• Journal of the Korean Chemical Society
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• v.19 no.6
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• pp.438-442
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• 1975

The syntheses of anomeric mixtures of 1-(4-thio-${\alpha},{\beta}$-D-ribofuranosyl)-5-fluoro-and 5-chlorouracils from their corresponding bis(trimethylsilyl) derivatives of 5-halogenouracils and 2,3,5-tri-O-acetyl-4-thio-${\alpha},{\beta}$-D-ribofuranosyl chloride are described. Preliminary biochemical studies showed that in leukemia 1210 cells and Streptococcus faecium, the ${\beta}$-anomeric 5-chloro-4'-thionucleoside is not greatly different from the corresponding 4'-oxygen analog. However, the 5-fluoro-4'-thionucleoside showed a growth inhibitory effect more than that of the oxygen counterpart. The potential chemotherapeutic use of the analog is to warrant further study.

• The Korean Journal of Food And Nutrition
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• v.15 no.2
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• pp.151-157
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• 2002

This study was carried out to investigate functional activities of the free radical scavenging and germ of Glycin max. Merrill fur cytotoxicity toward P338 and L1210 cells derived from mouse. Effect of crude saponin were examined to oxygen radicals and their scavenger enzymes in liver fractions of Spragae-Dawley(SD) rats. Male rats were fed basic diets of control and experiment diets of 0.5∼1.0% crude saponin. There were no significant differences in hydroxy radical($.$OH) formation of liver mitochondria and microsomes in 1.0% group, while $.$OH formations were significantly decrease in 0.5% and 1.0% saponin compared with control group. Their oxygen radical(O$_2$$\^$$.$/) scavenging activities were significantly decrease in liver cytosol of 0.5% and 1.0% saponin group compared with control group. Soybean germ saponin was isolated purified by the method of HPLC to investigate the cytotoxicity of mouse cells by using the MTT assay. SA-1 saponin fraction of soybean germ showed to inhibit toward growth cell of P338 and L1210 cells and its showed less than 50% cytotoxicity These results suggest that the saponin may play a effective role in attenuating a oxygen radical formations and increasing a scavenger enzyme activities.

• Journal of the Korean Society of Food Science and Nutrition
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• v.33 no.3
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• pp.475-479
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• 2004

The proteinpolysaccharides (PPS) from Polyporus umbellatus (P. umbellatus) screlotium is composed by 78.2% of saccharide, 16.8% of protein, and 4.0% of ash. PPS from P. umbellatus showed antitumor activities against 180 solid tumor in ICR mice at the concentration of 20-160 mg/kg/day. PPS from P. umbellatus inhibited cell viability to 47.4% and 45.0% in leukemia cell lines, L-1210 and K-562 cells at 50-400 $\mu\textrm{g}$/mL concentration, respectively. But the hall mark of cell apoptosis, DNA fragmentation was not observed at those concentration. 2.5-10.0% of PPS from P. umbellatus inhibited mutagenecity evoked by 2-nitrofluorene and sodium azide in Salmonella typhimurium TA 98 and TA 100. From these results, it is suggested that the PPS of P. umbellatus has antitumor and antimutagenic effect, and its cytotoxic effect may not be ascribed to the apoptosis.

• Korean Journal of Food Science and Technology
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• v.30 no.3
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• pp.702-708
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• 1998

The effects of mushrooms such as Lentinus edodes and Pleurotus ostreatus on anti-cancer activity through in vivo and in vitro experiments were powders of protein-bound polysaccharides in mushrooms were solubilized in 0, 5, 25 mg/kg saline, respectively and were used in vitro experiments. The in vivo experiments were carried out as followed: i) anti-cancer activities on Leukemia $(L_{1210})$, Hepatlicus cancer $(H_{22})$ and Sarcoma180/(S180), and ii) the effect on immune system through changes in intestine weight and the number of hemolytic plague forming cells. Protein-bound polysaccharides of all showed anti-cancer activity on $L_{1210}$ and fruit body of Lentinus edodes 25 mg/kg treatment group showed the highest inhibition rate (86%). Pleurotus ostreatus mycelial in medium of cultivate 25 mg/kg treatment. Fruid body of Lentinus edodes 25 mg/kg treatment group showed the highest inhibition rate (86% and 71%, respectively) on $H_{22}$ among them. The inhibition rates of fruit body and mycelial of Lentinus edodes 25 mg/kg treatment groups on S180 were 33.9% and 30.9%, respectively. Each samples of 50, 100, 200, $400\;{\mu}g/{\mu}L$ on in vitro cell toxicity test did not show significantly different cell death rates at P<0.05. In immune test, weights of liver and spleen were increased according to increase in conc. but were not significantly different at P<0.05. The weights of thymus were heavy in fruit body and mycelial of Lentinus edodes treatment group but were not significantly different at P<0.05. Hemolytic plague forming cells with antibody formation capability were significantly high in fruit body and mycelial of Lentinus edodes treatment samples.

• Journal of Haehwa Medicine
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• v.10 no.2
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• pp.73-81
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• 2002

In the literal study of anti-tumor effects of Jakeumjung. the results were as follows. 1. Jakeumjung is a traditional oriental medical prescription which is composed of Cremastare appeniculatae tuber, Euphorbiae pekinensis radix, Toosendan fructus, Chinensis galla, Moschus, Realgar and Cinnabaris. 2. Jakeumjung is applied to patients by administering or external application. When it is administered for patients, pertinent dose is 0.6~1.5g twice or three times per one day. When it is applied by external application, we melt it by water or vinegar and apply it to patients. 3. Effects of Jakeumjung are expelling toxin and pestilence, counteracting pathogen and relieving stagnation, detumescence and stopping pain. So it is used for detoxification from ancient. In recent, it is often used for cancer such as breast cancer, pancreatic cancer, epigastric cancer, acute leukemia, lymphoma, thymus cancer and skin cancer. 4. From the various experiments, Jakeumjung has been proved to have antifungal and antitumor effects. It inhibits and kills L7212, L1210 cells of leukemia. Especially, it acts in S stage of cell period. 5. Jakeumjung includes mineral medicines such as Realgar, Cinnabaris. So if we execute progressive study for anticancer effects and safety, the boundary of oriental medicine of using mineral medicines for cancer therapy will magnify in the future.

• 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.

• YAKHAK HOEJI
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• v.44 no.5
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• pp.463-469
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• 2000

Protein-polysaccharide fractions separated from nine Korean wild mushrooms were subjected to an in vitro screening test for lymphoblastogenic activity. Of these, PPLP, the protein-polysaccharide fraction of Lycoperdon pedicellatum, showed the most potent activity and were further investigated for its antitumor activity. When intraperitoneally injected into ICR mice once daily for six days at a dose of 30 mg/kg, PPLP strongly inhibited the growth of sarcoma 180 tumor cells, showing the inhibition ratio of 97.6%. PPLP also showed in vitro inhibitory activity on sarcoma 180 or leukemia L1210 at the concentration of 500 $\mu\textrm{g}$/$m\ell$ or higher. These results strongly suggest that PPLP might exert its antitumor activity through immunostimulation as well as inhibitory activity on the tumor cells.

• Advances in Traditional Medicine
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• v.1 no.2
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• pp.45-51
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• 2000

This study was carried out to evaluate cytotoxicity of the methanol extract from Sophora flavescens Ait. against L1210 (lymphocytic leukemia) and $P388D_1$ (lymphoid neoplasma) Cells in vitro. We have determined cytotoxicity by the MTT (3- (4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H- tetrazolium bromide) assay. The order of cytotoxicity of Sophora flavescens Ait. extracts against L1210 and $P388D_1$ cells in vitro is as follows: Fr. 4 > Fr. 3 > Fr. 5 > Fr. 2 > Fr. 1. These results suggest that the fraction 4 of the methanol extracts from Sophora flavescens Ait. may be a valuable choice for the development of antitumor agents. In order to develop an antimicrobial agent, dried Sophora flavescens Ait. was extracted with hot methanol, and then antimicrobial activity (MIC test) was investigated. In this study, the fraction 3 of the methanol extracts from the roots of S. flavescens showed strong growth inhibition activity against gram-positive and gram-negative bacteria (MIC, $3.125\;{\mu}g/ml$) such as S. mutans, S. epidermidis and P. putida. These results indicate that fractions 3 and 4 inhibit tumor cells and bacteria.

• The Korean Journal of Pharmacology
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• v.29 no.2
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• pp.283-295
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• 1993

Pt-complexes is currently one of the most compounds used in the treatment of solid tumors. However, its used is limited by severe side effects such as renal toxicity. Our platinum-based drug discovery program is aimed at developing drugs capable of diminishing toxicity and improving antitumor activity. We synthesized new Pt (II) complex analogues containing 1, 2-diaminocyclohexane (dach) as carrier ligand and 1, 3-bis (diphenylphosphino) propane (DPPP)/1,2-bis (diphenylphosphino) ethane (DPPE) as a leaving group. Furthermore, nitrate was added to improve the solubility. A new series of (KHPC-001) [Pt (trans-1-dach)(DPPP)] $2NO_3$ and (KHPC-002) [Pt (trans-1-dach)(DPPE)] $2NO_3$ were synthesized and characterized by their elemental analysis and by various spectroscopic techniques [infrared (IR), $^{13}carbon$ nuclear magnetic resonance (NMR)]. KHPC-001 and KHPC-002 demonstrated acceptable antitumor activity aganist P-388, L-1210 lymphocytic leukemia cells and significant activity as compared with that of cisplatin. The toxicity of KHPC-001 and KHPC-002 was found quite less than that of cisplatin using MTT, $[^3H]$ thymidine uptake and glucose consumption tests in rabbit proximal tubule cells and human kidney cortical cells.

• The Korean Journal of Pharmacology
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• v.31 no.1 s.57
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• pp.103-114
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• 1995

Platinum coordination complexes are currently one of the most compounds used in the treatment of solid tumors. However, its use is limited by severe side effects such as renal toxicity. Our platinum-based drug discovery program is aimed at developing drugs capable of diminishing toxicity and improving antitumor activity. We synthesized new Pt (Ⅱ) complex analogue containing 1,2-diaminocyclohexane (dach) as carrier ligand and 1,2-bis(diphenylphosphino) ethane (DPPE) as a leaving group. Furthermore, nitrate was added to improve the solubility. A new series of [Pt(trans-ddach)(DPPE).$2NO_3(PC)$ was synthesized and characterized by their elemental analysis and by various spectroscopic techniques [infrared (IR), $^{13}carbon$ nuclear magnetic resonance (NMR)]. PC demonstrated acceptable antitumor activity aganist P388, L-1210 lymphocytic leukemia cells and SK=OV3 human ovarian adenocarcinoma cells, and significant. activity as compared with that. cisplatin. The toxicity of PC was found quite less than thar of cisplatin using MTT, $[^3H]$ thymidine uptake and glucose consumption tests in rabbit proximal tubule cells, human kidney cortical cells and human renal cortical tissues. Based on these results, this novel platinum compound represent a valuable lead in the development of a new anticancer chemotherapeutic agent capable of improving antitumor activity and low toxicity.