• Title/Summary/Keyword: 14-3-$3{\beta}$

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Synthesis of Fluorinated New Thebaine Derivatives (불소기가 치환된 새로운 티베인 유도체 합성 -진통작용 검색 및 친화력 검토를 중심으로)

  • Kim, Keun-Jae;Kim, Su-Man
    • YAKHAK HOEJI
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    • v.42 no.3
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    • pp.257-264
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    • 1998
  • 5-Methylthebaine was obtained by treating thebaine with n-butyllithium and methylfluorosulfonate. Hetero Diels-Alder reaction of thebaine and 5-methylthebaine with trifluoroacet aldehyde afforded 14-${\beta}$-(triflu-oro-2-hydroxyethyl)codeine (2) and 14-${\beta}$-(trifluoro-2-hydroxyethyl)-5-methylcodeinone (9). 6-${\alpha}$-OH compound (4) was obtained by employing $CeCl_2$ and $NaBH_4$. After synthesized a derivative substituted for 3-OH (5), using boron tribromied, We synthesized a new derivative that make double bond in C-7, C-8 into epoxode (6), (10). Through inspecting an influence on structure-activity and analgetic action, we are going to examine which opiold acceptor has a selectivity.

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Acylucosyl Sterols from the Roots of Caragana chamlagu (골담초근의 Lipid성분에 관한 연구)

  • Cho, Young-Kyung;Lee, Myung-Whan;Kang, Hyun-Mo;Lee, Han-Koo;Kang, Sam-Sik
    • Korean Journal of Pharmacognosy
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    • v.23 no.1
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    • pp.14-19
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    • 1992
  • A mixture of acylglucosyl sterols together with ${\beta}-sitosterol$, ${\beta}-sitosterol\;3{\beta}-O-glucoside$ and fatty acids was isolated from the roots of Caragana chamlagu as their acetate forms and the structure elucidated by chemical and spectroscopic means. The major acylglucosyl sterol was ${\beta}-sitosteryl\;3-O-[6'-O-oleoyl]-{\beta}-D-glucopyranoside$ while the minor components were $6'-O-palmitoyl-\;and\;6'-O-stearoyl-{\beta}-D-glucosyl$ sitosterol congeners. The isolation and structure elucidation of these acylglucosyl sterols are reported for the first time from the genus Caragana.

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Cytotoxic Ergosterols from Paecilomyces sp. J300

  • Kwon, Hak-Cheol;Zee, Sang-Deuk;Cho, Sae-Yun;Choi, Sang-Un;Lee, Kang-Ro
    • Archives of Pharmacal Research
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    • v.25 no.6
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    • pp.851-855
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    • 2002
  • Seven ergosterol derivatives (1-7) were isolated from silkworm larvae infected with Paecilomyces sp. J300. On the basis of spectroscopic means, their structures have been elucidated as 3$\beta$,5$\alpha$-dihydroxy-ergosta-7,22-diene (1), 5$\alpha$,6$\alpha$-epoxy-(22E,24R)-ergosta-8(14), 22-diene-3$\beta$,7$\alpha$-diol (2), 5$\alpha$,6$\alpha$-epoxy-(22E,24R)-ergosta-8, 22-diene-3$\beta$,7$\alpha$-diol (3), ergosta-4, 6, 8(14), 22-tetraene-3-one (4), ergosterol (5), ergosterol endoperoxide (6), 3$\beta$,5$\alpha$-dihydroxy-6$\beta$-methoxyergosta-7,22-diene (7). Compounds 3~7 showed moderate cytotoxicity against five tumor cells.

Phytochemical Constituents of Schizonepeta tenuifolia Briquet

  • Lee, Il-Kyun;Kim, Min-Ah;Lee, Seung-Young;Hong, Jong-Ki;Lee, Jei-Hyun;Lee, Kang-Ro
    • Natural Product Sciences
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    • v.14 no.2
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    • pp.100-106
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    • 2008
  • Column chromatographic separation of the MeOH extract from the aerial parts of Schizonepeta tenuifolia Briquet led to the isolation of twelve terpenes (1 - 11 and 17), four phenolics (13 - 16) and a hexenyl glucoside (12). Their structures were determined by spectroscopic means to be (-)-pulegone (1), piperitenone (2), p-cymene-3,8-diol (3), schizonepetoside A (4), schizonepetoside C (5), (+)-spatulenol (6), ursolic acid (7), $2{\alpha}$,$3{\alpha}$,$24{\alpha}$,-trihydroxyolean-12en-28oic acid (8), $5{\alpha}$,$8{\alpha}$-epidioxyergosta-6,22-diol-$3{\beta}$-ol (9), stigmast-4-en-3-one (10), ${\beta}-sitosterol$ (11), (Z)-3-hexenyl-1-O-${\beta}$-D-glucopyranoside (12), rosmarinic acid (13), apigenin-7-O-${\beta}$-D-glucopyranoside (14), luteolin-7-O-${\beta}$-D-glucuronopyranoside (15), hesperidin (16) and trans-phytol (17). Compounds 2, 3, 8, 9 and 12 were for the first time isolated from S. tenuifolia Briq.

Nuclear Receptor PPARα Agonist Wy-14,643 Ameliorates Hepatic Cell Death in Hepatic IKKβ-Deficient Mice

  • Kim, Taehyeong;Wahyudi, Lilik Duwi;Gonzalez, Frank J.;Kim, Jung-Hwan
    • Biomolecules & Therapeutics
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    • v.25 no.5
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    • pp.504-510
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    • 2017
  • Inhibitor of nuclear factor kappa-B kinase beta ($IKK{\beta}$) plays a critical role in cell proliferation and inflammation in various cells by activating $NF-{\kappa}B$ signaling. However, the interrelationship between peroxisome proliferator-activated receptor ${\alpha}$ ($PPAR{\alpha}$) and $IKK{\beta}$ in cell proliferation is not clear. In this study, we investigated the possible role of $PPAR{\alpha}$ in the hepatic cell death in the absence of $IKK{\beta}$ gene using liver-specific Ikkb-null ($Ikkb^{F/F-AlbCre}$) mice. To examine the function of $PPAR{\alpha}$ activation in hepatic cell death, wild-type ($Ikkb^{F/F}$) and $Ikkb^{F/F-AlbCre}$ mice were treated with $PPAR{\alpha}$ agonist Wy-14,643 (0.1% w/w chow diet) for two weeks. As a result of Wy-14,643 treatment, apoptotic markers including caspase-3 cleavage, poly (ADP-ribose) polymerase (PARP) cleavage and TUNEL-positive staining were significantly decreased in the $Ikkb^{F/F-AlbCre}$ mice. Surprisingly, Wy-14,643 increased the phosphorylation of p65 and STAT3 in both Ikkb and $Ikkb^{F/F-AlbCre}$ mice. Furthermore, BrdU-positive cells were significantly increased in both groups after treatment with Wy-14,643. Our results suggested that $IKK{\beta}-derived$ hepatic apoptosis could be altered by $PPAR{\alpha}$ activation in conjunction with activation of $NF-{\kappa}B$ and STAT3 signaling.

Effect of Dietary β-1,3/1,6-glucan Supplementation on Growth Performance, Immune Response and Plasma Prostaglandin E2, Growth Hormone and Ghrelin in Weanling Piglets

  • Wang, Zhong;Guo, Yuming;Yuan, Jianmin;Zhang, Bingkun
    • Asian-Australasian Journal of Animal Sciences
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    • v.21 no.5
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    • pp.707-714
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    • 2008
  • The experiment was conducted to evaluate the effect of ${\beta}$-1,3/1,6-glucan on growth performance, immunity and endocrine responses of weanling piglets. One hundred and eighty weanling piglets (Landrace$\times$Large White, $7.20{\pm}0.25kg$ BW and $28{\pm}2$ d of age) were randomly fed 1 of 5 treatment diets containing dietary ${\beta}$-1,3/1,6-glucan supplemented at 0, 25, 50, 100 and 200 mg/kg for 4 wks. Each treatment was replicated in 6 pens containing 6 pigs per pen. On d 14 and 28, body weight gain, feed consumption and feed efficiency were recorded as measures of growth performance. Peripheral blood lymphocyte proliferation and serum immunoglobulin G (IgG) were measured to study the effect of dietary ${\beta}$-1,3/1,6-glucan supplementation on immune function. Plasma prostaglandin E2 (PGE2), growth hormone (GH) and ghrelin were measured to investigate endocrine response to ${\beta}$-1,3/1,6-glucan supplementation. Our results suggest that average daily gain (ADG) and feed efficiency had a quadratic increase trend with dietary ${\beta}$-1,3/1,6-glucan supplementation from d 14 to 28, whereas it had no significant effect on average daily feed intake (ADFI). The treatment group fed with 50 mg/kg dietary ${\beta}$-1,3/1,6-glucan supplementation showed a numerical increase in ghrelin, a similar change trend with ADG and no significant effect on GH. Lymphocyte proliferation indices, serum IgG and plasma PGE2 concentrations varied linearly with dietary supplementation levels of ${\beta}$-1,3/1,6-glucan on d 14. Higher levels of ${\beta}$-1,3/1,6-glucan may have a transient immuno-enhancing effect on the cellular and humoral immune function of weanling piglets via decreased PGE2. Taking into account both immune response and growth performance, the most suitable dietary supplementation level of ${\beta}$-1,3/1,6-glucan is 50 mg/kg for weanling piglets.

The Effect of Ultrasound on $TGF-\beta$ Expression in the Injured Achilles Tendons of Rats (초음파가 흰쥐 아킬레스건 손상부위의 $TGF-\beta$발현에 미치는 영향)

  • Yoon Soo-Jin
    • The Journal of Korean Physical Therapy
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    • v.14 no.3
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    • pp.145-173
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    • 2002
  • This study was performed to investigate the effect of ultrasound irradiation on $TGF-\beta_1$ expression in the surgically injured achilles tendons of rats. The results of this study were as following: 1. The control group (3 days after injury) expressed little immunoreactivity for $TGF-\beta_1$. 2. In the experimental groups, $TGF-\beta_1$ immunoreactivity of group 11(applied US for 3 days) was increased markedly than that of group 1(applied US for 1 day). 3, The experimental group 11(applied US for 3 days) expressed higher immunoreactivity for $TGF-\beta_1$ than control group. These findings suggest that ultrasound irradiation on the injured Achilles tendon may be of benefit such as increasing $TGF-\beta$ release in the inflammatory phase of heal ins process.

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Saponins from the Fructus of Kochia scoparia

  • Whang, Wan-Kyunn;Hahn, Dug-Ryong
    • Archives of Pharmacal Research
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    • v.14 no.2
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    • pp.176-180
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    • 1991
  • Two new triterpenoidal saponins B(1) and C(2) were isolated from the fructus of Kochia scoparia. On the basis of chemico-spectral evidences, the structures of 1 and 2 were elucidated as oleanolic acid 3-O-$\beta$-D-ribopyranosyl-(1$\rightarrow$2)-.betha.-D-glucuronopyranoside and 3-O-$\beta$-D-xylopyranosyl-(1$\rightarrow$3)-$\beta$-D-glucuronopyranosyl-olean-12-en-28-O-$\beta$-D-glucopyranosyl ester, respectively.

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Effects of irradiation on TGF-${\beta}_1$ mRNA expression and calcific nodule formation in MC3T3-E1 osteoblastic cell line (방사선조사가 MC3T3-E1 골모세포주의 TGF-${\beta}_1$ mRNA 발현과 석회화결절 형성에 미치는 영향)

  • Song, Ju-Seop;Kim, Kyoung-A;Koh, Kwang-Joon
    • Imaging Science in Dentistry
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    • v.38 no.3
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    • pp.125-132
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    • 2008
  • Purpose : To investigate the effects of irradiation on transforming growth factor ${\beta}_1$ (TGF-${\beta}_1$) mRNA expression and calcific nodule formation in MC3T3-E1 osteoblastic cell line. Materials and Methods : Cells were cultured in alpha-minimum essential medium ($\alpha$-MEM) supplemented with 10% fetal bovine serum and antibiotics. When the cells reached the level of 70-80% confluence, culture media were changed with $\alpha$-MEM supplemented with 10% FBS, 5 mM $\beta$-glycerol phosphate, and $50\;{\mu}g/mL$ ascorbic acid. Thereafter the cells were irradiated with a single dose of 2, 4, 6, 8 Gy at a dose rate of 1.5 Gy/min. The expression pattern of TGF-${\beta}_1$ mRNA, calcium content and calcific nodule formation were examined on day 3, 7, 14, 21, 28, respectively, after the irradiation. Results : The amount of TGF-${\beta}_1$ mRNA expression decreased significantly on day 7 after irradiation of 4, 6, 8 Gy. It also decreased on day 14 after irradiation of 6, 8 Gy. and decreased on day 21 after irradiation of 8 Gy. The amount of calcium deposition decreased significantly on day 7 after irradiation of 4, 8 Gy (P < 0.01) and showed a decreased tendency on day 14, 21 after irradiation of 4, 6, 8 Gy. The number of calcific nodules was decreased on day 7 after irradiation of 4, 8 Gy. Conclusion: Irradiation with a single dose of 4, 6, 8 Gy influences negatively the bone formation at the molecular level by affecting the TGF-${\beta}_1$ mRNA expression that was associated with proliferation and the production of extracellular matrix in MC3T3-E1 osteoblastic cell line.

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Dexamethasone Downregulates Expressions of 14-3-3β and γ-Isoforms in Mice with Eosinophilic Meningitis Caused by Angiostrongylus cantonensis Infection

  • Tsai, Hung-Chin;Chen, Yu-Hsin;Yen, Chuan-Min;Chung, Li-Yu;Wann, Shue-Ren;Lee, Susan Shin-Jung;Chen, Yao-Shen
    • Parasites, Hosts and Diseases
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    • v.57 no.3
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    • pp.249-256
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    • 2019
  • Steroids are commonly used in patients with eosinophilic meningitis caused by A. cantonensis infections. The mechanism steroids act on eosinophilic meningitis remains unclear. In this mouse experiments, expressions of 14-3-3 isoform ${\beta}$ and ${\gamma}$ proteins significantly increased in the CSF 2-3 weeks after the infection, but not increasedin the dexamethasone-treated group. Expression of 14-3-3 ${\beta}$, ${\gamma}$, ${\varepsilon}$, and ${\theta}$ isoforms increased in brain meninges over the 3-week period after infection and decreased due to dexamethasone treatment. In conclusion, administration of dexamethasone in mice with eosinophilic meningitis decreased expressions of 14-3-3 isoform proteins in the CSF and in brain meninges.