• YAKHAK HOEJI
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• v.31 no.2
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• pp.70-81
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• 1987

To elucidate action mechanism of lyophyllan A, an antitumor polysaccharide of Lyophyllum decastes, its immunological activities were examined. Lyophyllan A increased significantly the weights of spleen and liver of mice. Lyophyllan A also restored the decreased thymic weight in tumor-bearing mice. It did not show any direct cytotoxicity against tumor cells, but showed immunopotentiating activities by increasing the number of the plaques in hemolytic plaque assays. Lyophyllan A increased the number of peritoneal exudate cells (PEC) and inhibited the growth of sarcoma 180 mixed with PEC. Moreover the macrophages from lyophyllan A-treated mice exhibited a strong cytotoxic activity towards L5178Y target cells.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.345.1-345.1
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• 2002

${\alpha}$-terthienyl the first isolated from natural products shows potent antitumor activity, which encouraged us to study terpyridine and its biological properties. Terpyridine has also been reported as having carcinogenicity, and it's erivatives showed high cytotoxic activities against several human cancer cell lines and topoisomerase I inhibitory ctivity. Mannich free base from condensation reaction was allowed to react with pyridinum salts to give activity. (omitted)

• Microbiology and Biotechnology Letters
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• v.23 no.3
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• pp.329-336
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• 1995

For the development of new antitumor antibiotics produced by microorganisms, Streptomyces sp. YBE-316 was isolated from soil. The productivity of the antitumor antibiotic from Streptomyces sp. YBE-316 gradually increased after 60 hours, and was maximum after 100 hours after inoculation in growth medium (2.0% sucrose, 1.0% soybean meal, 0.1% K$_{2}$HPO$_{4}$, pH 7.0) at 30$\circ$C, 150 rpm, 5 NL/min by 30 l jar fermentor. This antitumor antibiotic was present only in mycelium, and stable in pH 5.0-10.0 for 20 minutes at 100$\circ$C. Antitumor and antibiotic activities were maintained at neutral pH, and heat stability was low. This antitumor antibiotic was soluble in methanol and ethanol, and insoluble in water, ethyl acetate, chloroform, and n-hexane. This antitumor antibiotic was sequentially purified by acetone extraction from mycelium, butanol extraction, and silica gel column chromatography. Antitumor activity was low against most tested cell lines, but antibiotic activity was high and low against yeasts and bacteria, respectivelv. The visualization test showed that this antitumor antibiotic had higher hydroxyl, ketone, amino, carboxyl groups, and sugar(s) in its structure. Instrumental analyses showed that this antitumor antibiotic was a pentaene in polyene class antibiotics. In pentaene class antibiotics, this was considered as an eurocidin or capacidin type antibiotics. The molecular weight of this antitumor antibiotic was higher than 683.0 daltons, and this antitumor antibiotic might be glycosylated by other sugar(s), instead of mycosamine or perosamine, an amino sugar.

• Biomolecules & Therapeutics
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• v.6 no.4
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• pp.395-399
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• 1998

DW2282, (S)- (+)-4-phenyl -1-[N-(4-am mob enzoyl) -indolin-5- sulfonyl]-4,5- dihydro-2-imidazolone hydrochloride, is a novel anticancer agent thought to have an unique mechanism of action on the inhibition of tumor growth. In this study, we estimated in vivo antitumor activities and pharmacokinetics of Dw2282 depending on various vehicles. The inhibition rate of tumor growth was increased by 50, 100 and 200 mg/kg of Dw2282 in a dose-dependent manner. When Dw2282 dissolved in 4 sorts of vehicles was orally single dosed to rats at 50 mg/kg, Cmax of Dw2282 in 0.5% CMC.Na was a half as high as those in PG, PG+CP and PG+CP+DW. When Dw2282 was orally administered to mice for 5 days, antitumor activity of 130 mg/kg suspended in 0.5% CMC.Na was as effective as that of 65 mg/kg dissolved in the rest of vehicles. Taken together, it is thought that antitumor activities of Dw2282 are resulted from the absorption extent of it and related to the vehicle used.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1998.11a
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• pp.185-185
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• 1998

As part of our continuing attempts to evaluate biologically active compounds from fruiting bodies of cultivated fungus of Paecilomyces japonicus Yasuda, we conducted series of experiments on various fractions and compounds isolated by systematic fractionations. Our main efforts were concentrated on searching for compounds showing antitumor activities, which were tested on mice carrying Sarcoma-180 ascitic tumor. The antitumor activity was assessed by the life spans after these mice were administered Lp. with test compounds for consecutive 20 days. One of two pure compounds, which we have isolated to date, demonstrated significant prolongation of life span. ( Mean Survival Time: 30.3 days compared to that of control: 23.6 days). Structural analysis showed that this compound corresponds to D-mannitol. On the other hand, Ergosterol, another isolated pure compound didn't show efficient antitumor activity. We also obtained water-soluble fractions containing protein-bound polysaccharides and n-butantol fractions, which showed strong antitumor activities, 35.4(150%) and 32.1(136.0%) days of MST, respectively. In SRB assay, however, the test materials didn't show any toxic effects, but the level of acid phosphatase increased significantly when they were applied in cultured macrophage in vitro. Therefore, we concluded that antitumour activities might be attributed to immunostimulating rather than cytotoxic effects. Further experiments are underway to purify and structurally characterize new antitumour compounds from the active fractions.

• Archives of Pharmacal Research
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• v.12 no.2
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• pp.138-142
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• 1989

The nucleophilic substitution reaction of 6-chloro purines (I) with malononitrile and ethyl cyanoacetate is carried out in DMSO and in the presence of an alkali. The possible tautomeric-ylidene form for the products is considered and discussed in view of IR, UV, NMR and mass spectral determinations. The derivatives were tested for their antitumor activities.

• Macromolecular Research
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• v.11 no.5
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• pp.317-321
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• 2003

In order to prepare a prodrug, poly(polyethylene glycol methacrylate-co-methacryloyloxymethyl-5-fluorouracil) (poly(PEGM-co-MAOFU)) prodrug particles were prepared by precipitation polymerization of MAOFU and PEGM in polyacrylic acid solution. The size of prodrug particles were 0.2-0.35 ${\mu}{\textrm}{m}$. The antitumor activity of prodrugs against sarcoma-l80 tumor cell in mice was demonstrated and the polymer particles themselves showed low toxicity and good biocompatibility when they were administrated into mice.

• Archives of Pharmacal Research
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• v.13 no.3
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• pp.285-288
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• 1990

The polysaccharide fraction from the rhizome of Trichosanthes kirilowii (Cu-curbitaceae) showed marked antitumor and cytotoxic activity with immunopotentiating activity. It was evidenced by the increase in the number of circulating leucocytes and peritoneal exudate cells and the recovery of lowered antibody forming activity in mice. The polysaccharide was mainly composed of glucose, galactose, fructose, manmose and xylose and a small amount of protein.

• Journal of Pharmaceutical Investigation
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• v.24 no.4
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• pp.245-250
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• 1994

An attempt was made to develop new water-soluble antitumor Pt(ll) complexes containing ethylenediamine, and their structures were determined by infrared spectroscopy, $^{13}C$ nuclear magnetic resonance and elemental analysis. Their antitumor activities in vitro against L-1210, p-388 leukemia cells and M-14 melanoma cells were investigated and acceptable antitumor activity was found as compared with cisplatin.

• Archives of Pharmacal Research
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• v.25 no.6
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• pp.781-785
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• 2002

A series of pyrazoloxyphenyl benzoyl urea derivatives was designed and synthesized for cytotoxic evaluation as potential antitumor agents. The synthetic compounds were evaluated for in vitro cytotoxicity against five human tumor cell lines, including A-549, SKOV-3, SK-MEL-2, XF-498 and HCT-15. Among others, compound 11 exhibited 50∼100 times greater antitumor activities than the commercial product, Cisplatin.