• YAKHAK HOEJI
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• v.48 no.2
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• pp.117-121
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• 2004

Ranunculin, a potent cytotoxic component of P. koreana, was synthesized by reacting (s)-(-)-5-(hydroxymethyl)-2(5H)-furanone with 2,3,4,6-tetra-O-acetyl-$\alpha$-D-glucopyranosyl bromide and successive removal of the acetyl protecting group by 0.5 M HCl/MeOH. A new deacetylation process of the intermediate tetraacetylranunculin was deviced giving a yield of 83% of ranunculin. Protoanemonin, the cytotoxic structural moiety of ranunculin, was synthesized by dehydration of (s)-(-)-5-hydroxymethyl-2(5H)-furanone. Ranunculin showed a moderate cytototoxic activity against A-549 (ED$_{50}$=7.53 $\mu\textrm{g}$/$m\ell$), NIH3T (ED$_{50}$=13.6$\mu\textrm{g}$/$m\ell$), and SK-OV-3 (ED$_{50}$=17.5 $\mu\textrm{g}$/$m\ell$). Meanwhile, protoanemonin also exhibited moderate cytotoxicity against A-549 (ED$_{50}$=9.38 $\mu\textrm{g}$/$m\ell$), NIH3T (ED$_{50}$=13.8 $\mu\textrm{g}$/$m\ell$), and SK-OV-3 (ED$_{50}$=15.1 $\mu\textrm{g}$/$m\ell$). It was found that both of the synthetic products showed a potenter cytotoxicity against A-549.ainst A-549.

• Herbal Formula Science
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• v.7 no.1
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• pp.107-120
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• 1999

The purpose of this Study was to investigate effects of KaegiBokryengHwan(KBH) on anti-tumor, immunocytes and nitric oxide(NO). This Study estimated the proliferation of L1210 cell lines, HeLa cell lines, SK-OV3 cell lines, MCF-7 cell lines, balb/c mouse 3T3 cell lines, mouse thymocytes and mouse splenocytes and NO production from peritoneal macrophages in vitro. and estimated the proliferation of L1210 cells, mouse thymocytes and splenocytes and NO production from peritoneal macrophages and body weight in L1210 cells-transplanted mice in vivo. The result were obtained as follow ; 1. KBH inhibited significantly SK-OV3 cell lines in vitro. 2. KBH was accelerate significantly the proliferation of balb/c mouse thymocytes in vitro. 3. KBH increased significantly NO production from peritoneal macrophages in vitro. 4. KBH didn't effect the cytotoxicity of L1210 cells in L1210 cells-transplanted mice. 5. KBH was accelerate the proliferation of splenocytes in L1210 cells-transplanted mice. 6. KBH increased NO production from peritoneal macrophages in L1210 cells-transplanted mice. 7. KBH increased the body weight as comparing with control group in L1210 cells-transplanted mice.

• The Korean Journal of Zoology
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• v.38 no.2
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• pp.204-211
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• 1995

In an effort to develop a new therapeutic strategy for human gene therapy of solid ovarian tumor, we studied the expression of the p53 tumor suppressor Sene as well as regulatory subunits of cyclic AMP (cAMP)-dependent protein kinase in human ovarian carcinoma cells. Four cell lines (2774, Caov-3, SK-OV-3 and OVCAR-3) were selected for the analyses. The p53 transcript and protein were detected only in the 2774 cell line by Northern and Western Bnalysis. In the relatively fast growing cell line, SK-OV-3, the %rope 1 a regulstorv subunit (RIA of CAMP-dependent protein kinase was the highest among the four cell lines. The expression level of $RII\beta$ protein was low in the four cell lines examined. These results maw point to a direction to select the target gene(sl to be employed for gene therapy to control the ovarian cancer.

• Journal of Haehwa Medicine
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• v.10 no.1
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• pp.109-114
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• 2001

To evaluate the antitumor activity of Paridis Rhizoma(PR), studies were done experimentally. The results were obtained as follows: 1. In cytotoxicity against MCF-7, SK-OV-3, HCT15, concentration inhibiting cell growth up to below 50% of control was recognized at $100-200{\mu}g/m{\ell}$ of PR and also against A549, XF498 was recognized at $50-100{\mu}g/m{\ell}$. 2. In Inhibitory effect on activity of DNA topoisomerase I, the $IC_{50}$ was shown $50-100{\mu}g/m{\ell}$ of PR. 3. The concentration inhibiting adhesion of A549 and SK-OV-3 to complex extracellular matrix up to below 50% of control was recognized at $10-100{\mu}g/m{\ell}$ of PR. 4. The T/C% was 137.9 in PR-treated group in S-180 bearing ICR mice. From above results it was concluded that PR could be usefully applied for the prevention and treatment of cancer.

• Archives of Pharmacal Research
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• v.25 no.4
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• pp.416-420
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• 2002

A series of isoindoloquinoline derivatives was synthesized and evaluated in vitro cytotoxicity against four human cancer cell lines (HCT15, SK-OV-3, MDA-MB-468 and T-47D).

• Archives of Pharmacal Research
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• v.28 no.3
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• pp.285-289
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• 2005

Two new sulfated saponins designated as certonardosides P$_{2}$ and I$_{3}$ (1 and 2) were isolated from the brine shrimp active fraction of the MeOH extract of the starfish Certonardoa semiregularis. The structures were determined on the basis of spectral analysis. Compounds 1 and 2 were tested for cytotoxicity against five human tumor cell lines (A549, SK-OV-3, SK-MEL-2, XF498, and HCT15), and compound 1 displayed significant cytotoxicity against the SK-MEL-2 skin cancer cell.

• Biomolecules & Therapeutics
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• v.9 no.3
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• pp.143-155
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• 2001

Many attention has been focused on developing new chemotherapeutic agents for a treatment of cancer from natural products. From Carpesium divaricatum S. et Z. (Compositae), various monoterpenoid compounds were isolated and exhibited mild antitumor activity against human tumor cell lines. These facts prompted us to explore the structure-activity relationship of these compounds. The synthesis of monoterpenoid compound was accomplished by Fries rearrangement, Grignard reaction, elimination, allylic oxidation, esterification and epoxidation as key steps. The results of in vitro cytotoxicity (A549, SK-OV-3, SK-MEL-2, XF498, HCT15) of the synthesised compounds are as follows: First of all, epoxide moiety is prerequisite for cytotoxic activity in diester compound. Any kind of compounds with olefin or diol moiety instead of epoxide ring exhibited poor or mild cytotoxic activity respectively. Of o-acetoxy and isobutoxy epoxy esters, p-sub-stituted phenylacetate compounds exhibited high cytotoxic activities against SK-MEL-2 and HCT15.

• The Journal of Korean Medicine
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• v.23 no.2
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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.

• Proceedings of the Ginseng society Conference
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• 1993.09a
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• pp.132-137
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• 1993

Several Prosapogenins and sapogenins obtained by acid hydrolysis or alkaline cleavage of Korean red ginseng saponins were separated and identified by spectral and physical methods. Some of these degradation products showed the cytotoxic activities against various cancer cell lines, that is, A549, SK - OV - 3, L121O, P388 and K562. The significant difference of activity between stereoisooers was not approved and the activity was inversely proportional to the number of sugars binding to sapogenins. It was clear that diol type prosapogenins and sapogenins were more cytotoxic than triol type ones.

• Archives of Pharmacal Research
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• v.26 no.7
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• pp.521-525
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• 2003

Phytochemical works on the aerial parts of Aster oharai (Compositae) led to the isolation of a new sesquiterpene hydroperoxide, 7$\alpha$-hydroperoxy-3, 11-eudesmadiene (2) and seven known compounds, teucdiol B (1), $\alpha$-spinasterol (3), oleanolic acid (4), $\alpha$-spinasterol 3-Ο-$\beta$-D-glucopyranoside (5), methyl 3,5-di-Ο-caffeoyl quinate (6), 3,5-di-Ο-caffeoylquinic acid (7), 3,4-di-Ο-caffeoylquinic acid (8). The chemical structures of 1-8 were established by chemical and spectroscopic methods. Compound 2 showed cytotoxicity against cultured human tumor cell lines in vitro, SK-OV-3 (ovarian), SK-MEL-2 (skin melanoma), and HCT15 (colon) with $ED_{50}$ values ranging from 3.86-17.21 $\mu$g/mL.