• Toxicological Research
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• v.4 no.2
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• pp.95-105
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• 1988

The effects of polyacetylenes on living membrances, rat erythrocyte and murine leukemic L1210 cell as well as artificial lipid bilayer were determined to investigate the cytotoxic mechanism of polyacetylenes against cancer cell lines. As results, panaxydol and panaxynol caused erythrocyte hemolysis dose-dependently while panaxytriol had no lysis. For liposomes composed of phosphatidyl choline (PC) and phosphatidic acid(PA), all three polyacetylenes supressed the osmotic behavior at the same degree.

• Archives of Pharmacal Research
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• v.8 no.3
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• pp.187-190
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• 1985

A cytotoxic coumarin against L1210 cell was isolated from the unripe fruit of Poncirus trifoliata ($ED_{5}$) = 10.2 $\mu$ g/ml. Its structure was identified as aurapten, 7-geranyloxycoumarin. Hydrolysis of the substance gave umbelliferone and geraniol. Only geraniol showed the cytotoxic activity ($ED_{53}$ = 6.5 $\mu$g/ml) while umbelliferone and its methyl or allyl derivatives were not active.

• Archives of Pharmacal Research
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• v.19 no.6
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• pp.543-550
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• 1996

Analogues of $2(S)-5, 2^{l}, 5^{l}$-trihydroxy-7, 8-dimethoxyflavanone, a naturally-occurring compound, which had been reported to have potent antitumor activity, were synthesized and examined for the cytotoxicity against three cancer cell lines. Among the intermediate chalcones and synthetic 5-hydroxy-7, 8-dimethoxyflavanone analogues, $({\pm})2^{l}, 5^{l}-dibenzyloxy-5, 7, 8-trimethoxyflavanone$ exhibited about 2-8 times stronger activity than $2(S)-5, 2^{l}, 5^{l}$-trihydroxy-7, 8-dimethoxyflavanone against L1210, K562 and A549 cancer cell lines. In the structure-activity relationship, it is suggested that among analogues of 5-hydroxy-7, 8-dimethoxyflavanone, the existence of two oxygenated groups of para-relation at $C-2^{I} and C-5^{I}$ positions on flavanone B-ring, may be necessary to exhibit effective cytotoxic activity.

• Korean Journal of Pharmacognosy
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• v.31 no.1
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• pp.51-56
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• 2000

This study was carried out to evaluate cytotoxic effects of the roots of Sophora flavescens Ait. extracts on murine leukemia tumor cells lines $(P388D_1\;and\;L1210)$. Disruptions in cell organelles were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. The comparison of $IC_{50}$ values of the ethyl acetate of Sophora flavescens Ait. extract in leukemia cell lines showed that their susceptibility to these extracts decreased in the following order : Adriamycin>Fr.4>Fr.5>Fr.3>Fr.1>Fr.2 by the MTT assay. These results suggest that the fraction 4 of the ethyl acetate soluble extract of Sophora flavescens Ait. may be a valuable choice for the studies on the treatment of murine leukemia cell lines.

• Microbiology and Biotechnology Letters
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• v.10 no.1
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• pp.53-58
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• 1982

In order to obtain anticancer substances from natural products, extracts of dry herbs, which have long been used to treat cancer or canter-like diseases in oriental countries, were screened. Extracts were made with hot water and/or organic solvents. With the extracts we treated murine leukemic L1210 cells growing in Fischer's medium. After 48 hours of incubation, cells were counted and concentrations of dry extracts to achieve 50 percent inhibition of the control growth, ED$_{50}$ values, were determined. Among the 38 species of medicinal plants tested, water extracts of six species showed ED$_{50}$ values of substantially low. Further extraction with organic solvents could reduce their ED$_{50}$ values within the range of the NCI quality control limit. The promising species as potential sources of anti-cancer substances included Cinnamomum cassia, Citrus trifoliata, Coptis japonica, Panax ginseng, Phellodendron amurense, and Scutellaria baikalensis.

• Archives of Pharmacal Research
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• v.27 no.9
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• pp.893-900
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• 2004

2- or 6-Substituted BZT-N derivatives were synthesized, and their cytotoxic activity against can-cer L1210 and SNU-1 cells was examined. The antitumor action was also assessed in mice bearing S-180 cells in peritoneal cavity. In a comparison, it was found that 6-substituted BZT-N derivatives exhibited higher potencies in both bioactivities than 2-substituted BZT-N derivatives against L1210 cells in in vitro and S-180 in vitro tests exception of compound 36. Interestingly, it was observed that 2-substituted compound 36, which has methyl group at RI position, exhib-ited a better antitumor activity than 6-substituted compounds against L1210 and SNU-1 in vitro. The EDso value of 2-substituted compound 36 against L1210 was found to be comparable to the EDso value of adriamycin and was even better against the solid cancer cell line SNU-1. It was also observed that 2-substituted compound 36 showed better antitumor activity in mice bearing S-180 cells in the peritoneal cavity. The T/C (％) value of 2-substituted compound 36 was simi-lar to that of adriamycin. Quantitative structure-activity relationship (QSAR) tests reveal that the experimental E $D_{50}$ values against SNU-1 closely correlate with both the calculated HOMO ener-gies ( $E_{HOMO}$) and the measured H-NMR chemical shift of 3-H ($\delta$$_{H}$). The results suggests that a compound having higher $E_{HOMO}$ and $\delta$$_{H}$ values usually should have a lower E $D_{50}$ (SNU-1) value.lue.lue.lue.

• Korean Journal of Pharmacognosy
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• v.17 no.2
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• pp.168-177
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• 1986

Bioassay-directed isolation has yielded some cytotoxic substances against L1210 cell from the Korean traditional medicine. These include 5,2'-dihydroxy-6,7,8,6'-teramethoxyflavone $(IV,\;scutellaria\;root,\;ED_{50}\;=\;1.7\;{mu}g/ml)$, 7-geranyloxycoumarin $(XXXII,\;poncirus\;fruit,\;10.2\;{mu}g/ml) $and panaxydol $(I,\;white\;ginseng,\;0.03\;{mu}g/ml)$. IV, XXXII and their derivatives were synthesized in the purpose of in vivo tests and for observation of structure-activity relations. Among the flavone derivatives, 5,2',6'-trihydroxy-6,7,8-trimethoxy flavone (XVIII), 5-hydroxy-6,7,8-trimethoxy-6'-benzyloxyflavone (XVII) and 5,8-dihydroxy-6,7-dimethoxyflavone (X) showed the cytotoxicity which has no correlation to the flavone structures. Of the coumarins synthesized, 7,8-dihydroxycoumarin (XXVI), 6-7-dihydroxycoumarin (XXIX) and 6-hydroxy-5,7-dimethoxycoumarin (XXXI) showed considerable activities. Acetylated XXXI has moderate activity $(ED_{50}=17.2\;{mu}g/ml)$. Monobydroxycoumarins or their methyl and allyl ether were inactive. IV inhibits the growth of the solid form of S-180 by 70% at 40 mg/kg and shows T/C of 166% on the ascitic S-180 at 40 mg/kg. It strongly inhibits the activity of the membrane bounded ATPase from L1210 cell. The most cytotoxic fraction of the antitumor materials studied is the one from the trichosanthes root showing $ED_{50}=0. 0003\;{mu}g/ml$ against L1210 cell. This fraction, obtained from ethyl acetate extract, showed T/C of 130 and 135%, on ICR mice bearing S-180 and $BDF_1$ mice bearing L1210 at 10 mg/kg and 7.5 mg/kg, respectively.

• Journal of Physiology & Pathology in Korean Medicine
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• v.16 no.2
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• pp.327-331
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• 2002

The purpose of this research was to investigate the immuno-modulatory effect and anti-carcinogenic property of Cordyceps militaris(CM) and/or Paecilomyces japonicus (PJ). The proliferation of cultured splenocytes and thymocytes were enhanced by the addition of 10 ㎍/ml of CM and/or PJ. B lymphocytes subpopulation in splenocytes were increased both CM and/or PJ administered(p.o. for 7 days)-mice. Thymic T lymphocytes, especially TH cells were significantly increased in CM-administered mice. CM and/or PJ treatment inhibited the cell viability of L 1210 mouse leukemia and HL60 human leukemia cells and induced the apoptosis of L1210 and HL60 cells. In addition, CM and/or PJ increased the hemaggutination(HA) titer against SRBC. These results suggest that CM and/or PJ have an immuno-modulatory action and anti-carcinogenic property.

• Korean Journal of Pharmacognosy
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• v.17 no.4
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• pp.286-291
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• 1986

Forty herbal drugs which are described to have potential antitumor activity were solvent-fractionated with petroleum ether, ether and ethyl acetate in sequence. The cytotoxic activity was mostly shown in the ether fraction(40.54%) and petroleum ether fraction (35.15%), but scarcely in the water phase (10.8%), meaning that most of the active components had less polar property. Twenty-seven percent of the drugs tested were active, which is higher value than 10.4% of the random sampled drugs The drugs possessing the $ED_{50}$ values less than $10{mu}g/ml$ were the roots of Lithospermum erythrorhizon, Curcuma domestica, Salvia miltiorrhiza, Astragalus membraneceus and Scutellaria indica, the leaves of Panax ginseng, S. indica and Liriodendron tulipifera, the barks of Picrasma ailanthoides and Rhus vernifera, the herbs of Agrimonia pilosa and Siegesbeckia pubescens the seeds of Tricosanthes kirilowii, P. ailanthoides, and the stem of P. ginseng.

• Microbiology and Biotechnology Letters
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• v.25 no.5
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• pp.477-482
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• 1997

To investigate the cytotoxicity of Korean traditional fermented soybean products using the MTT assay, we extracted soybean, Kanjang, Doenjang, Kochujang, and Chongkukjang with water, methanol, and hexane. Primary testing of cytotoxicity of 14 extracts was done for P388D1(mouse lympoid neoplasm) and L1210(mouse leukemia) cell lines. Doenjang methanol extract, Kochujang hexane extract, Chongkukjang methanol extract, and Chongkukjang hexane extract showed cytotoxicity of 86.1, 94.3, 83. 6, and 81.1%, respectively against P388D1, and showed cytotoxicity of 69.4, 96.9, 51.4, and 95.1%, respectively against L1210. All the other extracts showed less than 50% cytotoxicity. Methanol extracts of Doenjang and Chongkukjang showed dose-dependent cytotoxicity against P388DI, L1210, SNU-16 (human stomach cancer), HepG2(human hepatic cancer), WiDr(human colon cancer) cell lines, and IC$_{50}$ of Doenjang methanol extract was 67.7, 90.4, 1338.0, 706.4, and 371.2 $\mu$g/ml, respectively, and IC$_{50}$ of Chongkukjang methanol extract was 107.1, 228.3, 756.2, 1346.0, and 327.0 $\mu$g/ml, respectively.