• Proceedings of the Korean Society of Toxicology Conference
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• 2003.05a
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• pp.77-77
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• 2003

We have previously shown that 2, 3' , 4, 5' -tetramethoxystilbene(TMS), a trans-stilbene analogue, is one of the most potently selective inhibitor of recombinant human cytochrome P450 1B1 in vitro. In the present studies, the effects of TMS on the expression of cytochrome P450 1B1 were investigated in human mammary cell lines such as MCF-7 and MCF-10A. (omitted)

• 한국약용작물학회:학술대회논문집
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• 2007.11a
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• pp.300.1-300.1
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• 2007

• Natural Product Sciences
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• v.15 no.1
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• pp.17-21
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• 2009

Column chromatographic separation of the alcoholic extract from the roots of Berberis amurensis yielded eight phenolic constituents including six lignans, hanultarin (1), (-)-secoisolariciresinol (3), (+)-lyoniresinol (5), (+)-syringaresinol (6), (+)-syringaresinol-O-$\beta$-D-glucopyranoside (7), liriodendrin (8), and two phenylpropanoids, 4-glucosyloxy-3-methoxyphenyl trans-propenoic ethyl ester (2), trans-ferulic acid (4). The structures were determined on the basis of NMR spectroscopic data. All isolated compounds(1-8) were reported for the first time from this source. Compound 1 exhibited moderate cytotoxicity against four human cancer cell lines in vitro using sulforhodamin B bioassay.

• Natural Product Sciences
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• v.12 no.4
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• pp.214-216
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• 2006

Isorhamnetin from the aerial parts of Persicaria thunbergii has been reported to have anti-tumor activity mediated by the inhibition of farnesyl protein transferase. In this study, we investigated the anti-proliferation effects of isorhamnetin on NIH3T3, K-RAS, H-RAS and SW620 cells, and it showed anti-proliferative effects in a dose-dependent manner with $IC_{50}$ value 4.1, 7.9, 20.2, and $22.4{\mu}g/ml$, repectively.

• Natural Product Sciences
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• v.9 no.2
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• pp.109-111
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• 2003

A bioassay-guided fractionation of the active chloroform extracts of the rhizomes of Zingiber cassumunar Roxb. led to the isolation of a potential cytotoxic principle, curcumin (1), along with two inactive compounds, (E)-4-(3',4'- dimethoxyphenyl)but-3-en-1-ol (2) and (E)-4- (3',4'-dimethoxyphenyl)but-3-en-1- yl acetate (3). Curcumin (1) showed a significant cytotoxicity against several human cancer cell lines $(Col2;\;2.30,\;A549;\;12.30,\;SNU638;\;IC_{50}\;18.80\;{\mu}g/ml)$.

• Natural Product Sciences
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• v.17 no.2
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• pp.100-103
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• 2011

Phytochemical study on the ethanol extract of a Crinum species by bioassay-guided fractionation resulted in the isolation of an active principle, which was determined as parthenin (1) on the basis of physicochemical and spectroscopic analyses. This is the first report on the existence of a sesquiterpenoid from Crinum ensifolium. Compound 1 was found to show strong cytotoxic activity against some cancer cell lines and strongly inhibit NF-${\kappa}$B activity with the $IC_{50}$ value of 1.82 ${\mu}M$.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.04a
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• pp.92-92
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• 1993

Point mutations in a highly conserved central region of the HIV-1 integrase protein were analyzed for their effects on viral replication and virion morphogenesis. Conservative amino acid replacements of two amino acid residues invariant un retroviral integrases, D116 and E152 of HIV-1, as well as the highly conserved amino acid S147, completely blocked viral replication in two CD4$\^$＋/ human T cell lines. Mutation of four other highly conserved amino acids in the region had no detectable effect on viral replication, while Mutations at two positions, N117 and Y143, resulted in viruses with a delayed replication phenotype. Characteristic and reproducible defects id virion core structure were observed by electron microscopic analysis of sore of the replication defective integrase point mutants, indicating that mutant integrase proteins can interfere with the process of virion core maturation.

• Archives of Pharmacal Research
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• v.28 no.3
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• pp.290-293
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• 2005

A known monoalkyl glycerol ether, ($\pm$)-1-nonadecyloxy-2,3-propanediol (1) was isolated from the ethyl acetate extract of a soft coral Dendronephthya gigantea as a weakly cytotoxic constituent against four human cancer cell lines, A549, HT-29, HT-1080, and SNU-638. In addition, a known ceramide, (28,3R,4E,8E)-N-hexadecanoyl-2-amino-4,8-octadecadiene-1 ,3-diol (2), was also isolated as an inactive constituent. This is the first report on the isolation of the compounds 1 and 2 from the octocoral, Dendronephthya species.

• Archives of Pharmacal Research
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• v.27 no.5
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• pp.485-494
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• 2004

Thirty-eight 5-arylidene-2(5H)-furanone derivatives possessing halo-, methoxy-, oxo-, dioxo-, and thiophenyl groups as well as anthraquinone and naphthquinone moieties were synthesized, and their cytotoxicity was evaluated against various cancer cell lines. The introduction of halogen atoms or nitro group at aromatic ring of 5-arylidene-2(5H)-furanone was shown to increase the cytotoxicity with 5-(3-nitrobenzylidene )-2(5H)-furanone (21) being the most potent. Among anthracenyl or naphthalenyl derivatives, (E)-5-[2-(1 ,4-dimethoxy-9, 10-dioxo) anthracenyl]-2(5H)-furanone (34) showed the most potent cytotoxic activity.

• YAKHAK HOEJI
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• v.43 no.3
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• pp.385-390
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• 1999

Camptothecin (CPT) has been known to induce apoptosis in various cancer cell lines. To examine the intracellular apoptotic death signal initiated by CPT, we investigated the possible connection between caspase-3 activation and GSH depletion during CPT-induced apoptosis in HL-60 cells. Treatment of cells with $1{\;}{\mu}M$ CPT induced PARP cleavage accompanied by DNA fragmentation. z-VAD-fmk, a caspase-3 inhibitor, blocked the CPT-induced DNA fragmentation. Pretreatment of cells with N-acetylcysteine, a precursor of GSH biosynthesis, failed to inhibit CPT-induced PARP celavage and DNA gragmenatation. No significant changes in GSH depletion is not essential for caspase activation during CPT-induced apoptosis. We also investigated whether CPT-induced apoptosis is associated with changes of the levels of Bax and Bcl-2, two proteins involved in the control of apoptosis. Bcl-2 levels exhibited a late decrease compared with the kinetics of DNA fragmentation, whereas Bax levels increased more rapidly after CPT treatment. These results suggest that Bax plays more important role than Bcl-2 in inducing DNA fragmentation and may function upsteam of proteolytic activation of caspase-3 pathway in CPT-induced apoptosis.