• YAKHAK HOEJI
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• v.36 no.5
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• pp.491-495
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• 1992

For the research of cytotoxic natural products, 50 medicinal plants were extracted with benzene and methanol, separately, and screened against L1210 cells. From the results(Table I), 6 samples showed cytotoxicity both in benzene and methanol extracts of 17 samples in benzene extracts and 3 samples in methanol extracts, respectively. Generally, the cytotoxicity exhibited high frequency (34%) in benzene extract but low frequency in methanol extract (6%), it meant that active cytotoxic components had less polarity. $ED_{50}$ values less than $10\;{\mu}g/ml$ were observed in 17 medicinal plants.

• YAKHAK HOEJI
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• v.32 no.2
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• pp.125-128
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• 1988

Geranylation of some synthetic and natural flavones have yielded cytotoxic products against L1210 coll; 5,2´-dihydroxy-6,7,8-trimethoxy-6´-geranyloxyflavone 4$(8.5{\mu}g/ml)$, 5,6-dihydroxy-7-gerenyloxyflavone 9$(2.3{\mu}g/ml)$. 2 has showed the same range of cytotoxicity as the starting material, 5,2´-dihydroxy-6,7,8-trimethoxy-6´-benzyloxyflavone$(17.0{\mu}g/ml)$. The cytotoxicity of 4 was lower than its starting substance, 5,2´,6´-trihydroxy-6,7,8-trimethoxyflavone $(4.5{\mu}g/ml)$. On geranylating 5,6,7-trihydroxyflavone(baicalein, $15.0{\mu}g/ml$) the cytotoxic activity has been strongly potentiated($2.3{\mu}g/ml$ of 9). The presence of at least a free hydroxy group in B-ring of Skullkapflavone II-type flavones. was essential for a high activity. A larger RD-group than methoxy in the B-ring has weakened the activity. The cytotoxicities of baicalein series could not be correlated to their structures.

• Journal of Ginseng Research
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• v.8 no.2
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• pp.153-166
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• 1984

The anticancer activities of petroleum ether extract of Panax ginseng root(crude GX) and its partially purified fraction from silicic acid column chromatography (7:3 GX) were studied with Sarcoma 180(S-180) or Walker carcinosarcoma 256 (Walker 256) in vivo and with L1210 leukemic lympocyte in vitro. Potential cytotoxic activities of the crude GX and against L1210 cells were compared with those of 5-Fluorouracil (5-FU) and saponin derivatives (Panax-diol, Panax-triol, Diol saponin, Triol saponin) in vitro. In order to observe the physiological effects of the crude GX and 7:3 GX on the animals with cancer, hemoglobin(Hb), red blood cell(R.B.C) and white blood cell after treatment with each GX in comparison with corresponding control groups, respectively. The anticancer effects of the crude GX and 7:3 GX were estimated by measuring the survival time of S-180 bearing mice after treatment with them. The experimental results obtained are summarized as follows; 1. The one unit of cytotoxic activity against L1210 cells was equivalent to 2.54$\mu\textrm{g}$ and 0.88$\mu\textrm{g}$of the crude GX and 7:3 GX per ml of culture medium, respectively. 2. The cytotoxic activities of Panax-diol, Panax=triol, Diol saponin and triol saponin against L1210 cells were not detected. 3. The anticancer activities of 5-FU against L1210, S-180 and Walker 256 were very effective in vivo and vitro tests. 4. The significantly increased W.B.C values of mice after inoculation with S-180 cells were reduced to normal range by the crude GX treatment. 5. The significantly decreased Hb values of rats after inoculation with Walker 256 were recovered to normal range by oral administration of the crude GX. 6. The survival times of mice inoculated with S-180 cells were extended about 1.5 to 2 times by the 7:3 GX treatment compared with their control group.

• 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.9 no.2
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• pp.115-117
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• 1986

Some coumarins were sythesized for the screening of their cytotoxic activities against L1210 cell. Of the conmarins sythesized, 6, 7-dihydroxycoumarin (esculetin) and 7, 8-dihydroxycoumain (dephnetin) as coumarins with dioxygenated A-ring, and 6-acetoxy-5, 7-dimethoxycoumarin and5, 7-dimethoxy-6-hydroxycoumarin as trioxygenated ones, show considerable cytotoxic activities, ED 50 being 4. 3, 8. 8, 17.2 and 5.5 $\mu$g/ml in the same other as the substances. THe extent oxygenation of the A-ring and the positions of the oxygen functions eventually play an important role for the cytotoxic activity.

• Archives of Pharmacal Research
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• v.20 no.4
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• pp.342-345
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• 1997

A cytotoxic constituent was isolated by bioassay-guided procedure from the roots of Sophora flavescens Aiton (Leguminosae). The constituent was identified as sophoraflavanone G (I) by means of chemical methods and in comparsion with spectral data of standard compound. The $ED_50$ values of constituent I were 0.78, 1.57, 2.14 and $8.59{\mu}g/ml$ against A549, HeLa, K562 and L1210 cell lines, respectively. Constituent I exhibited highly cytotoxic activities against A549, K562 and HeLa cells, but showed a mild activity $$(ED_50 value, 5{\mu}g/ml)$$ against L1210 cells. Among the tested cell lines, A549 cells were the most sensitive to constituent I.

• Proceedings of the Ginseng society Conference
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• 1988.08a
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• pp.19-24
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• 1988

We have isolated two new cytotoxic polyynes against $L_{1210}$ cell from the root of Panax ginseng. namely acetylpanaxydol and panaxydolchorhydrin. The epoxy group in C-9 and the heptyl group on C-10 of the panaxydol-analogues potentiate the activity. Panaxydol has cis-configuration in epoxy group. There is no diffrernce in activity between cis-. trans- and cis/trans-configurational isomers. The essential structure for the cytotoxicity of panaxydol and its isomers is hept-l-en-4.6-diyn-3-ol.

• 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.33 no.4 s.131
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• pp.376-383
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• 2002

The methanol extracts prepared from ten kinds of culinary herbs were investigated for the cytotoxcic effect againt L1210 cancer cells and the mode of action. The substantial cytotoxic effects were observed in all cases with the most prominent effect demonstrated by lemon verbena extract showing $87{\pm}4.1%$ cytotoxicity with $100{\mu}g/ml$ concentration and 3 days culture period. The cytotoxic effect was found to be dose and culture period dependent. With respect to the mechanism of the cytotoxicity, the augmented generation of $O_2{^-}ion$ and the dramatically escalated activities of antioxidant enzymes such as superoxide dismutase(SOD) and glutathione peroixdase (GPx) with addition of the herb methanol extractw suggested that there would be the involvement of reactive oxygen species (ROS) metabolism in the course of L1210 cancer cell death by the mothanol extract of the edible herbs.

• Archives of Pharmacal Research
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• v.12 no.1
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• pp.48-51
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• 1989

A new polyacetylene compound with cytotoxic activity against L1210 cells having diyne-ene and epoxy moiety, named panaxyne epoxide, was isolated from Panax ginseng C.A. Meyer. The chemical structure of the polyacetylene was determined to be tetradeca-13-ene-1,3-diyne-6,7-epoxide by UV, IR, $^1H-NMR,\;^{l3}$C-NMR and mass spectra.