• 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.

• Korean Journal of Pharmacognosy
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• v.17 no.1
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• pp.39-48
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• 1986

To find antitumor components in the shake-cultured mycelia of Volvariella bombycina, the mycelia were extracted with hot water. After the extract was dialyzed and freeze-dried, a protein-polysaccharide fraction was obtained and examined for antitumor activity against the solid form of sarcoma 180 in ICR mice. It showed 60.3% inhibition ratio at a dose of 20mg/kg/day for 10 days. It was found to consist of a polysaccharide moiety and a protein moiety. After gel filtration on Sepharose 4B, Fraction B was obtained and showed the highest inhibition ratio of 71.1%. When the antitumor component was examined for immunopotentiating activity, it was found to increase the macrophage accumulation in the peritoneal cavity as well as the antibody production of the spleen cells of the mice.

• Natural Product Sciences
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• v.2 no.1
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• pp.43-47
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• 1996

Macrophages play an important role in host defense against tumors by killing tumor cells. Our work is directed toward studying the effect of the extracts of Salvia plebeia on induction of antitumor activity in macrophages, since it has been usezd as a folk-medicine for the treatment of hepatitis and tumors. The ability of macrophage treated with the plant extracts to inhibit the growth of tumor cells was assessed. The Extracts of the plant induced antitumor activity and could enhance the tumoricidal activity of macrophages when used in combination with $IFN-{\gamma}$. These results suggest that Salvia plebeia extract contain immunomodulatory factors responsible for the induction of the antitumor activity.

• Microbiology and Biotechnology Letters
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• v.22 no.1
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• pp.45-51
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• 1994

Antitumor polysaccharides were known to activate complement system and to increase specific serum proteins in mouse, and researcher reported that antitumor activity of polyasccharides might be correlated with their biological properties such as activation of complement system and increase of specific protein $L_{A}$, $L_{B}$ and $L_{C}$ within the mouse serum. In case of several Ganoderma lucidum, there was no correlation between their antitumor activities and their bioloical properties, but the antitumor activities against sarcoma 180 of the alkali extracted crude polysaccharide fractions of the Ganoderma lucidum IY 009. AS, T, AI and M were correlated with their bioloical properties such as anticomplementary activity and intensity of mouse serum protein $L_{A}$, $L_{B}$ and $L_{C}$.

• IMMUNE NETWORK
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• v.2 no.2
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• pp.115-124
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• 2002

Background: The chemical characteristics of the exo-secretion from Phellinus linteus (referred to as exo-secretion) including the compositions of amino acids and monosaccharides were investigated. In addition, cytotoxicity of the exo-secretion on 5 tumor cell lines derived from human cancers and its antitumor activity against ascitic sarcoma-180 cells were examined. Methods: The antitumor activity of exo-secretion from Phellinus linteus was determined by measuring parameters including tumor weight, life span of mice, chemotatic activity of leukocytes, counts of immune cells, and activity of cytokines. Results: The exo-secretion from Phellinus linteus showed no direct cytotoxicity to the five tumor cell lines tested, but it had a strong antitumor activity against sarcoma-180 cells in ICR mice as measured by tumor weight and life span of mice. The exo-secretion stimulated the chemotaxis of leukocytes and production of immune cells and cytokines. Conclusion: These results suggest that the exo-secretion from Phellinus linteus do not act as a direct cytotoxic substance to cancer cells but as an immunomodulator.

• BMB Reports
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• v.32 no.6
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• pp.561-566
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• 1999

CA(1-8)-ME(1-12) [CA-ME], composed of cecropin A(1-8) and melittin(1-12), is a synthetic antimicrobial peptide having potent antibacterial and antitumor activities with minimal hemolytic activity. In order to investigate the effects of the flexible hinge sequence, Gly-Ile-Gly, of CA-ME on antibiotic activity, CA-ME and three analogues, CA-ME1, CA-ME2, and CA-ME3, were synthesized. The Gly-Ile-Gly sequence of Ca-ME was deleted in CA-ME1 and replaced with Pro and Gly-Pro-Gly in CA-ME2 and CA-ME3, respectively. CA-ME1 and CA-ME3 showed a significant decrease in antitumor activity and phospholipid vesicle-disrupting ability. However, CA-ME2 showed similar antitumor and vesicle-disrupting activities, as compared with CA-ME. These results suggest that the flexibility or ${\beta}$-turn induced by Gly-Ile-Gly or Pro in the central part of CA-ME may be important in the electrostatic interaction of the N-terminus cationic ${\alpha}$-helical region with the cell membrane surface and the hydrophobic interaction of the C-terminus amphipathic ${\alpha}$-helical region with the hydrophobic acyl chains in the cell membrane. CA-ME3 exhibited lower antitumor and vesicle-disrupting activities than CA-ME and CA-ME2. This result suggests that the excessive ${\beta}$-turn structure caused by the Gly-Pro-Gly sequence in CA-ME3 seems to interrupt ion channel/pore formation in the lipid bilayer. We concluded that the appropriate flexibility or bilayer. We concluded that the appropriate flexibility or ${\beta}$-turn structure provided by the central hinge is responsible for the effective antibiotic activity of the antimicrobial peptides with the helix-hinge-helix structure.

• Archives of Pharmacal Research
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• v.20 no.3
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• pp.264-268
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• 1997

In order to study the structure-activity relationship of 7, 8-dimethoxy-2-methyl-3-(4, 5-methylenedioxy-2-vinylphenyl)isoquinoline-1(2H) -one (2), which has exhibited significant antitumor activity, chemical modifications of 2 were performed to yield the corresponding products (3-7). Further systematic uses of an efficient procedure for the synthesis of 3-arylisoquinoline derivatives produced the substituted compounds (9a-9g), which were tested for in vitro antitumor activity against five different human cancer cell lines.

• Microbiology and Biotechnology Letters
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• v.21 no.3
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• pp.247-255
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• 1993

Antitumor activity of Lactobacillus casei YIP 9018(LC9018) was studied in mice by using sarcoma 180(S-180) and Lewis lung carcinoma (3LL). Following the eatablishment of in vivo tumor models such as ascites form S-180, solid form S-180 and 3LL for estimating antitumor activity of Lactobacilli, optimal dose and injection route of heat-killed LC9018 for supperssion of local tumor were examined. Administration of 100ng/mouse of LC9018 significantly inhibited the growth of ascites form S-180, solid form S-180 and 3LL.

• Archives of Pharmacal Research
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• v.25 no.4
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• pp.457-462
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• 2002

Oregonin, a diarylheptanoid derivative from Alnus hirsuta Turcz, Betulaceae, was evaluated for its antitumor activity. Oregonin, known to have an antitumor function, and is a novel immunomodulator, which may augment macrophage activity. MTT assays and NO production tests were performed in order to investigate the cytotoxicity of oregonin in tumor cells and to examine its influence on macrophage in detail. In this study, the tumoricidal activity was also evaluated by a MTT assay. The cytotoxicity measurements in the oregon in-treated group both in vitro and in vivo showed a significant difference from that of the control group. In vivo, oregonin significantly increased NO production in a dose-dependent manner, and in vitro, the thioglycolate-induced inflammatory macrophages increased NO production in a dose-dependent manner after incubation. These results suggest that oregonin reacts with both the inflammatory and non-inflammatory macrophages in a similar way.

• Toxicological Research
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• v.16 no.4
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• pp.263-267
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• 2000

The cytotoxic and antitumor activity of 23,24-dihydrocucurbitacin D (dhc D) isolated from Bryonia alba L. was examined. Our results showed that dhc D strongly inhibited the viability of the cultured cancer cells, A-549, COLO 205, SK-MEL-2, and L121O. It also exhibited effective antitumor activity in ICR mice, which had been intra peritoneally implanted with sarcoma 180 ascites tumor cells. The dhc D also strongly inhibited the viability of immortalized macrophages RAW 264.7, but not normal peritoneal macrophages. These results indicate that dhc D has antiproliferative effect on cancer cells and it may more sensitive on immortalized cells than normal cells.