• YAKHAK HOEJI
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• v.40 no.1
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• pp.10-18
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• 1996

Daunirubicin and doxorubicin analogues (5,7,8,9,) in which the natural amino sugar, daunosamine, is replaced by rhamnopyranosyl or 4'-amino rhamnopyranosyl residues have been p repared. The in vitro cytotoxicity of compound 5 or 7 was similar to that of doxorubicin for P388 murine leukemic cell line. But compound 8 or 9 was less cytotoxic than doxorubicin. When administered intravenously on day 1, compound 9 showed antitumor activity comparable to that of doxorubicin against ip-inoculated L1210 murine leukemia and found to be less toxic than doxorubicin. But the in vivo antitumor activity of compound 7 or 8 was inferior to that of doxorubicin.

• Archives of Pharmacal Research
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• v.15 no.3
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• pp.256-262
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• 1992

For the evaluation of the role of substituents of ar-turmerone for its anticancer activity, ar-turmerone (1a) and its analogs like 2-methyl-6-(4'-methyphenyl)-2-octen-4-one (1b), 2-methyl-6-phenyl-2-hepten-4-one (1c), 2-methyl-6-phenyl-2-octen-4-one (1d) and 2 methyl-6-(trans-4'-methylcyclohexyl)-2-hepten-4-one (1e) were preparedd and their cytotoxic activities against $L_{1210}$ cell were determined. Omission of methyl group at para-position dose not variate the cytotoxicity of ar-turmerone. Elongation of alkyl group at 6-position decreases $ED_{50}$ value. Saturation of aromatic ring of ar-turmerone markedly decreases the cytotoxicity. Therefore the smaller size of alkyl group at 6-position and aromatic ring of ar-turmerone should be essential for exhibiting its anticancer activity.

• Archives of Pharmacal Research
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• v.21 no.6
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• pp.738-743
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• 1998

Thirty six 5,8-dimethoxy-1,4-naphthoquinone derivatives, which bear unsaturated alkyl side chain with ester bond, were synthesized and tested cytotoxic activity on L1210 cells a nd antitumor activity against ICR mice bearing S-180 cells. It could be recognized that the cytotoxicities of naphthoquinones with R1, being methyl and propyl (IV1~24) were not enhanced by replacing the alkanoyls with alkenoyls. In contrast, the introduction of the alkenoyl moieties on the compounds with $R_1$=hexyl (IV25~36) resulted in the enhancement of their cytotoxicities. Replacement of alkanoyl group with an alkenoyl group generally increased the T/C value of the mice bearing S-180 cells.

• Natural Product Sciences
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• v.6 no.4
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• pp.165-169
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• 2000

In vitro cytotoxic activities of cisplatin combined with Chungpesagan-tang or puerarin, which were treated with or without human intestinal bacteria, were measured. When cisplatin was combined with Chungpesagan-tang and its ingredient treated without intestinal bacteria, they did not affect the in vitro cytotoxicity of cisplatin against tumor cell lines. However, when cisplatin was combined with intestinal bacteria-treated Chungpesagan-tang and its ingredients, the cytotoxicities against SNU C4, L1210, A549 and P388 tumor cell lines were synergistically increased. Puerarin, which was isolated from Puerariae Radix, did not show in vitro cytotoxicity. However, its metabolite, daidzein, showed potent cytotoxicity against tumor cell lines and was synergistic by the combined usage of cisplatin. These results suggest that natural glycosides are not only prodrugs which can be transformed to active compounds by intestinal microflora, but the combined usage of cisplatin with natural components, such as daidzein, and herbal medicinal polyprescriptions, such as Chungpesagan-tang, may be a new method for prevention and minimization of the toxicity of cisplatin.

• 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.

• Journal of Society of Preventive Korean Medicine
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• v.4 no.2
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• pp.235-241
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• 2000

This study was carried out to evaluate cytotoxic effects of Poncirus trifoliata Raf. extract on lymphocytic leukemia tumor (L1210) cell lines. Disruptions in cell organelles were determined by 3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide (MTT) assay The comparison of Ic50 Values of Poncirus trifoliata Raf. extract in L1210 cell lines showed that their susceptibility to these fractons decreased in the following order: adriamycin > Fr.4> Fr. 6> Fr. 5> Fr. 3> Fr. 1> Fr. 2 by the MTT assay. In order to develop an antumicrobial agent, Poncirus trifoliata Raf. was extracted wit ethanol, and then it was fractionated with several mobile phase. The antitumor activities of fractions of the ethanol soluble extract was investigated. The minimal inhibitory concentrations (MIC) of fractions of the ethanol soluble extract of Poncirus trifoliata Raf. against microorganisms were also examined. Antimicrobial activities of ampicillin and ketoconazole as references were compared to those of fractions of the ethanol soluble extract of Poncirus trifoliata Raf. The antimicrobial activities of all fractions from the extract had growth inhibition activities against gram-positive bacteria, gram-negative bacteria and fungi $(MIC\;>\;200{\mu}g/ml)$. These results suggest that fraction 4 of the ethanol soluble extract of Poncirus trifoliata Raf. possessed the most antitumorous agent.

• Korean Journal of Veterinary Research
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• v.33 no.4
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• pp.701-710
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• 1993

The pine needles, Pinus densiflow Sieb. et Zucc., which is a feed for goats showing a low incidence rate of cancer were evaluated to confirm the potent anticancer effects, with or without several conventional anticancer drugs. The pine needles collected from Mt. Buk-Han located near Seoul were extracted with 95% methanol and methand and concentrated. From the methanol extract, SOM-A, was extracted dichlormethane and SOM-B was extracted with ethyl acetate. SOM-C was extracted with distilled water. These extracts were tested for their antitumor activities in vitro and in vivo. Among them, SOM-A and SOM-C exhibited potent antitumor activities described as belows. 1. The cytotoxic effects of SOM-A and SOM-C were examined against in vitro cultured murine and humman tumor cells. SOM-A showed strong cytotoxicity against human tumor cell lines and SOM-C showed strong cytotoxicity against murine tumor cell lines tested. 2. The antitumor effects of SOM-A and SOM-C were examined against P388 and L1210 of mouse ascitic tumors. The highest mean survival time(MST) ration was 151%(P388) for SOM-C(90mg/kg). 3. To compare the antitumor effects of SOM-A, SOM-B, and SOM-C against solid tumors, S-180 and Ehrlich carcinoma were implanted subcutaneously to mice on Day O. The drugs were given intraperitoneally to mice once a day on Days 1-20, and the tumor weights were measured on Day 21. SOM-A showed inhibition of tumor growth more than 50% in the experiment on S-180 and Ehrlich, and SOM-C also markedly inhibited tumor growth. However, SOM-B had no effect. 4. SOM-C combined with ${\alpha}$-interferon and SOM-C combined with Mitomycin-C enhanced the antitumor activities against murine ascitic tumors P388 leukemia.

• Journal of the Korean Society of Food Science and Nutrition
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• v.21 no.4
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• pp.353-366
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• 1992

This study was devised to purify the compound from tuna that have cytotoxic activities against various cancer cell lines and to observe its immunopotentiating activities. The cytotoxic compound was partially purified 277 fold, from petroleum ehter extract (crude extract) of tuna by silicic acid column chromatography (fraction D) and thin layer chromatography (Spot I). Cytotoxic activity was monitored using human colon cancer cell, HCT-48. The active compound (Spot I) was composed of seven materials which are fatty acids of four kinds ($C_{14:0},\;C_{16:0},\;C_{17:1},\;and\;C_{18:0}$) and unknown three fat materials. The active compound has cytotoxic activities against various cancer cell lines, that is, murine leukemic lymphocytes (L1210, P388) and human rectal (HRT-18) and colon cancer cells (HCT-48, HT-29). The patterns of size distribution of HCT-48 cells in the medium containing tuna extract were shifted to direction of the small size region. Also, the microscopic shape of HCT-48 cells were shrinked and distracted. The number of plaque forming cell and immunoglobin fraction of serum protein obtained from tuna-treated mice were increased, but natural killer cell activity was not affected.

• Korean Journal of Pharmacognosy
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• v.31 no.1
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• pp.72-76
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• 2000

This study was carried out to evaluate cytotoxic effects of Ajuga multiflora Bunge extracts on murine leukemia tumor $(P388D_1)$ cell lines. Disruptions in cell organelles were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide (MTT) assay. The comparison of $IC_{50}$ values of Ajuga multiflora Bunge extracts in L1210 and $P388D_1$ cell lines showed that their susceptibility to these extracts decreased in the following order: Adriamycin>methanol extract>chloroform extract>ethyl acetate extract>hexane extract>water extract by the MTT assay. In order to develop an antimicrobial agent, dried Ajuga multiflora Bunge was extracted with several solvents, and then antimicrobial activity was investigated. The minimal inhibitory concentration (MIC) of the extract against microorganisms were also examined. Antimicrobial activities of amocla and ketoconazole as references were compared to those of extracts of $H_2O$, n-hexane, chloroform, ethyl acetate and methanol. The antimicrobial activity of all extracts from the sample had growth inhibition activity against gram-negative bacteria, gram-positive bacteria and fungi $(MIC>200\;{\mu}g/ml)$. These results suggest that the methanol soluble extract of Ajuga multiflora Bunge may be a valuable choice for the studies on the treatment of murine leukemia tumor cell lines.

• Journal of Society of Preventive Korean Medicine
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• v.4 no.1
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• pp.144-151
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• 2000

This study was carried out to evaluate cytotoxic effects of Houttuynia cordata Thunberg extracts on murine leukemia tumor cell lines. Disruptions in cell organelles were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazol iumbromide (MMT) assay. The comparison of $IC_{50}$ values of Houttuynia cordata Thunberg extracts on $L1210,\;P388D_1$ and Vero cell lines showed that the methanol extract of Houttuynia cordata Thunberg indicated the most antitumor activity in the MTT assay. In order to develop a antimicrobial agent, dried Houttuynia cordata Thunberg was extracted with several solvents, and then antimicrobial activity was investigated. The minimal inhibitory concentration (MIC) of the extracted substance against microorganisms were also examined. Antimicrobial activity of amocla and ketoconazole as references was compared to those of other solvent extracts such as $H_2O$, n-hexane, chloroform, ethyl acetate ethanol and methanol. The antimicrobial activity of all extracts from the sample had growth inhibition activity against gram-negative bacteria, yam-positive bacteria and fungi $(MIC,\;>\;200\;{\mu} g/ml)$. These results suggest that the methanol soluble extract of Houttuynia cordata Thunberg may be a valuable choice for the studies on the treaeent of murine leukemia tumor cell lines and antimicrobial agents.