• BMB Reports
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• v.31 no.6
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• pp.560-564
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• 1998

Echinomycin-7 is an echinomycin derivative, Smethylated sulfonium perchlorate of echinomycin. We studied the in vitro cytotoxicity and in vivo antitumor activity of echinomycin-7 against P388 leukemia cells and compared the results with echinomycin. With respect to the cytotoxic effects, echinomycin-7 had cell line-dependent $IC_{50}$ values while echinomycin had similar values to several tumor cell lines. Also, in vivo antitumor activities were observed in tumor-bearing mice treated with both agents, which showed that echinomycin-7 had a broad therapeutic dose range. We also observed the apoptosis on leukemia cells treated with echinomycin-7 which exihibited the ladder pattern of DNA on electrophoresis. In addition to apoptosis, echinomycin-7 arrested $G_1/S$ phases of the cell cycle at the same time. We then examined the signaling pathway of echinomycin-7-induced apoptosis and showed that ERK of the MAP kinase family was activated and translocated into the nucleus by echinomycin-7 stimulation. This study suggests that echinomycin-7 acts as an antitumor agent through in vitro cytotoxicity and has in vivo antitumor activity against leukemia cells, and that the echinomycin-7- induced apoptosis might involve signal transduction via MAP kinases.

• Archives of Pharmacal Research
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• v.25 no.6
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• pp.781-785
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• 2002

A series of pyrazoloxyphenyl benzoyl urea derivatives was designed and synthesized for cytotoxic evaluation as potential antitumor agents. The synthetic compounds were evaluated for in vitro cytotoxicity against five human tumor cell lines, including A-549, SKOV-3, SK-MEL-2, XF-498 and HCT-15. Among others, compound 11 exhibited 50∼100 times greater antitumor activities than the commercial product, Cisplatin.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1998.11a
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• pp.56-61
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• 1998

For the screening of bioactive natural products, the benzene or methanol extracts from 93 medicinal plants of Korea were prepared, and tested for the cytotoxicity against L1210 cells and for the antitumor action (Bae et al., 1992 and 1996). Of 93 extracts tested, 6 samples showed a cytotoxicity in both benzene and methanol extract, 39 samples in benzene and 13 samples in methanol extract. The benzene extract of the root of Scutellaria indica L., Sophora fIavescens Solander ex Aiton, Carpesium abrotanoides L., Gymnaster koraiensis (Nakai) Kitamura, Pyrola japonica Klenze, and Forsythiae Fructus showed a potent cytotoxic activity. This observation led to isolate active cytotoxic components, some of which demonstrated some antitumor action. In addition, the structure-activity relationship was discussed.

• Archives of Pharmacal Research
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• v.25 no.4
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• pp.493-499
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• 2002

We investigated the antitumor activity of oregonin, a diarylheptanoid derivative purified from Alnus hirsuta Turcz, Betulaceae. Oregonin is a potential novel immunomodulator, which augments the activation of natural killer (NK) cells, and thereby leads to a powerful antitumor activity. To evaluate the cytotoxicity of oregonin against tumor cells, we examined the effectiveness of NK cells and determined that oregonin could increase NK cell cytotoxicity. This was confirmed by MTT assay. In addition, the survival time of C57BL/6 mice were measured by inoculating 816-F10 melanoma cells to mice via intra muscular (i.m.) injection. Oregonin treatment after 10 hours of inoculation at 10 mg/kg dosage showed a significant extension of survival time by up to 51.32%, when compared to the control group. Moreover, oregonin significantly reduced the incidence of pulmonary metastasis, which may be developed from 816-F10 melanoma cells. These findings suggest that oregon in may be classified as a new and novel immunomodulator due to its potential antitumor activity.

• Korean Journal of Plant Resources
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• v.4 no.1
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• pp.17-22
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• 1991

Codonopsis lanceolata and C.pilosula medicinal plants were subjected to preliminary antitumor screening test with Sarcoma 180 ascites and screning on V-79 cell. This ex-periments Iwere conducted in accordance with the Total packed cell Volume methodand Cytotoxicity method .

• 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).

• Korean Journal of Pharmacognosy
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• v.13 no.2
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• pp.55-61
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• 1982

Thirtyfour species of Korean medicinal plants which have been frequently used in oriental herb prescriptions were evaluated on their cytotoxicity and potential antitumor activities against AC glioma(9 ASK) in vitro. Dose of $100{\mu}g/ml$ of plant extracts appeared to exhibit slight cytotoxicity. Seven plant extracts, Aralia continentalis(Araliaceae), Lycium chinensis(Solanaceae), Epimedium koreanum(Berberidaceae), Platyodon grandiflorium(Campanulaceae), Pleuropterus multiflorus(Polygonaceae), Rheum undulatun(Polygonaceae) and Scutellaria baicalensis(Laminaceae), exhibited significant reversal$(51{\sim}90%)$ of astrocyte formation into original neuroglial cells' morphology through the prescreen tests.

• YAKHAK HOEJI
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• v.38 no.6
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• pp.627-636
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• 1994

Several Pt(II) and Pt(IV) complexes of N,N'-bis(2-hydroxyethyl)ethylenediamine(2-HEen) and N,N'-bis(2-chloroethyl) ethylenediamine(2-CEen) as carrier ligand were prepared. Water soluble Pt complexes were also synthesized by modification of leaving groups. The cytotoxicity of these compounds against leukemia L1210 and P388 cell in vitro were examined. The Pt complexes containing 2-CEen showed more effective cytotoxicity than those containing 2-HEen. Through the nephrotoxicity tests on the primary cultured proximal tubular cells of rabbit kidney and human kidney cells in vitro, Pt complexes with 2-CEen showed higher than those with 2-HEen which were consistent with cytotoxicity but showed very low nephrotoxicity compared with cisplatin. Also the values of BUN and creatinine in serum of Pt complexes were reduced remarkably compared with cisplatin, therefore it can be concluded that new Pt complexes seems to have much lower nephrotoxicity than cisplatin.

• Journal of Haehwa Medicine
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• v.5 no.2
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• pp.503-507
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• 1997

The cytotoxicity-guided fractionation of the roots of Sophora flavescens (Leguminosae) extracts led to the isolation of fifteen active principles 1~15, responsible for the cytotoxicity against five kinds of cultured human tumor cell lines, i.e., A549(non small cell lung), SK-OV-3(ovary), SK-MEL-2(skin), XF498(central nerve system) and HCT-15(colon), evaluated by SRB method in vitro. Compounds 2~14 were classified as unusual flavonoid occurred exclusively in this species and the proliferation of each examined tumor cells were significantly inhibited during the continuous exposure to compounds 1~15 for 48 hours, respectively.

• Biomolecules & Therapeutics
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• v.5 no.2
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• pp.215-221
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• 1997

In an effort to screen new selective antitumor agents from the broth of soil microorganism, cytotoxicity oriented screening was performed against tumor cells and 3 compounds (Compound 1, 2 and 3) were isolated from Sreptomyces parvullus ISP 5048 and their chemical structures were determined. Among these compounds, Compound 2 showed the highest cytotoxicity against P388Dl and L1210. While the $IC_{50}$/ values of compound 2 against P388Dl and L1210 were 0.073$\mu$g/ml and 0.07$\mu$g/ml, respectively, and the $IC_{50}$/ value of Compound 3 was 0.17$\mu$g/ml against human lung cancer cells, A549, the cytotoxicity of Compound 2 and 3 against normal cell line, Vero E6 cell was about 4- and 8-fold lower than that of adriamycin. Based on the chemical analysis data, Compound 3 was octacosamicine A, a known antibiotic, which was reported by Dobasih et al. (1988). Taken together the results demonstrated that Compound 2 and Compound 3 has the possibility to be developed as antitumor agent because of its potent cytotoxicity as well as high selectivity against various cancer cell lines.