• Proceedings of the PSK Conference
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• 2002.10a
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• pp.233.3-234
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• 2002

SB31, an extract of Pulsatilla koreana, has been tried as an antitumor agent by traditional medicine pratitioner in Korea for the past 30 years, SB31 was evaluated for cytotoxic and antitumor activity against a variety of cancer cell lines. The SB31 exhibited 5-6 fold less cytotoxic activity against normal mononuclear cells (ED$\sub$50/. 1.1 mg/$m\ell$) than against cancer cell lines (ED$\sub$50/ 0.14-0.19mg/$m\ell$). (omitted)

• Archives of Pharmacal Research
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• v.17 no.2
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• pp.60-65
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• 1994

Reaction of c-chloro-9-benzyl-8-(methylthio)purine 3 with primary amines afforoded, the comesponding 6-(substitutedamino)purines 4a-g. The latter products when methylated with methyl iodide yielded smoothly $N^3$-methyl purinium iodide salts 5a-f rather than the probable $N^1\;and\;N^7$-derivatives. 9-Benzyl-3-methyl-6-(methylmino)-8-(methylthio)purine 8 was obtained upon treating the purinium iodide 5a with alkali. Most of the synthesized compounds were screened for their antitumor activity.

• 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.

• 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.

• The Korean Journal of Mycology
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• v.11 no.1
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• pp.35-37
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• 1983

To investigate antitumor components in Korean higher fungi, the carpophores of Pholiota squarrosa belonging to the family Strophariaceae were collected and extracted with hot water. A protein-bound polysaccharide fraction was obtained by adding ethanol to the extract and by dialyzing through Visking tube. The fraction was examined for antitumor activity against sarcoma 180 implanted in mice. It showed an inhibition ratio of 78.7% at the dose of 20mg/kg/day. The tumor in two of the ten mice was completely regressed. The chemical analysis of the antitumor fraction by Anthrone and Lowry-Folin methods showed that it consisted of 42% polysaccharide and 55% protein. The enzyme fraction of the carpophores showed no proteolytic activity on casein.

• 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.

• The Journal of Internal Korean Medicine
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• v.24 no.2
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• pp.315-328
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• 2003

This study was performed to investigate the effect of Bunsimgieum on antitumor effect after sarcoma-180 cells transplantation into peritoneal cavity or left groin and immune responses on the depressed immunity induced by methotrexate in mice. The Bunsimgieum extract of 10mg/kg was orally administered 14 days for antitumor effects and 21 days for immune responses. 50% inhibitory concentration($IC_{50}$) of SUN-1, SUN-C4, and SUN-396 cancer cell, mean sunvival days and body weight of tumor bearing mice, and growth of tumor mass for antitumor effect; delayed type hypersentivity, hemagglutinin titer, hemolysis titer, rosette forming cells, natured killer cell activity, lymphocyte transformation, productivity of interleukin-2, and phagocytic activity for their immune responses were measured in ICR mice. Significance in antitumor effect is noted in the enlongation of mean life days and inhibition of tumor growth(p<0.01, respectively). Significance of immune responses is also noted in hemolysis titer, lymphocyte transfumotion, IL-2 productivity, phagocytic activity, and natural killer cell activity at E/T ratio 100:1(p<0.01, respectively). Significant in rosette cell formation was seen at dosage of 20mg/kg(p<0.01). However, Difference of body weight as antitumor effect, delayed type hypersensitivity, and hemagglutinin titer were not shown significantly. According to the above results, it could be suggested that Bunsimgieum has prominent antitumor and immunity enhancing effect.

• Korean Journal of Pharmacognosy
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• v.29 no.1
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• pp.22-27
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• 1998

This study was carried out to develop antitumor agents based on effects of the ethyl acetate soluble fraction of the methanolic extract of Lonicerae flos on human oral epitheloid carcinoma cells. Human oral epitheloid carcinoma cells were cultured in RPMI-1640 media containing 10% fetal bovine serum, antibiotic, and fungizone. After incubation for 24 hrs, the cells were treated with A, B, C, D, and E fractions for 48hrs under the same condition. MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide), NR (Neutral red) and SRB (Sulforhodamine B protein) assay were performed. The light microscopic findings were observed by inverted microscope. In MTT assay, fraction B was shown significant antitumor activity (P<0.001), fraction E was shown significant antitumor activities (P<0.05), but the other fractions were not shown. In NR assay, fraction B was shown significant antitumor activity (P<0.001). In SRB assay, fractions B was shown significant antitumor activities (P<0.01). fractions A and D were shown significant antitumor activities (P<0.05). but the other fractions were not shown. In light microscopy. the fraction B of the ethyl acetate soluble fraction of the methanolic extract of Lonicerae flos showed the highest antitumor activity. These finding suggested that fraction B possessed the most antitumorous agent.

• Journal of Ginseng Research
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• v.29 no.4
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• pp.176-181
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• 2005

Our previous reports demonstrated that ip. administration of Korean red ginseng acidic polysaccharide (RGAP) exerts antitumor activity In mice. The present study was carried out to compare the effects of ip. and p.o. routes of administration of RGAP on either normal or tumor-bearing BALB/c mice. RGAP was administered either ip. or p.o. at doses of 100, 300, 500, 1000 mg/kg for 1 or 5 weeks. Peritoneal macrophages from mice treated with RGAP p.o. at a dose of 300 mg/kg either for 1 or 5 weeks did not exhibit growth inhibition activity toward WEHI-I64 tumor cells. However, administration of RGAP at a dose of 600 mg/kg for both 1 and 5 weeks increased the antitumor activity of macrophages. Oral administration of RGAP (600 mg/kg) for 5 weeks and ip. administration of RGAP (300 mg/kg) for 1 week resulted in antitumor activities of $40\%$ and $45\%$, respectively, indicating that the effect of i.p. injection is more potent 2 and 5 times than that of p.o. one in terms of dose and duration, respectively. Tumor inhibition rates of RGAP at doses of 300, 500, 1000 mg/kg in mice transplanted with B16-F10 melanoma were 4.4, 12.0, and $45.4\%$, respectively, meaning that p.o. dose higher than 500 mg/kg possess marked antitumor activity. The results above suggests that p.o. administration of RGAP also show antitumor activity in vivo depending on the dose.