• Environmental Analysis Health and Toxicology
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• 제8권3_4호
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• pp.23-32
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• 1993

This study was designed to elucidate the mechanism of nephrotoxicity caused by antitumor agent tetraphosphine platinum (II) complex (RC-1), which was synthesized as a tetraphosphine Pt (II) derivatives recently. Rats treated with RC-1 (20mg/kg/day) showed the increase of BUN value and malondialdehyde contents in kidney homogenate, compared to the control and which means the lipid peroxidation was a main cause of nephrotoxicity. In order to investigate the cytotoxic mechanism of RC-1, we also tested and revealed the generation of oxygen free radicals derived from neutrophil stimulated by RC-1 and interaction of the oxygen free radicals with the erythrocyte membrane. From the above results, we suggest that nephrotoxicity of general platinum (II) antitumor compounds as well as RC-1 were inhibited by radical scavengers.

• Preventive Nutrition and Food Science
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• 제4권2호
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• pp.117-121
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• 1999

The anititumor and immunologic activities of the glycoproteins extracted from sea cucumber (Stichopus japonicus) on mice bearing sarcoma 180 cells were investigated . Maximum tumor suppression (64%) occurred at the dose of 100mg glycoprotein/kg. The highest prolongation ratio was achieved at the level of 100mg/kg an dincreased by 395 more than that of control. Glycoproteins from sea cucumber exhibited direct cytotoxic effect on the tumor cells. Dose dependent increase of leucocyte, peritoneal exudate cell and weights of immunoorgans revealed the improvement of immunity. When the glycoportein-administered group was compared with the control, a significant difference was not noted in the clinico-chemical values such as S-GOT, S-GPT , alkaline phoshatse activity, total protein, cholesterol, triglyceride, urea nitrogen and glucose levels in blood. These results suggests that the antitumor activity of sea cucumber glycoprotein is associated with activation of cells in the immune system.

• Journal of Ginseng Research
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• 제15권2호
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• pp.99-105
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• 1991

This experiment was performed to investigate the effects of ginseng saponin fraction and cyclophosphamide (CY) on the tumor development, the antitumor effect and the tumoricidal activity of mouse macrophage. When mice were treated with saponin or CY following inoculation with Sarcoma 180, tumor development was inhibited and survival ratio increased, and a combination of both treatments further inhibited the tumor development. Tumoricidal activity of macrophage was effectively increased at 10-7% concentration of CY and it was further increased when macrophage was cotreated with saponin and CY. Tumoricidal activity of macrophage was greatest at the third day after inoculating tumor cell. Both saponin and CY increased the chemiluminescence of macrophage, but CY had no effect on releasing TNF, unlike saponin.

• Archives of Pharmacal Research
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• 제8권1호
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• pp.42-44
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• 1985

Polysaccharides were isolated with alkaline extraction method from twelve pharmaceutical plants, which have been used against the various tumors in the oriental herb medicine, and examined for their antitumor activities. When the polysaccharides were administered i. p. at the dose of 10mg/kg/day for ten consecutive days to the male ICR mice, which had been implanted with $1{\times}10^{6}$ cells of sarcoma 180 twentyfour hours before the first injection of polysaccharides, those from Forsythia Corea, Curcuma, Zedoaria, Albizzia Julibrissin, Prunuts Persica, Foeniculum Vlugare and Daphne Pseudogenkwa showed inhibition ratios of 88.0%, 61.1%m 73.0%, 72.8% 55.1% and 71.7%. The significant prolongation of life span was observed only in the case of Forsythia Corea (18.1%). Other six polysaccharide fractions from Olibanum, Lonicera Japonica, Rheum Coreanum, Scirpus Maritimus, Gleditchia Officinalis and Brassica Juncea showed negligible inhibition ratios.

• 한국자원식물학회지
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• 제5권2호
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• pp.73-84
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• 1992

Many types of compounds have been isolated from higher plants till now, that is, alkaloids, terpenes, lignans, steroids and so on. One of them, named as RA series Cyclic hexapeptides isolated from Rubia akane and R. cordijofia also have strong antineoplastic activity against various types of tumors. Till now 10 kinds ofRA series compounds were isolated and named as RA - I, II, III, IV, V, VI, VII, VIII, IX and X. Moreover,monogl-ucoside of RA - V newly Isolated from same plant. Many kinds of derivatives including natural RAcompounds were tested for QSAR, and one of them, RA - VII was screened up as a most suitable substance asan antitumor agent. RA - VII(=RA-700) has strong cytotoxic activity against KB cells, P388 Iymphocyticleukemia and MM2 mammary carcinoma cells. RA - VII has been under investigation for Phase I clinical trials.

• 한국자원식물학회지
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• 제5권2호
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• pp.95-103
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• 1992

Present anticancer drugs in the clinical side have not showed a conclusive effect of the chemotherapy for cancer patients. In order to find much more efficient antitumor agents fromnatural resources, various screening methods vivo and in vitro have been developed by manyresearchers. The intention of this paper is to provide an outline of some background on the tumorsystem in drug development of natural products, to review some screening programs for theevaluation of antitumor activity and to introduce the practical procedures of some antitumorscreening methods in vivo and in vitro. At the end of this paper, the current literatures related toantitumor natural products from higher plants at our laboratory are described.Key words'anticancer drugs, screening methods.

• 약학회지
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• 제32권5호
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• pp.334-339
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• 1988

AraC-5'-methylthioacetate (araC-MTA, 1) and araC-5'-butylthioacetate (araC-BTA, 2) were prepared and their physical and chemical properties and in vivo antitumor activities were examined. Both compounds were found to have higher partiton coefficients (n-hexanol/water) than their parent araC and to be hydrolyzed to araC within an hour in mouse plasma and ascitic fluid solutions. In in vivo antitumor activity test they showed similar potency to araC, which were assumed due to too quick hydrolyses of them to parent in the body fluid.

• 약학회지
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• 제49권1호
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• pp.60-67
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• 2005

Nonclassical aminobenz[cd]indole antifolates 4, 5 and 6, in which the glutamic acid moiety of the classical antifolates is substituted by 2-phenylglycinamide or 3-aminobenzamide, were synthesized and their in vitro antitumor activity was evaluated. The purpose of this substitution is that the lipophilicity is enhanced due to the aromatic ring of the target compounds for the passive transport through lipid membrane of cells while the hydrogen bonding of the amide is retained in the active site of the enzyme, thymidylate synthase, where the glutamate is originally present. The target compounds were highly cytotoxic against tumor cell lines of murine and human origin with micromolar to nanomolar $IC_{50}$ values. Most effective was compound 4 ($N^6-methyl-N^6$-[4-[(${\alpha}$(S)-aminocarbonylbenzyl) aminocarbonyl]benzyl]-2,6-diaminobenz[cd]indole)with $IC_{50}$ of 2 nM against SW480, human colon adenocarcinoma cell line, which is 650-fold more potent than the reference compound 3.

• Archives of Pharmacal Research
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• 제8권4호
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• pp.277-282
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• 1985

Polysaccharide fractions were prepared from Albizzia julibrissin by different extraction schedules. The fractions obtained were designated as PS-I and PS-II, respectively. Further purification of PS-I by Sephadex G-200 column chromatography gave two subfractions, Alju A and alju B, Each fraction showed marked antitumor activity against sarcoma 180 solid form but not ascite form. PS-I and PS-II increased delayed hypersensitivity in normal and tumor bearing mice. PS-I treatment led to moderate restoration of the suppressed antibody production in tumor bearing mice.

• Archives of Pharmacal Research
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• 제22권6호
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• pp.575-578
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• 1999

Derivatives of elema-1,3-diene were synthesized in several steps as polar analogs of $\beta$-elemene, antitumor agent under clinical phase. The lactone ring of compound 1 was opened by LiAlH4 to give diol 2 which was selectively protected by TBDPSCI. After acetylation of the secondary alcohol, the acetylated product was ozonolyzed and reduced to give elemene derivative 4 which was converted to diolefin 8 via selenides subsequent deprotection by tetrabutylammonium fluoride gave two compounds 9, 10.