• Journal of Microbiology and Biotechnology
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• v.14 no.2
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• pp.411-414
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• 2004

Although conjugated linoleic acid (CLA) exerted potent antitumor activities in several animal models, application of CLA as a bioactive ingredient has been limited due to its hydrophobicity. This study was designed to determine the antitumor activity of arginine-CLA complex (Arg-CLA), a hydrophilic form of CLA. Mouse forestomach cancer was induced by gavage with benzo(a)pyrene (B(a)p) for 4-weeks prior to Arg-CLA (0.2 and 0.5％) feeding. Complete necropsies were performed to determine the number, size and locations of all the forestomach tumors at 20 weeks post-B(a)P administration. All mice in the B(a)P group developed tumors, and tumor incidences were decreased by 31 ％ and 44％ in 0.2％ and 0.5％ Arg-CLA-fed groups, respectively, whereas no decrease was observed when Arg or com oil was given alone. Our results suggest that Arg-CLA suppresses mouse forestomach cancer.

• Journal of Life Science
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• v.9 no.1
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• pp.58-62
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• 1999

Several nucleoside 5'-monophosphate analogues and lipophilic nucleoside 5'-(3-pyridinylcarbonyl)monophosphate analogues were synthesized. Antitumor activities of the synthesized nucleoside malogues against P338 mouse leukemia, FM3A murine mammary carcinoma, and U937 human histiocytic lymphoma cells were determined by MTT assay. Antitumor activities of the lipophilic uridine 5'-(3-pyridinylcarbonyl) monophosphate(7) and 2',3'-didehydro-3'-deoxy-thymidine-5'-(3-pyridinylcarbonyl) monophosphate(8) were stronger than those of uridine 5'-monophosphate(1) and 2',3'-didehydro-3'-deoxythymidine-5'-monophosphate(4). This preliminary experimental result suggests that nucleoside 5'-(3-pyridinylcar-bonyl)monophosphate analogues may be new prodrugs to overcome the clinical limit.

• Microbiology and Biotechnology Letters
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• v.22 no.2
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• pp.182-189
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• 1994

The highest antitumor activity was observed in water soluble AS fraction of the Ganoderma lucidum IY 009. AS fraction did not show any cytotoxicity on sarcoma 180 cell but stimulated antibody production, opsonization of macrophage in ICR mouse and superoxide ion production from isolated macrophage. AS fraction activated complement C3 in human serum, and their antitumor activity was inhibited by EDTA, a chelator of cation related complementary activation. AS fraction exerted om prolong of life span and ingibition of tumor growth in the leukemia P388 or L1210 transplanted inbreed mouse,k BDF1 but krestin did not. AS fraction did not show any serious and lethal effects through oral administration on ICR mouse, and LD$_{50}$ of those was above 2,230 mg/kg.

• KSBB Journal
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• v.17 no.6
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• pp.520-524
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• 2002

The present study was designed to investigate the effects of Stachys Sieboldii MIQ as a new natural antitumor agent or immunomodulator. To obtain the above objectives, Stachys sieboldii MIQ was extracted with ethanol. Stachys sieboldii MIQ accelerated mouse spleen cell growth, but inhibited FM3A/S°-cell growth. However, no significant difference was found for CD4+ / CD8+ cells. The growth rates of CD4+ and CD8+ T cells were accelerated more than those normal mouse group. Stachys sieboldii MIQ fed mice showed a significant enhancement of IL-2 receptor expression, increased numbers of CD4+ T cells, and CD8+ T cells. Stachys sieboldii MIQ also stimulated the production of NO by peritoneal macrophages and the production of NO by and the growth of mouse spleen cells. On the other hand, lung localization of Bl6Fl0 melanoma cells was inhibited by ethanol extract of Stachys sieboldii MIQ. These results show that Stachys sieboldii MIQ is a useful new functional antitumor agent or immunomodulator.

• 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.

• Korean Journal of Veterinary Research
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• v.45 no.2
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• pp.151-154
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• 2005

The purpose of this study is to examine the elemental compositions, antioxidant and antitumor activity of water, 20%, 40%, 60%, and 80% ethanol extracts obtained from the fruiting body of Phellinus gilvus. In electron donating ability test, the strong activities more than 70% were observed in $80{\mu}g/ml$ of 20%, 40%, 60% and 80% ethanol extracts from the fruiting body of P. gilvus grown in oak and sawdust. The antitumor activity was evaluated by sulforhodamine B (SRB) in terms of cell survival level. The tumor cells (sarcoma 180) were treated with various ethanol extracts (water, 20, 40, 60 and 80%). The results showed that all extracts inhibited proliferation showing a dose-dependent manner against tumor cells.

• Environmental Analysis Health and Toxicology
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• v.13 no.3_4
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• pp.87-94
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• 1998

The use of cisplatin is limited by severe side effects such as renal toxicity. Our platinum-base drug discovery is aimed at developing drugs capable of diminishing toxicity and improving antitumor activity. We synthesized new Pt (II) complex analogue [Pt (cis-DACH)(DPPP)]. 2NO$_3$ (PC) containing cis-1,2-diaminocyclohexane as a carrier ligand and 1,3-bis(diphenylphosphino) propane as a leaving group. Furthermore, nitrate was added to improved the solubility. In this study, its structure was determined and its antitumor activity against SKOV-3 and NIH-OVCAR-3 human ovarian adenocarcinoma, and in vitro cytotoxicity was determined against primary cultured rabbit kidney proximal tubular and renal cortical cells of human kidney using colorimetric MTT assay. PC demonstrated acceptable antitumor activity against SKOV-3 and NIH-OVCAR-3 human ovarian adenocarcinoma and significant activity as compared with that of cisplatin. The toxicity of PC was found quite less than that of cisplatin using MTT and $^3$H-thymidine uptake tests in rabbit proximal tubular cells and human kidney cortical cells. PC was used for human cortical tissue in 7 weeks hitoculture by the glucose-consumption tests. We determined that the new platinum drug has lower nephrotoxicity than cisplatin. Based on these results, this novel platinum (II) complex compound (PC) represent a valuable lead in the development of a new anticancer chemotherapeutic agent capable of improving antitumor activity and low nephrotoxicity.

• Archives of Pharmacal Research
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• v.17 no.3
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• pp.135-138
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• 1994

Acyclonucleoside homologues of 1-$(\omega$-cyabnoalkyl)-and 1, 3-bis $(\omega$-cyanoalkyl) uracils were synthesized by the series of alkylation reactions of uracil with the $\omega$-chloroalkyl nitrile ${(Cl-(CH}_2)_n$-CN;n=1, 2, 3, 4) in DMSO under $50-70^circ{C}$ temperature. The 1-$(\omega$-cyanoalkyl)-and 1, 3-bis$(\omega$-cyanoalkyl) uracils were separated either by the fractional crystallization or column chromatography. The antitumor activities for these synthesized compounds were determined against four cell lines (J-82 cell, P388 cell, FM-3A cell and U-937 cell lines). These compounds failed to exhibit any significant antitumor activity.

• YAKHAK HOEJI
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• v.42 no.4
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• pp.345-352
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• 1998

Praecoxin A, an ellagitannin, purified from Alnus hirsuta var.microphlla was evaluated on the antitumor activity. Praecoxin A had the significant cytotoxicity to s ix tumor cell lines: human chronic myelogenous leukemia K-562, human promyelocytic leukemia HL-60, mouse leukemia P388, mouse lymphocytic leukemia L-1210, sarcoma-l8O, mouse lymphoma L5178Y except L-1210. And the most sensitive cell line was K-562 ($ED_{50}=2.43{\mu}g/ml$). The $ED_{50} of praecoxin A against HL-60, P388, L-1210, sarcoma7l8O and L5178Y were 6.28, 8.66, 10.00, 7.01, $9.32{\mu}g/ml$, respectively. Praecoxin A showed the increasing effect in life span by 36.8% on the 1st day after treatment of 10mg/kg in mice bearing sarcoma-180 tumor cells (ascitic form) via NCI (National Cancer Institute, U.S.A.) protocol in vivo assay. As a result, praecoxin A is considered to show the antitumor activity.

• YAKHAK HOEJI
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• v.42 no.4
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• pp.388-394
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• 1998

The lectin from starfish, Asterina pectinifera, was purified and tested for its potential antitumor activity. It was shown to possess considerable toxicity toward various tumor cell lines. Concentration of Asterina pectinifera lectin (APL) at 4mg/$5{\times}10^5$ cells resulted in 28% death of Ehrlich ascites tumor cell, 40% of L929, 60% of A549, and 52% of HeLa cells after 48 hours incubation. Toxicity of APL to L929, Ehrlich ascites, A549, and HeLa cells revealed a reduction in cell viability of approximately 70% at APL concentration of 8mg/$5{\times}10^5$ cells after 48 hours incubation. Administration of APL ($100{\mu}g/day$ or $300{\mu}g/day$) inhibited the growth of Ehrlich ascites cells in vivo. Mice given only Ehrlich cells survived an average of $15{\pm}1$ (S.E.) days. Mice given Ehrlich cells and $100{\mu}g\;or\;300{\mu}g$ APL had 58% and 67% survival, respectively, after 20 days. These results suggest that APL has antitumor activity.