• 생약학회지
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• 제43권1호
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• pp.6-9
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• 2012

The $CH_2Cl_2$ soluble part of the leaves of Helianthus tuberosus L. (Compositae) exhibited a potent cytotoxic activity against the cultured human tumor cell lines including A-549, SK-OV-3, SK-MEL-2, XF498 and HCT-15 in vitro. Bioassaydirected fractionation of the $CH_2Cl_2$ soluble part of this plant led to the isolation of four cytotoxic sesquiterpene lactones having ${\alpha}$-methylene-${\gamma}$-lactone ring in the molecule. On the basis of physical and spectral evidences, their structures were characterized as ${\Delta}^{4,15}$-isoatripliciolide tiglate (1), ${\Delta}^{4,15}$-isoatripliciolide methacrylate (2), budlein A isobutylate (3) and budlein A tiglate (4). The ${\Delta}^{4,15}$-isoatripliciolide tiglate (1) showed the most potent cytotoxic activity ($0.26{\mu}M<ED_{50}<2.16{\mu}M$) against all of the cell lines tested.

• Archives of Pharmacal Research
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• 제20권5호
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• pp.491-495
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• 1997

All fifteen flavonoids (1-15) have been isolated from the roots of Sophora flavescens (Leguminosae) as active principles of the cytotoxic property toward human tumor cell lines such as A549, SK-OV-3, SK-Mel-2, XF498 and HCT15, in vitro. By means of spectral analyses, particularlyby the aid of various two dimensional NMR experiments, all $^1H-NMR$ ad $^{13}C$ -NMR signals of 1-15 were completely assigned, and thus the structures of 1-15 were established unambiguously.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
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• pp.212-212
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• 1994

본 연구소에서 분리하여 항암활성을 측정한바 있는 Sesquiterpene lactone계열의 KR-53170이 in vitro에 비해 in vivo에서 상대적으로 낮은 효력을 보이는데 착안 그 유도체들을 합성함으로써 in vivo stability 및 efficacy를 개선하고자 하였다. 합성된 물질의 in vivo activity는 human tumor cell중에서 A549(폐암), SK-OV-3(난소암1, SK-MEL-2(피부암), XF-498(중추신경계암), HCT-15(직장암)의 5개 암세포를 이용하여 ED$_{50}$($\mu\textrm{g}$/ml )를 측정하였으며 대조물질로는 KR-53170과 Cisplatin이 사용되었다. 그 결과 HR-53170의 terminal methyl ketone이 carboxylic acid로 변환된 CW-251001과 이것의 methyl ester인 CW-251002, ethyl ester인 CW-251003, 그리고 morpheline과 수용성으로 N-methylpiperazine, N-methyl-N'-aminopiperazine, 4-Piperidinopiperidine을 결합시켜서 합성한 CW-251011, CW-251012, CW-251013, CW-251014가 in vitro에서 어느 정도 활성을 유지하였다. 특히 이들중 CW-251001, CW-251012, CW-251013, CW-2s1014는 물에 대한 용해도가 상당히 개선되어 in vivo 활성검색을 위한 후보물질로 고려되었다. 하지만 이들중 CW-251001은 in vivo에서 낮은 농도에서는 활성이 거의 없었으며 놓은 농도에서는 독성을 나타내었다.

• Archives of Pharmacal Research
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• 제20권1호
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• pp.85-87
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• 1997

The activity-guided fractionation upon the MeOH extract of the aerial parts of Sorbaria sorbifolia var. stellipila led to the isolation of two cucurbitacin-compounds, cucurbitacin D and cucurbitacin F, as active principles. Two compounds were shown to exhibit significant cytotoxicity against cultured human tumor cell lines, A-549, SK-OV-3, SK-MEL-2, XF-498, and HCT 15.

• Archives of Pharmacal Research
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• 제21권2호
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• pp.153-156
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• 1998

The crude extract of Saussurea lappa displayed significant lethality to brine shrimp larvae. Investigation of the causative components by bioactivity-directed fractionation resulted in the isolation of three $C_17$-polyene alcohols. Based on various nmr spectral data, these compounds were identified as shikokiols which had been previously isolated from Cirsium nipponicum and/or Centaurea aegyptica. These $C_17$-polyene alcohols exhibited moderate cytotoxicities against the human tumor cell lines, A549, SK-OV-3, SK-MEL-2, XF498, and HCT15.

• 생약학회지
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• 제26권4호
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• pp.323-326
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• 1995

Through bioassay-guided separation of the chemical constituents from the heartwood of Dalbergia odorifera, an 2'-O-methoxyisoliquiritigenin(1) was isolated as cytotoxic principle. 1 showed potent cytotoxic activity against the three kinds of human cancer cell lines (A-549, SK-MEL-2 and SK-OV-3) with similar activity to 5-Fluorouracil.

• 생약학회지
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• 제31권4호
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• pp.401-406
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• 2000

Marine sponges are known to be a source of diverse sterols. In our study on the cytotoxic components of the marine sponge Spirastrella abata, $5{\alpha},8{\alpha}-epidioxy\;{\Delta}^6$ sterols (1-5) and $5{\alpha},8{\alpha}-epidioxy\;{\Delta}^{6,9(11)}$ sterols (6-7) were isolated. The structures were identified based on the analyses of $^1H-NMR,\;^{13)C-NMR$, and MS data. These compounds were assayed for cytotoxicity against 5 human solid tumor cell lines including A549, SK-OV- 3, SK-MEL-2, XF498, and HCT15.

• 생약학회지
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• 제31권4호
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• pp.449-454
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• 2000

In search for plant-derived cytotoxic compounds, it was found that the $CHCl_3$ and EtOAC extracts obtained from the flowers of Paulownia coreana Uyeki (Scrophulariaceae) exhibited significant cytotoxic activity against human tumor cell lines, A549, SK-OV-3, SK-MEL-2, XF498, and HCT15. Activity-guided fractionation on the basis of the inhibitory activity against the growth of human tumor cell lines, in vitro, and repeated column chromatography afforded several cytotoxic compounds from P. coreana. The structures and stereochemistry of these compounds were established, on the basis of analysis of spectra including IR, UV, EI-MS, $^{1}H-NMR,\;^{13}C-NMR$ and some chemical transformations, as Compound PCCl $(2-hydroxy-4(15),11(13)-eudesmadien-8{\beta},12-olide)$, Compound $PCC2(2,3-dihydro-4-hydroxy-1(15),11(13)-xanthadien-8{\beta},12-olide)$, Compound PCE1 (chrysophanol), Compound PCE2 (emodin), Compound PCE3 (physcion). Cytotoxic activity of compounds obtained from P. coreana. on five tumor cells lines was evaluated by procedure of SRB methods.

• 한국응용과학기술학회지
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• 제24권2호
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• pp.109-116
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• 2007

2-Chlorobenzoyl hydrazine refluxed with benzoyl isothiocyanate and phenyl isothiocyanate in ethanol for 3 hours to give benzamide derivative (1) and anilinederivative (2) on yield of 71%and 95%, respectively. Benzamide derivative (1) reacted with ethanolic sodium hydroxide on reflux to afford cyclization product (3), followed by general substitution reaction of two steps to give acetamide (5), and derivatived acetamides 7a-7k, while aniline derivative (2) reacted with ethanolic sodium hydroxide on reflux to afford another cyclization product (4). Thiol (4) reacted with N-phenyl chloroacetamide in the presence of potassim carbonate to give acetamide derivative (6). Compounds 1-7kwere evaluated for their growth inhibition against five cancer cell lines, including human lung carcinoma (A-549), human prostate cancer (DU145), human colon adenocarcinoma (HT-29), human malignant melanoma (SK-MEL-2) and human ovary malignant ascites (SK-OV-3) with sulforhodamine B (SRB) assay. All compounds (1-7k) showed low inhibition activities under 50% on 100M concentration.

• 혜화의학회지
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• 제8권1호
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• pp.131-146
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• 1999

To evaluate the antitumor activity of Kamisagoonjatang(KST), Kami-jihwangtang (KJT) and Kamigoonjajihwangtang(KKJT), studies were done experimentally. The results were obtained as follows: 1. In cytotoxicity against B16-F10, HT1080, SNU, and L1210, con-centration inhibiting cell growth up to below 50% of control was recognized at $10^{-3}g/ml$ of KKJT. 2. In cytotoxicity against A549, SK-OV-3, XF498 and HCT15, concentration inhibiting cell growth up to below 30% of control was over $400{\mu}g/ml$ of KKJT only and also over $200{\mu}g/ml$ against SK-MEL-2. 3. In Inhibitory effect on activity of DNA topoisomerase I, the $IC_{50}$ was shown $200-400{\mu}g/m{\ell}$, of KST, over $400{\mu}g/m{\ell}$ of KJT and $100-200{\mu}g/m{\ell}$ of KKJT. 4. The T/C% was 122.8 in KJT, 127.4 in KST and 158.4 in KKJ-Ttreated group in S-180 bearing ICR mice. 5. In hematological changes in S-180 bearing ICR mice, numbers of WBC were decreased significantly in KJT and KKJT treated groups as compared with control, whereas those of platelet were increased with no significance in all groups as compared with control. From above results it was concluded that KKJT could be usefully applied for the prevention and treatment of cancer.