• Proceedings of the PSK Conference
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• 2002.10a
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• pp.357.1-357.1
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• 2002

Three-dimensional quantitative activity relationship (3D-QSAR) study for a series of arylsulfonylimidazolidinone derivatives with antitumor activity was conducted using comparative molecular field analysis (CoMFA) and comparative molecular similarity indices anaysis (CoMSIA). The in vitro cytotoxicity against human lung carcinoma (A549) exhibited a strong correlation with steric and electrostatic factors of the molecules. (omitted)

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.171.1-171.1
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• 2003

·The potent antitumor activities of 3-arylisoquinolines promoted us to explore the structure-activity relationship of these compounds. A series of 3-arylisoquinoline derivatives were evaluated for antitumor cytotoxicity against human lung tumor cell (A 549). For the next stage, we decided to prepare the constrained form of 3-arylisoquinolines as indeno[1,2-c]isoquinolines. As a result, diverse spectrum against human tumor cell lines was obtained. In order to study structure-activity relationship (SAT) of these compounds the comparative molecular field analysis (CoMFA) was carried out. (omitted)

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.188.1-188.1
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• 2003

The antiparasitic agent apicidin, which was recently isolated from cultures of Fusarium Pallidoroseum, belongs to a rare group of cyclictetrapeptide fungal metabolites. Apicidin inhibits protozoal HDAC and is orally active against Plasmodium berghei malaria in mice. The biological activity of apicidin appears to be attributable to inhibition of apicomplexan HDAC at low nanomolar concentrations. In the present, we have worked about the synthesis of new apicidin derivatives and discovered that apicidin and some derivatives have mild antitumor activity. (omiited)

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.233.2-233.2
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• 2002

Apio nucleosides whose 4'-hydroxymethyl group moves to 3'-position exhibit interesting biological activity such as antitumor or antiviral activity. On the other hand. neplanocin A is the representative of the carbocyclic nucleosides and has been recognized as a potent antitumor and antiviral agent. Based on these findings. it was of great interest to design apio neplanocia A which combined the properties of apio nucleosides and neplanocin A. (omitted)

• 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)

• Korean Journal of Pharmacognosy
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• v.15 no.2
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• pp.61-73
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• 1984

To investigate antitumor component of Lyophyllum decastes, the aqueous extract of its shake-cultured mycelia was subjected to antitumor test against sarcoma 180 cells implanted in ICR mice. The extract showed an inhibition ratio of 65.4% and was found to consist of a polysaccharide moiety and a protein moiety. After purification with DEAE-Sephadex A-50 ion exchange chromatography, Fraction D showed the highest inhibition ratio of 75.7%. The antitumor constituent was examined for immunoaccelerating activity and was found to increase macrophage accumulation in the peritoneal cavity and plaque forming cells of the spleen cells. It was named lyophyllan after the genus name.

• Journal of Life Science
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• v.7 no.2
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• pp.149-159
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• 1997

Chitin, a linked polysaccharide composed of 2-acetamido-2-deoxy-$\beta$-D-glucopytanose residues, is distributed widely in nature. It has been utilized on various application field due to the development of chitin derivatives such as chitosan, partial deacetylated chitin, carboxylmethyl chitin, sulfated chitin, and so on. Chitin and chitosan have been recently interested in antitumor and antimicrobial activities, because of a powerful tumor inhibitory effect against experimental mouse tumors. Especially, the oligosaccharides obtained by partial degradation of them exhibited a remarkable antitumor effect against sarcoma 180, MM 48 and Meth Asolid tumors and antimetastatic effect against Lewis lung carcinoma in mice. This review describes on antitumor effects of chitin, chitosan and their oligosaccharides by their mechanism of action involving enhancement of immunological system.

• Journal of Life Science
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• v.14 no.5
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• pp.815-820
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• 2004

A bacterum containing antitumor activity was isolated from traditional korean food, Jeotgal. Through the 16s rRNA sequence analysis, the bacterium was identitied as a strain of Bacillus subtilis SW-l. The best culture condition for antitumor activity of the bacterium is 3% of soluble starch and 1 % of yeast extract as corbon and nitrogen sources, respectively. Cytotoxicitic concentrations of the culture supernatant of B. subtilis SW-1 against cancer cell lines, A549 and SK-OV3 were 30 ul/ml and 40 ul/ml, respectively, as $IC_{50}$/ values. In DNA fragmentation assay, the culture supernatant showed the programmed cell death (apoptosis) to cause degrading the chromosomal DNA like ladder. Taken together, the culture supernatant of the B. subtilis SW-1 has some possibility to be used as an antitumor agent.

• BMB Reports
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• v.31 no.6
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• pp.560-564
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• 1998

Echinomycin-7 is an echinomycin derivative, Smethylated sulfonium perchlorate of echinomycin. We studied the in vitro cytotoxicity and in vivo antitumor activity of echinomycin-7 against P388 leukemia cells and compared the results with echinomycin. With respect to the cytotoxic effects, echinomycin-7 had cell line-dependent $IC_{50}$ values while echinomycin had similar values to several tumor cell lines. Also, in vivo antitumor activities were observed in tumor-bearing mice treated with both agents, which showed that echinomycin-7 had a broad therapeutic dose range. We also observed the apoptosis on leukemia cells treated with echinomycin-7 which exihibited the ladder pattern of DNA on electrophoresis. In addition to apoptosis, echinomycin-7 arrested $G_1/S$ phases of the cell cycle at the same time. We then examined the signaling pathway of echinomycin-7-induced apoptosis and showed that ERK of the MAP kinase family was activated and translocated into the nucleus by echinomycin-7 stimulation. This study suggests that echinomycin-7 acts as an antitumor agent through in vitro cytotoxicity and has in vivo antitumor activity against leukemia cells, and that the echinomycin-7- induced apoptosis might involve signal transduction via MAP kinases.

• Korean Journal of Pharmacognosy
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• v.25 no.4 s.99
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• pp.348-355
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• 1994

An antitumor component, F-D-P, was purified from the hot water extract of the carpophores of Elfvingia applanata by precipitation with ethanol, dialysis, and passage through a column of DEAE-cellulose ion exchange. F-D-P inhibited the growth of Sarcoma 180 in mice showing the tumor inhibition ratio of 88.3% in doses of 20 mg/kg for ten days. Chemical analysis of F-D-P showed that it was composed of polysaccharide(65.3%) and protein(6.5%0, and that the monosaccharides consisting of the polysaccharide was glucose(89.1%) and mannose(10.9%). The immunomodulatory activities of F-D-P were explored by determining its effect on the proliferation of the whole and subpopulations of lymphocytes, and on the generation of natural killer(NK) cell activity in vitro. F-D-P was mitogenic to total lymphocytes and B cells, but not to purified T cells, even in the presence of accessory cells. F-D-P did not increase NK cell activity when added to cultures of resting lymphocytes. From these results, it is clear that F-D-P modulates primarily the humoral immune responeses.