• Title/Summary/Keyword: inhibitory compound

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Alkoxybenzylcyanoguanidine Analogs as a Novel Class of Inhibitors for Restenosis

  • Lee, Sun-Kyung;Yi, Kyu-Yang;Hwang, Sun-Kyung;Suh, Jee-Hee;Lee, Byung-Ho;Yoo, Sung-Eun
    • Bulletin of the Korean Chemical Society
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    • v.25 no.7
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    • pp.1003-1008
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    • 2004
  • A novel class of alkoxybenzylcyanoguanidine analogs as the inhibitors of restenosis was discovered, which showed the inhibitory effects on angiotensin II-induced cell proliferation, determined by $[^3H]$thymidine incorporation method. The compound, N'-(4-nitrophenyl)guanidine analog 19, showed 62% inhibition of $[^3H]$thymidine incorporation at 1 ${\mu}M$ concentration. In addition, the compound 19 inhibited intimal thickening dose-dependently after balloon injury, which suggests the therapeutic potential for restenosis.

A Nitric Oxide Synthesis Inhibitor from the Roots of Gentiana scabra in RAW 264.7 Cells (용담의 RAW 264.7 세포주에서의 Nitric Oxide 생성 저해물질)

  • Kim, Na-Young;Kang, Tai-Hyun;Kim, Do-Hoon;Kim, Youn-Chul
    • Korean Journal of Pharmacognosy
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    • v.30 no.2
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    • pp.173-176
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    • 1999
  • Bioassay-guided fractionation of a $H_2O$ extract of the roots of Gentiana scabra has furnished 5-(hydroxymethyl)-2-furfural (1) as an inhibitory compound for nitric oxide (NO) production in murine macrophage RAW 264.7 cells stimulated with $interferon-{\gamma}$ plus lipopolysaccharide. Compound 1 showed the moderate inhibition of NO production with $IC_{50}$ value of $803\;{\mu}M$.

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A New Antioxidant from the Marine Sponge-derived Fungus Aspergillus versicolor

  • Li, Jian Lin;Lee, Yoon-Mi;Hong, Jong-Ki;Bae, Kyung-Sook;Choi, Jae-Soo;Jung, Jee-H.
    • Natural Product Sciences
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    • v.17 no.1
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    • pp.14-18
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    • 2011
  • A chemical investigation of the marine-derived fungi Aspergillus versicolor led to the isolation of a new aromatic polyketide (1), The structure was elucidated by spectroscopic analysis, and its radical-scavenging activity, reducing power, and inhibitory activity to lipid oxidation were investigated. Those activities of compound 1 were compared with standard antioxidants such as butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), tertiarybutylhydroquinone (TBHQ), and ascorbic acid ($V_C$). Compound 1 showed antioxidant activity comparable to that of BHA, and siginificantly higher than that of BHT.

Rengyolone Inhibits Apoptosis via Etoposide-Induced Caspase Downregulation

  • Kim, Jin-Hee;Lee, Choong-Hwan
    • Journal of Microbiology and Biotechnology
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    • v.19 no.3
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    • pp.286-290
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    • 2009
  • In the course of screening for substances inhibiting apoptosis of U937 human leukemia cells induced by etoposide ($10\;{\mu}g/ml$), Forsythiae fructus, which showed a high level of inhibition, was selected. The regulating compounds were purified from the ethyl acetate extract by silica gel column chromatography and HPLC. The active substance was purified and identified as rengyolone by spectroscopic methods. This compound showed inhibitory activity on caspase-3 induction, a major protease of the apoptosis cascade, with an $IC_{50}$ value of $38.96\;{\mu}M$ after 8 h of etoposide treatment in U937 cells. The expression level of caspase-3 and poly(ADP-ribose) polymerase (PARP) were dose-dependently inhibited by the compound, suggesting that rengyolone inhibits etoposide-induced apoptosis via downregulation of caspases.

A Phospholipase $A_2$ Inhibitor Isolated from Umilicaria esculenta (Umbilicaria esculenta가 생산하는 Depside계 화합물의 구조 및 Phospholipase $A_2$ 저해활성)

  • Kim, Jin-Woo;Song, Kyung-Sik;Chang, Hyeun Wook;Yu, Seung-Hun;Yoo, Ick-Dong
    • Microbiology and Biotechnology Letters
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    • v.23 no.5
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    • pp.526-530
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    • 1995
  • Phospholipase A$_{2}$ (PLA$_{2}$) is lipolytic enzyme that has known to be involved in inflammation. In the course of our screening for antiinflammatory compounds from natural products, a compound having PLA$_{2}$ inhibitory activities was isolated from the methanol extract of Umbilicaria esculenta. The compound was identified as lecanoric acid based on various NMR studies including DEPT, HETERO-COSY and HMBC experiments. Lecanoric acid inhibited human rheumatoid synovial PLA$_{2}$ activity with IC$_{50}$ of 0.17 mM and also exhibited antitumor activity (ED$_{50}$=2.7 $\mu $g/ml) against skin tumor cell line (LOX-IMVI).

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Component Characteristics of Each Extract Prepared by Different Extract Methods from By-products of Glycyrrhizia uralensis (추출 조건을 달리한 감초부산물 추출물의 성분 특성)

  • 강명화;박춘근;차문석;성낙술;정혜경;이제봉
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.30 no.1
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    • pp.138-142
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    • 2001
  • Solid contents, free sugars, phenlic compounds and glycyrrhizin of extracts obtained from by-products of Glycyrrhizia uralensis by three different methods, i.e., shaking, heating, and static methods, were determined. Solid contents of extracts obtained by shaking, heating and static method were 15.6%, 15.0% and 5.3%, respectively. Phenolic compound contents of them were 11.33 mg/100 mL, 11.21 mg/100mL and 10.15 mg/100 mL. Main free sugars in the extracts from the by-products of G. uralensis were fructose, glucose, sucrose, and maltose. Glycyrrhizin content of the extracts from the by-products of G. uralensis were 2.79%, 3.54% and 0.63%, respectively. Extract obtained by the shaking methods had an ability of donating electron to DPPH. The relative antioxidant effects of th extract obtained from the shaking method showed 70% inhibitory effect of peroxidation on egg yolk lecithin.

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STUDIES ON BIOLOGICALLY ACTIVE SUBSTANCES IN NON-SAPONIN FRACTION OF KOREAN RED GINSENG

  • Okuda Hiromichi;Zheng Yinan;Matsuura Yukinaga;Takaku Takeshi;Kameda Kenji
    • Proceedings of the Ginseng society Conference
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    • 1993.09a
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    • pp.110-112
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    • 1993
  • Acidic polysaccharide from Korean red ginseng was found to inhibit pancreatic lipase activity and cause reduction of plasma triglyceride level after oral administration of corn oil emulsion to rats. Thus acidic polysaccharide may reduce plasma triglyceride through its inhibitory action on pancreatic lipase and successive inhibition of intestinal absorption of fat due to reduction of lipolysis. In the course of this experiment, we found an unknown ninhydrin positive substance in Korean red ginseng. The unknown substance was identified to be arginyl-fructosyl glucose(Arg - Fru - Glc). Coment of this new compound was $5.37\%$ in Korean red ginseng powder. Sucrase and maltase activities in mucous layer of rat jejunum were found to be inhibited by Arg-Fru-Glc. Physiological significance of the new compound was discussed based on these experimental results.

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Inhibitory Effects of Actinidia chinensis and Zizyphus jujube on Histamine Release from Rat Peritoneal Mast Cells

  • Yang, Su-Ok;Ji, Geun-Eog
    • Preventive Nutrition and Food Science
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    • v.11 no.2
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    • pp.89-93
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    • 2006
  • Methanol extracts (80%, $10{\mu}g/mL$) of Actinidia chinensis (AC) and Zizyphus jujube(ZJ) inhibited histamine release from rat peritoneal mast cells (RPMCs) induced by compound 48/80. Evaluation of AC and ZJ solvent fractions (chloroform, ethylacetate, butanol and water) revealed that the butanol fraction of AC at $5{\mu}g/mL$ and water fraction of ZJ at $1{\mu}g/mL$ exhibited the highest anti-allergic effects. Combination of the butanol fraction of AC and water fraction of ZJ when combined showed higher inhibition of histamine release than either alone. The levels of cAMP in RPMCs treated with AC and ZJ were significantly increased compared to the compound 48/80 treated control. Our findings suggest that the extracts from AC and ZJ may alleviate immediate hypersensitivity reactions through the increase of cAMP in the mast cells.

Inhibitors of Melanogenesis from Atractylodes rhizomes (백출의 멜라닌 생성 억제 물질)

  • Jung, Min-Hwan;Moon, Chul-Soon;Lim, Young-Hee;Kang, Sang-Jin;Cho, Wan-Goo;Kim, Cheong-Taek
    • Korean Journal of Pharmacognosy
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    • v.36 no.1 s.140
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    • pp.60-63
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    • 2005
  • One sesquiterpenoid was isolated from the methanol extract of Atractylodes rhizomes which has been used as traditional medicine for diuresis and the compound was established as selina-4(14),7(11)-dien-8-one by the spectroscopic methods. The compound$(IC_{50}<10\;ppm)$ has inhibitory effects on melanogenesis in B16 mouse melanoma.

Cholinesterase Inhibitors Isolated from the Fruits Extract of Evodia officinalis (오수유의 Cholinesterase 저해활성 성분)

  • Lee, Ji-Young;Cha, Mi-Ran;Choi, Chun-Whan;Kim, Young-Sup;Lee, Bong-Ho;Ryu, Shi-Yong
    • Korean Journal of Pharmacognosy
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    • v.43 no.2
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    • pp.122-126
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    • 2012
  • The MeOH extract of Evodiae Fructus exhibited a significant inhibition on the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), in a dose dependent manner, respectively. The extensive bioactivity-guided fractionation process with the MeOH extract finally isolated four compounds, as rutaecarpine (1), evodiamine (2), limonin (3) and dehydroevodiamine (4). Among them, compound 2 exhibited specific inhibitory activity on BChE with the $IC_{50}$ values 1.7 ${\mu}g/ml$, whereas compound 4 showed the potent inhibition upon both AChE and BChE.