• Korean Journal of Pharmacognosy
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• v.19 no.4
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• pp.251-255
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• 1988

A cytotoxic sesquiterpene against L1210 cell, named pubetalin. was isolated from the herb of Siegesbeckia pubescens Makino. Its structure was identified as $6-formyl-2,\;3,\;3{\alpha},\;4,\;5,\;8,\;9,\;11{\alpha}-octahydro-10-hydroxymethyl-5-methoxy-3-methylene-2-oxocyclodeca[{\beta}]\;furan-4-ylester$ of 2-methyl-2-propenoic acid.

• Archives of Pharmacal Research
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• v.8 no.4
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• pp.283-284
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• 1985

It was previously reported that the petroleum ether fraction of the Korean ginseng root shows cytotoxic activities against L1210, L5178Y, Hela cell and Sarcoma 180 cell (1). In this study the cytotoxic substance against L1210 cell was isolated over a silica gel column and a preparative HPLC, followed by the cytotoxic assay (2).

• YAKHAK HOEJI
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• v.40 no.4
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• pp.462-467
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• 1996

Forsythiae Fructus was studied on cytotoxic activities for the purpose of finding out active consituents against L1210 and HL60 cells. To isolate the active ones, the methanolic extract was partitioned into water insoluble and water soluble fractions. Furthermore, the water soluble fraction was fractionated into four parts, n-hexane, benzene, ethylacetate and water fractions. Among these, the water insoluble fraction showed the most potent cytotoxic activities on L1210 and HL60 cells in vitro. The water insoluble fraction was applied to silica gel column chromatography and divided into 5 fractions(fr. 1-5). The active constituents I and II were isolated from fr.2 and 3, respectively, by repeated silica gel column chromatography and recrystallization. The constituents were identified as 3${\beta}$-acetylbetulinic acid and betulinic acid by means of physicochemical data. The $ED_{50}$ values of 3${\beta}$-acetylbetulinic acid and betulinic acid were 9.10 and 16.43${\mu}g$/ml against L1210 cells and 2.72 and 2.41${\mu}g$/ml against HL60 cells, respectively.

• Archives of Pharmacal Research
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• v.17 no.1
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• pp.45-47
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• 1994

A cytotoxic sesquiterpene against L1210 and Hl-60 cells was isolated from Angelicae Koreanae Radix (bulk-kang-hwal). The component was identified as bisabolangelone by means of chemical and physical methods. The $ED_{50}$ values of it were $1.20{\;}\mu\textrm{g}/ml$ against L1210 cells and $2.30{\;}\mu\textrm{g}/ml$ against HL-60 cells. Bisabolangelone was found in bulk-kang-hwal but not in kang-hwal.

• YAKHAK HOEJI
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• v.44 no.3
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• pp.213-223
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• 2000

SD-994 was prepared from methanol extract of Artemisia argyi by stepwise purification of solvent partioning and silica gel chromatography. In the course of this purification, fractions obtained at each step were investigated for their cytotoxicities against L1210 cells. Fractions A~G prepared from chloroform fraction showed considerable cytotoxicities raging 40~90% against L1210 cells. Subfractions I~IX obtained from fraction A exhibited various cytotoxicities and subfraction I (SD-994) was found to be the most effective compound. $IC_{50}$ values of SD-994 were measured to be $0.5{\;}{\mu\textrm{g}}/ml and less than $0.05{\;}{\mu\textrm{g}}/ml against L1210 cells and normal lymphocytes, respectively: When SD-994 was added to L1210 cell as cytotoxic agent, significantly increased amount of superoxide ($O_2^-$) and dramatically augmented activities of superoxide dismutase (SOD), specially MnSOD and glutathione peroxidase (GPx) were observed according to the concentration and incubation time. Whereas, in case of normal lymphocytes under the same condition, cytotoxicities were not apparent and the generation of superoxide ($O_2^-$) or the activity changes of SOD and GPx were insignificant. These results together indicate that the cytotoxic action of SD-994 against L1210 cell may be achieved via necrosis and/or apoptosis induced by reaction oxygen species which could not probably be completely abolished even by drastically increased antioxidant enzymes, SOD and GPx activities.

• Korean Journal of Pharmacognosy
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• v.20 no.4
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• pp.223-226
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• 1989

A cytotoxic sesquiterpene against L1210 cell has been isolated from the root of Curcuma domestica. Its structure was identified as ${\beta}-sesquiphellandrene$. The cytotoxicity-potentiating substance was (+)-ar-turmerone. (+)-ar-Turmerone potentiated the cytotoxicity of ${\beta}-sesquiphellandrene$(5 fold in $ED_{50}$ value) and an unknown sesquiterpene which was isolated from the root as well, and that of aurapten(6.3 fold) isolated from the unripe fruit of Poncirus trifoliata. Moreover, it potentiated the cytotoxic activities of MeCCNU 10 fold and cyclophosphamide 10 fold. Except the fact that all the effective cytotoxic substances possess relatively good lipophilicity, no relationship between structures of the cytotoxic substances and the cytotoxicity-enhancing effect of (+)-ar-turmerone could be observed.

• YAKHAK HOEJI
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• v.34 no.4
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• pp.262-266
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• 1990

Acetylshikonine, isolated from the root of Lithospermum erythrorhizon showed a strong cytotoxic activity ($ED_{50}=0.10\;ug/ml$) against L1210 cell and T/C = 182% in ICR mice bearing S-180 at a dose of 5 mg/kg. Administrations of 10 mg/kg and 15 mg/kg reduced the T/C values to 60 and 77% respectively. Higher doses reveal toxicity. Seven naphthazarin derivatives synthesized showed good cytotoxic activities against L1210 cell. Especially, naphthazarin and hydronaphthazarin have strong activities ($ED_{50}=0.05\;ug/ml$ for both). Naphthazarin showed a severe toxic effect on ICR mice bearing S-180; no significant toxic effect was observed at a dose of 1 mg/kg or 2 mg/kg, but a severe toxicity (T/C = 23%) by administration of 5 mg/kg. Alkylation of C-2 of naphthazarin is necessary for reducing the toxic effect on ICR mice bearing S-180.

• Korean Journal of Pharmacognosy
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• v.27 no.3
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• pp.173-177
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• 1996

For the search of anticancer compounds from natural products, 43 plants were extracted with benzene and methanol, separately, and the extracts were screened for the cytotoxicity against L1210 and HL60 cancer cell lines. From the results, 22 samples in benzene extracts showed cytotoxicity against L1210 cells and 23 samples against HL60 cells, respectively. However, any methanol extracts did not exhibit cytotoxicity against two cancer cell lines, it suggested that cytotoxic compounds seemed to have low polarity. $ED_{50}$ values less than $5\;{\mu}g/ml$ were observed in 14 and 9 samples in benzene extracts against L1210 and HL60 cancer cells, respectively.

• Korean Journal of Pharmacognosy
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• v.20 no.2
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• pp.71-75
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• 1989

A new polyyne, panaxyne, was isolated from the Korean red ginseng. The structure was determined as tetradeca-13-ene-1, 3-diyne-6, 7-diol by comparison of spectral data. The $ED_{50}\;value$ of panaxyne as cytotoxicity against L1210 cell was $11.0\;{\mu}g/ml$. The lower cytotoxic activity of the substance relative to other ginseng polyynes is presumably due to lack of the essential structural part of hept-1-en-4, 6-diyne-3-ol.

• Korean Journal of Pharmacognosy
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• v.22 no.4
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• pp.249-251
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• 1991

The cytotoxic and antibacterial activities of the leaf, the stem and the seed extracts of Luffa cylindrica were evaluated against L1210 cells and Streptococcus mutans OMZ176, respectively. Among hexane, ether, butanol and water fractions, the ether fraction demonstrated the most potent cytotoxic activity, and the $ED_{50}$ values of the ether extract from the leaf, the stem and the seed were 3.5, 3.7 and $13.7{\mu}g/ml$, respectively. Meanwhile, the other fractions showed negligible effect. Separately, it was found that the antibacterial activity of the respective fraction from three parts was insignificant.