• Title/Summary/Keyword: acetylation

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Protective Effects of Korean Red Ginseng against Alcohol-induced Hepatosteatosis (알코올에 의해 유발된 지방변성증에서 홍삼의 보호효과)

  • Kim, Sun Ju;Ki, Sung Hwan;Lee, Sangkyu
    • Journal of Life Science
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    • v.25 no.3
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    • pp.317-322
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    • 2015
  • Alcohol-induced fatty liver (steatosis) results from excessive generation of reducing equivalents by ethanol metabolism. Generally, chronic ethanol treatment causes hepatosteatosis by regulating sterol regulatory element-binding protein 1c (SREBP-1c), which increases the synthesis of hepatic lipids. The effect of ethanol on SREBP-1c is mediated through mammalian sirtuin-1 (SIRT-1), a NAD+-dependent protein deacetylase that regulates hepatic lipid metabolism. Ginseng is a widely used herbal medicine that is used in Asia for its anti-diabetes and anti-obesity effects. The pharmacological and therapeutic effects of ginseng are primarily produced by bioactive constituents known as ginsenosides. Here, we examined the regulatory effects of Korean red ginseng (KRG) extracts on SREBP-1c and SIRT-1 on lipid homeostasis in AML-12 mouse hepatocytes. AML-12 cells were treated with ethanol and/or KRG extracts (0 - 1,000 μg/ml). Lipid droplets were assayed using Oil red O staining, and western blotting was used to measure SIRT-1 and SREBP-1 expression. Treatment with KRG extracts restored SIRT-1 expression and reduced SREBP-1c expression in ethanol-treated cells. We also showed that KRG extract and ginsenosides Rb2 and Rd significantly decreased SREBP-1 acetylation in ethanol-treated cells. These results show that treatment with KRG extract and its active ginsenoside constituents Rb2 and Rd protected against alcohol-related hepatosteatosis via regulation of SIRT-1 and downstream acetylation of SREBP-1c, which altered hepatic lipid metabolism.

Regulation of Histone Acetylation and Methylation of the p11 Gene in the Hippocampus of Chronic Unpredictable Stress-induced Depressive Mice (장기간 예측 불가능한 스트레스를 받은 마우스 해마에서 p11 유전자의 히스톤 아세틸화 및 메틸화의 조절)

  • Seo, Mi Kyoung;Seog, Dae-Hyun;Park, Sung Woo
    • Journal of Life Science
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    • v.31 no.11
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    • pp.995-1003
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    • 2021
  • Chromatin remodeling regulates gene expression through epigenetic mechanisms. Aberrations in histone modification have been associated with depression-like behaviors in animal models. Additionally, growing evidence also indicates that epigenetic modification is associated with depression. p11 (S100A10) has been implicated in the pathophysiology of depression both in human and rodent models. In the present study, we investigated alterations in histone acetylation and methylation at the promoter of the p11 gene in the hippocampus of mice subjected to chronic unpredictable stress (CUS). C57BL/6 mice were exposed to CUS daily for 3 weeks. Depression-like behaviors were measured with the forced swimming test (FST). The levels of hippocampal p11 expression were analyzed by quantitative real-time polymerase chain reaction (PCR) and Western blotting. The levels of acetylated and methylated histone H3 at the promoter of p11 were measured by chromatin immunoprecipitation followed by real-time PCR. CUS-exposed mice displayed depression-like behaviors with prolonged immobility in FST. CUS led to significant decreases in the expression of p11 at both protein and mRNA levels. Meanwhile, there was a decrease in histone H3 acetylation (Ac-H3) and H3-K4 trimethylation (H3K4met3) and an increase in H3-K27 trimethylation (H3K27met3) at the p11 promoter. These results indicate that chronic stress causes the epigenetic suppression of p11 expression in the hippocampus.

Studies on 4-Aminosalicylic Acid Derivatives (II). Synthesis of 2-Ethoxy-4-acetamidobenzamide (4-Aminosalicylic Acid 유도체의 합성연구(II) 2-Ethoxy-4-acetamidobenzamide의 합성)

  • 이남순;유서홍
    • YAKHAK HOEJI
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    • v.19 no.2
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    • pp.96-100
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    • 1975
  • 2-Ethoxy-4-acetamidobenzoate (III) was synthesized by ethylation of N-formyl compound obtained with formylation of methyl 4-aminosalicylate and 2-ethoxy-4-acetamidobenzamide (VIII) was synthesized by ethylation of 4-acetamidosalicylamide (VII) formed by reacting methyl 4-acetamido-2-acetoxy benzoate with concentrated ammonia water under pressure. 2-Ethoxy-4-acetamido benzamide (VIII) was also synthesized by acetylation of 2-ethoxy-4-aminobenzamide (VI) obtained by pressure eraction of methyl 2-ethoxy-4-formylamido-benzoate (I) with concentrated ammonia water.

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Syntheses of Novel 10-Oxodaunomycinone Derivatives (새로운 10-옥소다우노마이시논 유도체의 합성)

  • 노영쇠;김선자;조인호;신홍식
    • YAKHAK HOEJI
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    • v.43 no.1
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    • pp.11-15
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    • 1999
  • A brief route for regiospecific synthesis of novel 10-Oxodaunomycinone Derivatives (10a, b) is described. Dimethoxy-l-tetralone 4 was converted to acetyl tetralone (5a, b) which was oxidized with oxygen to obtain cis-diol compound (8a, b). The construction of (10a, b) was completed by the condensation of phthaloyl dichloride 9 with cis-diol (8a, b)

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Functionalization of Calix[4]arene with Hydroxyalkyl Groups at Upper Rim

  • Kyung Lan Hwang;Si-Hyun Ham;Kwang Hyun No
    • Bulletin of the Korean Chemical Society
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    • v.14 no.1
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    • pp.79-81
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    • 1993
  • Synthetic routes are described for the introduction of hydroxyalkyl groups to the upper rim of calix[4]arene. Treatment of p-bromocalix[4]arene methyl ether 3 with n-BuLi followed by para-formaldehyde produced p-hydroxymethylcalix[4]arene methyl ether 4 in 60% yield. p-Acetylcalix[4]arene methyl ether 7, obtained by Friedel-Crafts acetylation of calix[4]arene methyl ether 6, was reduced with NaBH4 to produce p-(1-hydroxy ethyl)calix[4]arene methyl ether 8 in 67% yield.

Studies on the Consituents of Firmiana platanifolia Schott et Endell(1) (벽오동 firmiana platanifolia의 성분연구 (I))

  • 김재완;김학성;정우태;박해자
    • YAKHAK HOEJI
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    • v.13 no.2_3
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    • pp.76-79
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    • 1969
  • A colorless needle crystlline substance, m.p. 170-$171^{\circ}C$ was obtained from the bark of Firmiana platanifolia in 4% yield. The acetylation derivative of this compound shows m.p. 163--$164^{\circ}C$. Through pharmacological screening tests, it was found that the original substance has an augmented contractility for isolated frog muscle in doses of 2.5$\times$10$^{-4}$ - 1$\times$10$^{-3}$g/ml.

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Designing of Antiepileptic Ligands by Esterification and Acetylation of Dipeptides

  • Vishwakarma, K.K.;Saraf, S.K.;Uppadhyay, R.K.;Kohli, D.V.
    • Archives of Pharmacal Research
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    • v.15 no.3
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    • pp.204-207
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    • 1992
  • Glycylglycine, alanylalanine and alanylglycine were synthesized, their free carboxylic and amino groups were converted to methyl esters of N-acetylglycyglycine, N-acetylalanylglycine and N-acetylalanylalanine. The synthesized compounds were evaluated for antiepileptic activity, plasmaprotein binding, $TD_{50}$ and potentiating effect of phenobarbitone sodium.

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