• Archives of Pharmacal Research
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• v.28 no.2
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• pp.169-171
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• 2005

The methanolic extract of the aerial parts of Persicaria thunbergii was found to show inhibitory activity on Farnesyl Protein Transferase (FPTase). Bioassay-guided fractionation of the methanolic extract resulted in the isolation of isorhamnetin, as an inhibitor on FPTase. This compound inhibited FPTase activity in a dose-dependent manner, and the $IC_{50}$ value of isorhamnetin was $37.5\;{\mu}M$.

• Archives of Pharmacal Research
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• v.17 no.6
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• pp.470-475
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• 1994

The butanol extract of paulownia tomentosa stem showed antibacterial activity against staphyl ococcus aureus (SG511, 285 and 503), Streptococcus pyogenes (A308 and A77) and Streptococcus farcium MD8b etc. The most active compound of the extractg was identified to be campneoside I, which had a minimal inhibitory concentration(MIC) of $150{\;}{\mu}g/ml$ against Strptococcus and Staphylococcus species. From such antibacterial activity, the methoxy group of campneoside I was posulated to be the essential element for the antibacterial activity.

• Archives of Pharmacal Research
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• v.29 no.1
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• pp.64-66
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• 2006

The methanolic extract of the aerial parts of Centipeda minima was found to show inhibitory activity on farnesyl protein transferase (FPTase). Bioassay-guided fractionation of the methanolic extract resulted in the isolation of 6-O-angeloylprenolin, as an inhibitor on FPTase. This compound inhibited FPTase activity in a dose-dependent manner, and the $IC_{50}$ value of 6-O-angeloylprenolin was 18.8 ${\mu}M$.

• International Journal of Oral Biology
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• v.35 no.4
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• pp.177-184
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• 2010

In our present study, we investigated the effects of continentalic acid on Streptococcus mutans (S. mutans) biofilm. Methanol extract of Aralia continentalis (A. continentalis) was suspended in water and sequentially partitioned with CHCl3, ethyl acetate (EtOAc), and n-butanol (n-BuOH). The CHCl3 fraction showed the highest activity and an antibacterial compound against S. mutans was isolated from this preparation through various chromatography methods by bioassay guided fractionation. MS, $^1H-NMR$ and $^{13}C-NMR$ analysis showed that the active principle was continentalic acid which was confirmed to show significant inhibitory effects against S. mutans biofilm. These results may provide some scientific rationale for the traditional use these extracts for the treatment of dental diseases.

• Bulletin of the Korean Chemical Society
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• v.32 no.10
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• pp.3566-3570
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• 2011

A series of 2,4,6-tripyridyl pyridines were synthesized, and evaluated for their antitumor cytotoxicity, topoisomerase I and II inhibitory activity. From the eighteen prepared compounds, compounds 10-12 have shown better or similar cytotoxicity against several human cancer cell lines as compared to 2,2':6',2"-terpyridine and doxorubicin. Especially, compound 10 exhibited the most potent cytotoxicity better than positive controls. Structure-activity relationship study indicated that 2,2':6',2"-terpyridine skeleton has an important role in displaying significant cytotoxicity against several human cancer cell lines.

• Bulletin of the Korean Chemical Society
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• v.28 no.1
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• pp.73-76
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• 2007

Prunioside A, isolated from the methanol extract of Spiraea prunifolia var. Simpliciflora's root, is composed of coumaroyl, monoterpene-type, and glucosyl units. The esterase activity of tannase was used to remove the p-coumaroyl and glucopyranosyl groups. The enzymatically hydrolyzed compound was reacted with various acyl chlorides to synthesize its ester derivatives, which showed the inhibitory effects on NO production in murine machrophage?like RAW 264.7 cells stimulated with lipopolysaccharide and interferon-γ.

• YAKHAK HOEJI
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• v.43 no.6
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• pp.782-788
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• 1999

7-Oxocephalosporanate 1 was treated with phosphonium salts 2~4 by Wittig reaction to afford 7-exomethylene cephalosporanates 5~7. They were oxidized to sulfones 8~10 with mCPBA. Deprotecton of benzhydryl 7-exomethylene cephalosporanate with $AlCl_3$ and NaHCO_3$ gave sodium salts of 7-exomethylene cephalosporanates 11~16. The ${\beta}-lactamase$ inhibitory activity of synthesized compounds 11~16 were compared with sulbactam, tazobactam and clavulanic acid against Type I, II, III, IV and TEM-2 $\beta$-lactamase in vitro. Compound 15 showed more potent activity than sulbactam and clavulanic acid against Type III, IV ${\beta}-lactamase$ enzyme.

• The Korean Journal of Physiology and Pharmacology
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• v.10 no.2
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• pp.101-108
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• 2006

The aim of the present study was to elucidate whether gallic acid could modulate the inflammatory allergic reaction and to study its mechanism of action Gallic acid inhibited compound 48/80- or immunoglobulin E (IgE)-induced histamine release from mast cells. The inhibitory effect of gallic acid on the histamine release was mediated by modulation of cAMP and intracellular calcium. Gallic acid decreased the phorbol 12-myristate 13-acetate plus calcium ionophore A23187-stimulated pro-inflammatory cytokine gene expression and production such as TNF- ${\alpha}$ and IL-6 in human mast cells, and the inhibitory effect of gallic acid was on dependent nuclear factor- ${\kappa}$B and p38 mitogen-activated protein kinase. Our findings provide evidence that gallic acid inhibits mast cell-derived inflammatory allergic reaction by blocking histamine release and pro-inflammatory cytokine expression.

• Natural Product Sciences
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• v.13 no.4
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• pp.373-377
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• 2007

Antiscratching behavioral effects of the water extract of two black colored rice (BCR) varieties [Oryza sativa L. cv. Heugjinjubyeo (HJ) and Josaengheugchalbyeo (JH)], major pigment of which is cyanindin 3-glucoside, were investigated. Orally administered BCRs' extracts exhibited potent inhibitory activity against scratching behaviors which were induced by compound 48/80 and histamine. The inhibitory effect of Josaengheugchalbyeo in vivo and in vitro were more potent than those of Heugjinjubyeo. These finding suggest that black colored rice, especially Josaengheugchalbyeo, may inhibit scratching behaviors and anaphylaxis reaction by stabilizing membrane.

• Journal of Physiology & Pathology in Korean Medicine
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• v.19 no.2
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• pp.520-523
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• 2005

(R)-(-)-PGME amide of diterpene acid (2) was assigned the absolute configuration from NMR correlation experiments. The compound (2) was tested for its growth inhibitory effects against tumor cell lines by the MTT method.