• Title/Summary/Keyword: ${\beta}-1$

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Antioxidative flavonoids from the Leaves of Morus alba

  • Kim, Sun-Yeou;Gao, Jian Jun;Lee, Won-Chu;Ryu, Kang-Sun;Lee, Kang-Ro;Kim, Young-Choong
    • Archives of Pharmacal Research
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    • v.22 no.1
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    • pp.81-85
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    • 1999
  • Nine flavonoids (1-9) were isolated from the leaves of Morus alba (Moraceae). The structures of compounds were determined to be kaempferol-3-O-$\beta$-glucopyranoisde (astragalin, 1) kaempferol-3-O-(6"-O-acetyl)-$\beta$-D-glucopyranoside (2), quercetin-3-O-(6"-O-acetyl)-$\beta$-D-glucopyranoside (3), quercetin-3-O-$\beta$-D-glucopyranoside (4), kaempferol-3-O-$\alpha$-L-rhamnopyranosyl-(1 6)-$\beta$-D-glucopyranoside (5), quercetin-3-O-$\alpha$-L-rhamnopyranosyl-(1 6)-$\beta$-D-glucopyranoside (rutin, 6), quercetin-3-O-$\beta$-D-glucopyranosyl-(1 6)-$\beta$-D-glucopyranoside (7), quercetin-3,7-di-O-$\beta$-D-glucopyranoside (8) and quercetin (9) on th basis of spectroscopic and chemical studies. Compounds 7 and 9 exhibited significant radical scavenging effect on 1,1-diphenyl-2-picryl-hydrazyl radical.

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Regulation of Estrogen Receptor Under Hypoxia in Breast Cancer Cells

  • Lee, Young-Joo
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2008.04a
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    • pp.55-74
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    • 2008
  • Previously, we have shown that hypoxia, through HIF-1, induces ligand-independent $ER{\alpha}$ activation and the physical interaction of HIF-1 and $ER{\alpha}$. However, the effect of hypoxia on the transactivation of $ER{\beta}$ is not yet known. In the present study, we found that hypoxia activated the $ER{\beta}$-mediated transcriptional response in the HEK 293 cell line, as determined by the transient expression of$ER{\beta}$ and ER-responsive reporter plasmids. The hypoxia-induced estrogen response element-mediated transcriptional response was dependent on $ER{\beta}$ expression and was inhibited by the ER antagonist ICI 182,780. Transactivation of $ER{\beta}$ was induced by the expression of HIF-$1{\alpha}$ under normoxic conditions, as determined by the expression of oxygen-independent stable GFP-HIF-$1{\alpha}$. HIF-$1{\alpha}$-induced $ER{\beta}$ transactivation was abolished by the inhibition of HIF-$1{\alpha}$ activation. This was determined by using chemical inhibitors for the MAPK pathway. In addition, HIF-$1{\alpha}$ interacted with $ER{\beta}$ in a mammalian-two hybrid assay. We conclude that hypoxia activates $ER{\beta}$ in a ligand-independent manner, possibly through the interaction of HIF-$1{\alpha}$ and $ER{\beta}$.

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Discovery of Novel 11β-HSD1 Inhibitors by Pharmacophore-Based Virtual Screening

  • Kim, Nam-Doo;Lee, Youn-Ho;Han, Chang-Kyun;Ahn, Soon-Kil
    • Bulletin of the Korean Chemical Society
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    • v.33 no.7
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    • pp.2365-2368
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    • 2012
  • The $11{\beta}$-hydroxysteroid dehydrogenase type 1 ($11{\beta}$-HSD1) enzyme is involved in modulation of glucocorticoid activity within target tissues. This enzyme may contribute to obesity and/or metabolic disease through its action in adipose or liver tissue. Inhibition of $11{\beta}$-HSD1 has major therapeutic potential for glucocorticoid-associated diseases, including obesity, diabetes (wound healing), and muscle atrophy. To develop such therapeutics, we performed a pharmacophore-based virtual screening (VS) for identification of novel $11{\beta}$-HSD1 inhibitors and found that the VS hit compounds show potent inhibition of $11{\beta}$-HSD1 enzyme activity. Further, we present a binding model for active compounds. The proposed pharmacophore may serve as a useful guideline for future design of new chemical entities as $11{\beta}$-HSD1-targeted antidiabetic agents.

Comparisons of amino acid sequences of ${\beta}$-globin gene between carp and other vertebrates (잉어와 척추동물들의 ${\beta}$-globin 아미노산배열의 비교)

  • 진덕희
    • Journal of Life Science
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    • v.8 no.3
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    • pp.249-256
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    • 1998
  • The purpose of this study was to understand the evolutionary relationships between fish and other vertebrates which had DNA with the genetic defects in homoglobin expression, with comparison to the nucleotide homologies of the ${\beta}$-globin genes. The predicted amino acid sequence from carp ${\beta}$-globin gene was compared with those of other vertebrates from the published data. The nucleotide homologies of the predicted amino acid sequence from the carp ${\beta}$-globin gene with those of goldfish and mirror carp were high, and the rates were 97.3% and 93.9%, respectively. On the other hand, with the previously reported ${\beta}$-globins of goat, frog, human, rat, goose, chicken, and duck, it showed low homology ranging from 45.9 to 58.1%. The carp ${\beta}$-globin has one inserted amino acid residue, which was also found in other fish ${\beta}$globin, but not in other vertebrate ${\beta}$-globins.

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Expression of β-arrestin 1 in Gastric Cardiac Adenocarcinoma and its Relation with Progression

  • Wang, Li-Guang;Su, Ben-Hua;Du, Jia-Jun
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.11
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    • pp.5671-5675
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    • 2012
  • Objective: Arrestins act as mediators of G protein-coupled receptor (GPCR) desensitization and trafficking, also actin as a scaffold for many intracellular signaling network. The role that ${\beta}$-arrestin 1 plays in gastric cardiac adenocarcinoma (GCA) and its clinicopathologic significance are untouched. Methods: Fifty patients with gastric cardiac adenocarcinoma were retrospectively enrolled and ${\beta}$-arrestin 1 was detected using immunohistochemistry in tissue samples. Results: Nuclear expression of ${\beta}$-arrestin 1 was observed in 78% of GCA samples (39/50) and cytoplasmic expression in 70% (35/50). ${\beta}$-arrestin 1 could be found in both nucleus and cytoplasm of 54% GCA (27/50) or in either of them in 94% (47/50). ${\beta}$-arrestin 1 protein positivity in well/moderately differentiated carcinomas was significantly higher than that in poorly differentiated carcinomas (P=0.005). We found increased expression of ${\beta}$-arrestin 1 in cytoplasm was correlated with lymph nodal metastasis (P=0.002) and pathological lymph nodal staging (P=0.030). We also found ${\beta}$-arrestin 1 to be over-expressed in glandular epithelia cells of mucinous adenocarcinoma, a tumour type associated with an adverse outcome of gastric cardiac adenocarcinoma (P=0.022). Conclusion: ${\beta}$-arrestin 1 is over-expressed in the nucleus and/or cytoplasm of gastric cardiac adenocarcinoma. However, ${\beta}$-arrestin 1 has no relationship with the prognosis of gastric cardiac adenocarcinoma (P>0.05). Our data imply that ${\beta}$-arrestin 1 in cytoplasm may be involved in differentiation and metastasis of gastric cardiac adenocarcinoma.

Study on Relationship between Abdominal Connective Tissue Weakness and Interleukin-1 Gene Polymorphism in Iris Constitution Analysis Study on Relationship between Abdominal Connective Tissue Weakness and Interleukin-1 Gene Polymorphism in Iris Constitution Analysis (홍채 체질 분석에서 복부 결합조직 허약 체질과 인터루킨-1 유전자 다형성과의 상관성 연구)

  • 도금록;황우준;금경수;최성용;김종욱;조재운
    • The Journal of Korean Medicine
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    • v.25 no.1
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    • pp.31-39
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    • 2004
  • Objectives : The purpose of this study is to report the relationship between iridological constitution and interleukin 1 beta (IL-1 $\beta$) gene polymorphism. Methods : Iris constitution were diagnosed by automatic Iris analysis system, Bexel Irina(Korea). The blood was stored at - $20^{\circ}$... until it was ready to be extracted. The genomic DNA was extracted by inorganic procedure. The concentration of DNA was estimated by absorbance at 260 nm. The interleukin-1 beta (IL-1 $\beta$) gene polymorphism was detected by PCR amplification. Results & Conclusions : The author classified 166 individuals according to Iris constitution, and determined IL-1 $\beta$ genotype. The frequencies of Iris constitutions as follows : neurogenic type, 41 (24.7%); abdominal connective tissue weakness type, 53(31.9%); cardio-renal connective tissue weakness type, 50 (30.1%); the others type, 22 (13.3%). Especially, the frequency of abdominal connective tissue weakness type was significantly higher in err genotype than in the remaining constitutions. As a result, The author demonstrated the association among IL-1 $\beta$ genotype, IBD and Iris constitution.

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Tiul1 and TGIF are Involved in Downregulation of $TGF{\beta}1$-induced IgA Isotype Expression

  • Park, Kyoung-Hoon;Nam, Eun-Hee;Seo, Goo-Young;Seo, Su-Ryeon;Kim, Pyeung-Hyeun
    • IMMUNE NETWORK
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    • v.9 no.6
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    • pp.248-254
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    • 2009
  • [ $TGF-{\beta}1$ ]is well known to induce Ig germ-line ${\alpha}$ ($GL{\alpha}$) transcription and subsequent IgA isotype class switching recombination (CSR). Homeodomain protein TG-interacting factor (TGIF) and E3-ubiquitin ligases TGIF interacting ubiquitin ligase 1 (Tiul1) are implicated in the negative regulation of $TGF-{\beta}$ signaling. In the present study, we investigated the roles of Tiul1 and TGIF in $TGF{\beta}1$-induced IgA CSR. We found that over-expression of Tiul1 decreased $TGF{\beta}1$-induced $GL{\alpha}$ promoter activity and strengthened the inhibitory effect of Smad7 on the promoter activity. Likewise, overexpression of TGIF also diminished $GL{\alpha}$ promoter activity and further strengthened the inhibitory effect of Tiul1, suggesting that Tiul1 and TGIF can down-regulate $TGF{\beta}1$-induced $GL{\alpha}$ expression. In parallel, overexpression of Tiul1 decreased the expression of endogenous IgA CSR-predicitive transcripts ($GLT_{\alpha},\;PST_{\alpha},\;and\;CT_{\alpha}$) and $TGF{\beta}1$-induced IgA secretion, but not $GLT_{\gamma3}$ and IgG3 secretion. Here, over-expressed TGIF further strengthened the inhibitory effect of Tiul1. These results suggest that Tiul1 and TGIF act as negatively regulators in $TGF{\beta}1$-induced IgA isotype expression.

Effects of $(1R,9S)-{\beta}-Hydrastine$ hydrochloride on L-DOPA-Induced Cytotoxicity in PC12 cells

  • Yin, Shou-Yu;Lee, Jae-Joon;Kim, Yu-Mi;Jin, Chun-Mei;Yang, Yoo-Jung;Lee, Myung-Koo
    • Natural Product Sciences
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    • v.10 no.3
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    • pp.124-128
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    • 2004
  • Previously, $(1R,9S)-{\beta}-Hydrastine$ hydrochloride has been found to lower dopamine content in PC12 cells (Kim et al., 20001). In this study, the effects of $(1R,9S)-{\beta}-Hydrastine$ hydrochloride on L-DOPA-induced cytotoxicity in PC12 cells were investigated. Treatment with $(1R,9S)-{\beta}-Hydrastine$ hydrochloride at concentrations higher than $500\;{\mu}M$ caused cytotoxicity in PC12 cells. In addition, $(1R,9S)-{\beta}-Hydrastine$ hydrochloride at non-cytotoxic or cytotoxic concentrations significantly enhanced L-DOPA-induced cytotoxicity (L-DOPA concentration, $50\;{\mu}M$). Treatment of PC12 cells with $750\;{\mu}M$ $-1R,9S)-{\beta}-Hydrastine$ hydrochloride and $50\;{\mu}M$ L-DOPA, alone or in combination, also induced cell death via a mechanism which exhibited morphological and biochemical characteristics of apoptosis, including chromatin condensation and membrane blebbing. Exposure of PC12 cells to $(1R,9S)-{\beta}-Hydrastine$ hydrochloride, L-DOPA and $(1R,9S)-{\beta}-Hydrastine$ hydrochloride plus L-DOPA for 48 h resulted in a marked increase in the cell loss and percentage of apoptotic cells compared with exposure for 24 h. These data indicate that $(1R,9S)-{\beta}-Hydrastine$hydrochloride at higher concentration ranges aggravates L-DOPA-induced neurotoxicity cytotoxicity in PC12 cells. Therefore, it is proposed that the long-term L-DOPA therapeutic patients with $(1R,9S)-{\beta}-Hydrastine$ hydrochloride could be checked for the adverse symptoms.

HRTEM Study of Precipitation Behavior in Mg-6 wt%Zn-1 wt%Y Alloy (고분해능 전자현미경을 이용한 Mg-6 wt%Zn-1 wt%Y 합금의 석출거동에 관한 연구)

  • Baek, Sang-Yeol;Lee, Kap-Ho;Kim, Taek-Soo
    • Korean Journal of Materials Research
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    • v.18 no.7
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    • pp.362-366
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    • 2008
  • The precipitation behavior in Mg-6 wt%Zn-1 wt%Y alloy annealed at different temperatures of $200^{\circ}C$ and $400^{\circ}C$ has been characterized by high resolution transmission electron microscope. When the alloy is annealed at $200^{\circ}C$ for 6 hr, the plate- and the rod-shaped ${\beta}_2'$ phases are precipitated in the matrix. The orientation relationship of plate-shaped precipitates with the matrix exhibits a [$11{\bar{2}}0]{\beta}_2$ || [$10{\bar{1}}0$]Mg, $(0001){\beta}_2'$ || (0001)Mg. While the rod-shaped precipitates have two kinds of the orientation relationships with the matrix, i.e. $[11{\bar{2}}0]{\beta}_2'$||[0001] Mg, $(0001){\beta}_2'||(11{\bar{2}}0)$ Mg and $[11{\bar{2}}0]{\beta}_2'$||[0001] Mg, $({\bar{1}}106){\beta}_2'||(10{\bar{1}}0)$ Mg. With increasing annealing time at $200^{\circ}C$ the ${\beta}_1'$ phases are also precipitated in the matrix and the orientation relationship exhibits a $[010]{\beta}_1'$ || [0001]Mg, $(603){\beta}_1'$ || ($01{\bar{1}}0$)Mg between the ${\beta}_1'$ precipitate and the matrix. The icosahedral phases are precipitated in the alloy annealed at $400^{\circ}C$ and exhibit a $[I2]_I$ || [0001]Mg relationship with the matrix.

Saponins from the Roots of Pulsatilla koreana

  • Kang, Sam-Sik
    • Archives of Pharmacal Research
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    • v.12 no.1
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    • pp.42-47
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    • 1989
  • From the roots of Puisatiila koreana, three monodesmosides(pulsatilla saponins A, B and D) and two bisdesmosides(pulsatilla saponins F and H) were isolated. The structure of these saponins have been determined as hederagenin 3-O-${\beta}$-L-rhamnopyranosyl($1{\to}2$)- ${\alpha}$-L-arabinopyranoside(A), hederagenin 3-O-${\beta}$-D-glucopyrano syl($1{\to}4$) - ${\alpha}$-L-arabinopyranoside(B), hederagenin 3-O- ${\alpha}$-L-rhamnopyranosyl ($1{\to}2$)-[${\beta}$-D-glucopyranosyl($1{\to}4$]-${\alpha}$-L-arabinopyranoside(D), 3-O-${\alpha}$-L-rhamnopyranosyl($1{\to}2$)-{${\alpha}$-L-arabinopyranosyl hederagenin 28-O-${\alpha}$-L-rhamnopyrano syl($1{\to}4$)-${\beta}$-D-glucopyrano syl($1{\to}6$)-${\beta}$-D-glucopyranosyI ester (F) and 3-O-${\alpha}$-L-rhamnopyranosyl($1{\to}2$)-[${\beta}$-D-glucopyranosyl($1{\to}4$)]- ${\alpha}$-L-arabinopyranosyl hederagenin 28-O-${\alpha}$-L-lharnnopyranosyl($1{\to}4$)-${\beta}$-D-glucopyranosyl($1{\to}6$)-${\beta}$-D-glucop yranosyl ester(H) on the basis of chemical and spectral studies. Pulsatilla saponin B is the first report of its presence in plants but saponins A, D, F, and H have recently been isolated from the same genus p. cernua.

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