• Bulletin of the Korean Chemical Society
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• 제32권1호
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• pp.303-306
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• 2011

• Proceedings of the PSK Conference
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.422.1-422.1
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• 2002

This study examined the pharmacokinetic disposition of SJ-8029. a novel anticancer agent possessing microtubule and topoisomerase inhibiting activities. in mice. rats. rabbits and dogs after i.v. administration. The serum concentration-time curves of SJ-8029 were best described by tri-exponential equations in all these animal species. The mean CI. $V_{ss}$ and $t_{1/2}$ were 0.3 L/h. 0.1 Land 63.2 min in mice. 1.5 L/h. 1.6 Land 247.7 min in rats. 13.8 L/h. 39.6 Land 245.9 min in rabbits. and 29.2 L/h. 44.6 Land 117.4 min in dogs. respectively. (omitted)

• Proceedings of the PSK Conference
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• 대한약학회 2001년도 Proceedings of International Convention of the Pharmaceutical Society of Korea
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• pp.254.1-254.1
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• 2001

• The Journal of Korean Medicine
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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.

• Journal of Physiology & Pathology in Korean Medicine
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• 제16권4호
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• pp.667-673
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• 2002

The purpose of this study was to investigate the effect of Kamisamchulsamja-tang (KSST) water extract on the antitumor activity. The results were summarized as follows: KSST extract exhibited a weak cytotoxicity against HT1080, A549, SK-OV-3, B16-F10 and SK-MEL-2 cells. KSST extract showed a inhibitoty effect on DNA topoisomerase I from calf thymus in a dose-dependent manner. Also, KSST extract showed antiadhesive effect on HT1080 cells but didn't showed on A549 cells to complex extracellular matrix. In pumonary colonization assay, a number of colonies in the lungs were decreased significantly in KSST treated group as compared with control group. In vitro neovascularization assays, angiogenesis was significantly inhibited in KSST treated group than control group. In CAM assay, KSST extract inhibited angiogenesis significantly at 15㎍/egg concentration as compared with control. From the above results it was concluded that KSST showed antitumor effect through the antimetastatic effect. So it is expected to be clinically helpful on the prevention of metastasis of cancer.

• Archives of Pharmacal Research
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• 제27권8호
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• pp.829-833
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• 2004

The bioactivity-guided fractionation of the methylene chloride extract of the sclerotium of Poria cocos led to the isolation of (S)-(＋)-turmerone (1), ergosterol peroxide (2), polyporenic acid C (3), dehydropachymic acid (4), pachymic acid (5), and tumulosic acid (6). Compounds 4-6 exhibited moderate cytotoxicities, with $IC_{50}$ values of 20.5, 29.1, and $10.4{\;}\mu\textrm{m}$, respectively, against a human colon carcinoma cell line. However, 3-6 not only showed inhibitory activities as potent as etoposide used as a positive control on DNA topoisomerase II (36.1, 36.2, 43.9 and 66.7％ inhibition at a concentration of $20{\;}\mu\textrm{m}$, respectively), but also inhibition of DNA topoisomerase I (55.8, 60.7, 43.5, and 83.3％ inhibition at a concentration of $100{\;}\mu\textrm{m}$, respec-tively).

• The Journal of Korean Medicine
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• 제22권2호
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• pp.22-30
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• 2001

This study was attempted to investigate the anti-tumor and anti-metastatic effects of Sobokchukeotang(SBCT) and Kamisobokchukeotang(KSBCT). Cytotoxicity against various cancer cell lines, anti-adhesion, pulmonary colonization, anti-angiogenesis, and T/C% were evaluated. SBCT and KSBCT exhibited no cytotoxicity against HT-1080, A549, SK-OV-3, B16-F10 and SK-Mel-2 cell lines. In inhibitory effect on DNA topoisomerase I, the $IC_{50S}$ were shown $250-500{\;}\mu\textrm{g}/ml$ of SBCT and $62.5-125{\;}\mu\textrm{g}/ml$ of KSBCT respectively. In the in vivo experiments, SBCT(135.98%) and KSBCT(151.92%) apparently increased the life span of mice bearing sarcoma-180. KSBCT significantly inhibited the adhesion of HT-1080 to complex extracellular matrix in a dose-dependent manner in contrast to SBCT. In pulmonary colonization assay by B16-F10, a number of colonies in the lungs were decreased more significantly in KSBCT group than those in SBCT group. In vitro neovascularization and CAM assay, angiogenesis was more significantly inhibited in KSBCT-treated group than in SBCT- treated group. Above results suggests that KSBCT is more effectively applied to prevention and treatment of cancer than SBCT.

• Journal of Physiology & Pathology in Korean Medicine
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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.

• Bulletin of the Korean Chemical Society
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• 제30권7호
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• pp.1463-1469
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• 2009

Eleven novel oxiranyl and thiiranyl phenolic compounds were synthesized as potential antitumor agents using epichlorohydrin and epithiohydrin in the presence of $K_2CO_3$. Cytotoxicities were found in range of I$C_{50}$ values of 2.5-14.8 $\mu$M, which was partially attributed to topoisomerase II inhibition. Bis-thiiranyl anthraquinone analog, 19 showed more cytotoxicity against MDA-MB-231 (breast cancer cell) and PC3 (prostate cancer cell) after 24 and/or 48 h and more potent topoisomerase II inhibitory activity than etoposide.

• The Journal of Korean Medicine
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• 제23권2호
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• pp.211-224
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• 2002

Background and Objective : In order to investigate the effects of Gilgyunglwedok-tang (GRT) on antitumor activity and antimetastatic activity, studies were done experimentally. Materials and Methods : Experimental studies were perfonned for the cytotoxic effect on BALB/c mouse lung fibroblast cells, the proliferating effect of splenic lymphocyte, the expression of CD3e/CD4, CD3e/CD8, and B220 in peripheral blood mononuclear cells (PBMCs), the cytotoxic effect on A549, SK-OV-3, SK-MEL-2, MCF-7 cells, the inhibitory effect on the activity of DNA topoisomerase I, the T/C% in ICR mice bearing S-180, the inhibitory effect of Cell adhesive of A549 Cells and SK-OY-3 Cells to complex extracellular matrix, the inhibitory effect on lung colonies, the change of lung tissue, the antiangiogenic activity, and the effect on MMP-2 and MMP-9 gene expression in the RT1080 cell line. Results and Conclusion : The results were obtained as follows : 1. In the cytotoxic effect on BALB/C mouse lung fibroblast Cell, GHT didn't show the significant cytotoxic effect on BALB/C mouse lung fibroblast cell compared to the control group. 2. In thymidine uptake assay, GHT showed the significant proliferating effect of splenic lymphocyte in proportion to the concentration. 3. In the expression of CD3e/CD4, CD3e/CD8, and B220 in peripheral blood mononuclea cells (PBMCs) of mice, GRT had no significant change to the normal group in CD4. However, GRT showed an increase to the normal group in CD8 and GHT in the only $1\mu\textrm{g}/ml$ category showed an increase to the normal group in B220. 4. In the cytotoxic effect of GRT on A549, SK-OY-3, SK-MEL-2 and MCF-7 cells, there was no significant cytotoxic effect compared to the control group. 5. In the inhibitory effect on the activity of DNA topoisomerase I, GHT in the $10\mu\textrm{g}/ml$ category showed the inhibitory effect on the activity of DNA topoisomerase I in proportion to the concentration. 6. In the T/C% in ICRmice bearing S-180, GHTtreated group showed 123.7% of T/C% compared to the control group. 7. In the inhibitory effect of cell adhesive of A549 Cells and SK-OV-3 Cells to complex extracellular matrix, GRT in the only $100\mu\textrm{g}/ml$ category showed the significant inhibitory effect compared to the control group. 8. In the inhibitory effect on lung colonies, GHT showed the significant inhibitory effect on lung colonies compared to the control group. 9. In the change of lung tissue, GHT showed a significant decrease of lung cancer growth, interalveolar fibrosis and hyaline material compared to the control group. In the development of lymphocyte around lung cancer cells and lung parenchymal, GHT showed the significant inducement efficacy compared to the control group. 10. In CAM assay, the antiangiogenic activity of GHT showed 30%. 11. In the effect on MMP-2 and MMP-9 gene expression in the RT1080 cell line, GHT had no significant inhibitory effect on MMP-2 and MMP-9 gene expression compared to the control group. According to the above results, it could be suggested that GHT has an antitumor activity and antimetastatic activity.