protein and lipid contents between yellow soybeans (n=58) and black soybeans (n=59) was relatively stable, however, protein and lipid contents have no significant relationship with isoflavone content.