• 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.

• 대한한의학회지
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• 제20권2호
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• pp.128-140
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• 1999

To evaluate the antitumor activity, antimetastatic and immunomodulatory effects of samryongbakchulsankamibang(SBSK) studies were done experimentally, In cytotoxicity against P388, A549. SK-OV-3, B16-F10 and SK-MEL-2. concentration inhibiting cell growth up to below 40% of control was recognized at $10^{-3}g/ml$ of SBSK. In Inhibitory effect on activity of DNA topoisomerase I. the $IC_{50}$ was shown $200-400{\mu}g/ml$ of SBSK. The T/C was 154% in SBSK-treated group in S-180 bearing ICR mice, The concentration inhibiting adhesion of A549 and B16-F10 to complex extracellular matrix up to below 30% of control was recognized at $5{\times}10^{-4}$, $1{\times}10^{-3}\;g/ml$ of SBSK. In pumonary colonization assay with B16-BL/6, a number of colonies in the lungs were decreased significantly in SBSK-treated group as compared with control group, In hematological changes in B16-BL/6 injected C57BL/6, numbers of WBC and platelet were not changed significantly in SBSK-treated groups, In CAM and in vitro neovascularization assay, angiogenesis was inhibited significantly in SBSK-treated group as compared with control group. From above results it was concluded that SBSK could be usefully applied for the prevention and treatment of cancer.

• 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.

• 생약학회지
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• 제41권2호
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• pp.103-107
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• 2010

Extensive phytochemical investigation of the methanol extract from the whole plant of Youngia japonica (Asteraceae) led us to the isolation of a new guaiane-type sesquiterpene (1), together with three related guaianolides, youngiajaponicoside A (2), crepiside H (3) and crepeside E (4). The chemical structure of 1 was elucidated by the aid of spectroscopic analyses including 2D-NMR experiments (COSY, HMBC, HMQC and ROESY). The isolated components (1-4) were evaluated for the inhibitory effect on the proliferation of four cultured human tumor cell lines such as A549, SK-OV-3, SK-MEL-2 and HCT-15, in vitro.

• 혜화의학회지
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• 제8권2호
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• pp.93-106
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• 2000

To evaluate the antitumor activity and antimetastatic effects of Kamicheungyeolhaedog tang(KCHT), studies were done experimentally. The results were obtained as follows: 1. KCHT extracts exhibited a significant cytotoxicity against A549, SK-MEL-2, SK-OV-3, and B16-BL6 cell lines. 2. KCHT extracts showed significant inhibitoty effect on DNA topoisomerase I 3. The T/C% was 145.8% in KCHT treated group in S-180 bearing ICR mice. 4. KCHT extracts exhibited efficient affect adhesive effect of A549, B16-BL6 cell to complex extracellular matrix. 5. In vitro neovascularization assays, angiogenesis was insignificantly inhibited in KCHT treated group as compared with control group. These results suggested that KCHT extracts might be usefully applied for prevention and treatement of cancer.

• 동의생리병리학회지
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• 제16권3호
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• pp.472-478
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• 2002

The purpose of this study was to investigate the effect of Kamigedang-tang(KGDT) water extract on the antitumor and anti metastatic activity. The results were summarized as follows: KGDT extracts exhibited a significant cytotoxicity against P388, SK-MEL-2, SK-OV-3, and B16-F10 cell lines and showed significant inhibitoty effect on DNA topoisomerase I from calf thymus. The T/C% was 122.9% in KGDT treated group in S-180 bearing ICR mice. Also, KGDT extracts exhibited efficient affect adhesive effect of A549 cell to complex extracellular matrix. In CAM assay, KGDT extracts inhibited angiogenesis at 15㎍/egg concentration insignificantly as compared with control. These results suggested that KGDT extracts might be usefully applied for prevention and treatement of cancer.

• 혜화의학회지
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• 제9권1호
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• pp.155-167
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• 2000

To evaluate the antitumor activity and antimetastatic effects of Gobongeerlhobang(GG1B), studies were done experimentally. The results were obtained as follows: 1. GG1B extracts exhibited a significant cytotoxicity against HT1080, A549, SK-MEL-2 and SK-OV-3 cell lines. 2. The T/C% was 120.7% in GG1B treated group in S-180 bearing ICR mice. 3. GG1B extracts exhibited inefficient adhesive effect of A549, B16-BL6 cell to complex extracellular matrix. 4. GG1B extracts showed a significant inhibition of lung metastasis of B16-BL6 cells in C57BL/6. 5. In CAM assays, angiogenesis was insignificantly inhibited in GG1B treated group than control group. These results suggested that GG1B extracts might be usefully applied for prevention and treatment of cancer.

• 혜화의학회지
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• 제5권2호
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• pp.523-533
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• 1997

Ursolic acid(UA) was isolated from Oldenlandiae diffusae Herba, one of the commonly used medicinal herbs for the treatment of cancer. IC50 of UA against cancer cell lines as SNU-1, B16-Fo. SK-OV3, HCT15, XF498, SK-MEL and A549 was $6{\mu}g/ml$, 4$4.4{\mu}g/ml$, $4.5{\mu}g/ml$, $4.6{\mu}g/ml$ and $4.2{\mu}g/ml$ respectively suggesting cytotoxicity against cancer cells. DNA fragmentation was expressed from the concnetration of $5.5{\mu}g/ml$ of UA by agarose electrphoresis. In the observation of morphological changes by phase contrast microscope, SEM and TEM, cell injury and condensation of cytoplasm from nucleus began 4 hr after UA treatment. fragmentaion of nucleus and injury of cell membrane was shown 24 hr after UA treatmeilt with SNU-1 cells. Aurin tricarboxic acid as endonuclease inhibitor. and nicotinamide as poly(ADP-ribose) polymerase inhibitor protected over 50% of cytotoxicity of UA against SNU-1 was at the concentrations of $3{\mu}M$ and $300{\mu}M$ respectively suggesting UA acts on nucleus. These results suggest that UA had antimetastatic effect and induced apoptosis.

• 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.