• Title/Summary/Keyword: .Antitumor activity

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Antitumor compounds from fruiting bodies of cultivated fungus of Paecilomyces japonica

  • Nama Ryu;Lim, Soon-Sung;Jung, Sang-Hoon;Cho, Sae-Yun;Shin, Kuk-Hyun
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1998.11a
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    • pp.185-185
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    • 1998
  • As part of our continuing attempts to evaluate biologically active compounds from fruiting bodies of cultivated fungus of Paecilomyces japonicus Yasuda, we conducted series of experiments on various fractions and compounds isolated by systematic fractionations. Our main efforts were concentrated on searching for compounds showing antitumor activities, which were tested on mice carrying Sarcoma-180 ascitic tumor. The antitumor activity was assessed by the life spans after these mice were administered Lp. with test compounds for consecutive 20 days. One of two pure compounds, which we have isolated to date, demonstrated significant prolongation of life span. ( Mean Survival Time: 30.3 days compared to that of control: 23.6 days). Structural analysis showed that this compound corresponds to D-mannitol. On the other hand, Ergosterol, another isolated pure compound didn't show efficient antitumor activity. We also obtained water-soluble fractions containing protein-bound polysaccharides and n-butantol fractions, which showed strong antitumor activities, 35.4(150%) and 32.1(136.0%) days of MST, respectively. In SRB assay, however, the test materials didn't show any toxic effects, but the level of acid phosphatase increased significantly when they were applied in cultured macrophage in vitro. Therefore, we concluded that antitumour activities might be attributed to immunostimulating rather than cytotoxic effects. Further experiments are underway to purify and structurally characterize new antitumour compounds from the active fractions.

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Structure and Antibiotic Activity of a Porcine Myeloid Antibacterial Peptide, PMAP-23 and its Analogues

  • Shin, Song-Yub;Kang, Joo-Hyun;Jang, So-Yun;Kim, Kil-Lyong;Hahm, Kyung-Soo
    • BMB Reports
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    • v.33 no.1
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    • pp.49-53
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    • 2000
  • PMAP-23 is a 23-residue antimicrobial peptide derived from porcine myloid cells. In order to investigate the effects of two Pro residues at positions 12 and 15 of PMAP-23 on antibiotic activity, two analogues in which Ala was substituted for Pro residue at position 12 or 15 were synthesized. $Pro^{12}{\rightarrow}Ala$ (PMAPl) or $Pro^{15}{\rightarrow}Ala$(PMAP2) substitution in PMAP-23 caused a significant reduction on antitumor and phospholipid vesicle-disrupting activities, but did not cause a significant effect on antibacterial activity. PMAP-23 displayed the type I ${\beta}-turn$ structure with a negative ellipticity at near 205 om in SDS micelle, whereas PMAP1 and PMAP2 had a somewhat ${\alpha}-helical$ propensity in TFE solution, as compared to PMAP-23. These results suggest that two Pro residues of positions 12 and 15 in PMAP-23 play important roles in the formation of ${\beta}-turn$ structure on lipid membrane and its ${\beta}-turn$ structure may be essential for antibiotic activity including phospholipid vesicle-disrupting property.

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Studies on Antitumor Components of Collybia confluens (밀버섯의 항암성분에 관한 연구)

  • Kim, Sook-Hee;Kim, Jin-Sook;Jin, Mi-Rim;Kim, Ha-Won;Choi, Eung-Chil;Kim, Byong-Kak
    • Korean Journal of Pharmacognosy
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    • v.24 no.4
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    • pp.267-281
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    • 1993
  • To find antitumor components from higher fungi, the mycelia of Collybia confluens (Pers. ex Fr.) Kummer were cultured in artificial media. For efficient production of the mycelia, the influences of various modifications of culture conditions were examined. A water-soluble protein-bound polysaccharide fraction, Fr. A, was obtained from the mycelia by hot water extraction. When Fr. A was purified and fractionated by DEAE-cellulose and Sepbadex G-200 gel filtration chromatographies into four fractions which were designated B, C, C-I and C-II. The tumor inhibition ratios of these fractions ranged from 46% to 75% against the solid forms of sarcoma 180 in ICR mice at doses of 20 and 50 mg/kg/day when given intraperitoneally. Especially, Fr. C which was named Collyban(CB) exhibited a marked life-prolonging effect of the mice against ascitic forms of sarcoma 180 at a dose of 50 mg via i.p. administration. To extend spectra of the antitumor activities and eliminate the effects of allograft rejection, the characterization of antitumor effects of CB was performed in syngeneic host-tumor systems. It did not show any antitumor activity against L1210 murine leukemia in $CD_2Fl$ mice but prolonged their life span against ascitic forms of $MM_{46}$ carcinoma in $C_3H/He$ mice. Also it exhibited antitumor activity against human cervical cancer HeLa cells that were xenografted into nude mice having BALB/c genetic backgrounds by the i.p. injection at a dose of 100 mg/kg/day. In order to characterize the antitumor components, CB was examined by chemical analysis. It was acidic protein-bound polysaccharides composed of 31% polysaccharide, 27% protein and 3% hexosamine. CB was fractionated into two fractions, Fr. C-I(M.W.: 500 Kd) and Fr. C-II(M.W.:30 and 8 Kd) by Sephadex G-200 gel filtration chromatography.

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Enhanced Antitumor Effect of Curcumin Liposomes with Local Hyperthermia in the LL/2 Model

  • Tang, Jian-Cai;Shi, Hua-Shan;Wan, Li-Qiang;Wang, Yong-Sheng;Wei, Yu-Quan
    • Asian Pacific Journal of Cancer Prevention
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    • v.14 no.4
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    • pp.2307-2310
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    • 2013
  • Curcumin previously was proven to inhibit angiogenesis and display potent antitumor activity in vivo and in vitro. In the present study, we investigated whether a combination curcumin with hyperthermia would have a synergistic antitumor effect in the LL/2 model. The results indicated that combination therapy significantly inhibited cell proliferation of MS-1 and LL/2 in vitro. LL/2 experiment model also demonstrated that the combination therapy inhibited tumor growth and prolonged the life span in vivo. Furthermore, combination therapy reduced angiogenesis and increased tumor apoptosis. Our findings suggest that the combination therapy exerted synergistic antitumor effects, providing a new perspective fpr clinical tumor therapy.

Antitumor Activity of Peptide Fraction from Traditional Korean Soy Sauce

  • Lee, Hong-Jin;Lee, Ki-Won;Kim, Kyoung-Heon;Kim, Hyun-Kyung;Lee, Hyong-Joo
    • Journal of Microbiology and Biotechnology
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    • v.14 no.3
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    • pp.628-630
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    • 2004
  • Antitumor activities of a peptide fraction isolated from traditional Korean soy sauce (SSP) were investigated in vitro and in vivo using cancer cell lines and F9 teratocarcinoma-bearing BALB/c mice. SSP exerted a dose-dependent antiproliferative effect on P388D1 mouse lymphoma, F9 mouse teratocarcinoma, and DLD-l human colon cancer cells with $IC_{50}$ values of 11, 50, and $50\mug/ml$, respectively. Tumor growth in F9 teratocarcinoma-bearing BALB/c mice, orally administered with 80 and 200 mg/kg/day of SSPs, was inhibited 10.3% and 52.4%, respectively, and survival days increased by 11.9% and 22.1%, respectively, compared to the control group. The results of antitumor activities exerted by SSP in vitro and in vivo suggest the feasibility of using SSP as an antitumor agent.

Flow Cytometrical Analysis of the Antitumor and Immunomodulatory Activities of GLB-A and GLB-B, the Protein-polysaccharide Fractions of the Growing Tips of Ganoderma Lucidum (영지버섯 생장점 단백다당체 GLB-A, GLB-B의 항암효과 및 면역 활성에 관한 유세포 분석학적 연구)

  • Oh, Jung-Yeon;Chung, Kyeong-Soo
    • YAKHAK HOEJI
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    • v.42 no.5
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    • pp.487-493
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    • 1998
  • In the previous study we described the antitumor effect of GLB, a protein-polysaccharide fraction separated from the growing tips of Ganoderma lucidum, against sarcoma 18 0 solid tumor in ICR mice. In this study, we separated an acidic protein-polysaccharide fraction, GLB-A, and a basic protein-polyaccharide fraction, GLB-B, from GLB by differential precipitation, and elucidated their antitumor and immunomodulatory activities. When ip injected at the dose of 50mg/kg/day into the ICR mice, GLB-A and GLB-B inhibited the growth of ip implantated sarcoma 180 cells by 32.4% and 21.0%, respectively. Of these, GLB-A increased the % lymphoblast in the spleen of the tumor-bearing and the normal mice by 20.9% and 123.0%, and the CD4/CD8 ratio by 73.3% and 22.4%, respectively. GLB-A also increased the expression of CD25 (IL-2 receptor alpha ch0ain) in normal mice by 82.0%. These results strongly suggest that GLB-A is a promising candidate for antitumor immunomodulatory medicine.

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Effects of Buthus martensi Karsch on tumor promotion in two-stage carcinogenesis in mice (전갈(全蝎)이 노화(老化)에 따른 2단계(段階) 발암화(發癌化) 과정(過程)에 미치는 영향(影響))

  • Jeong, In-Chae;Jeong, Ji-Cheon;Yoon, Cheol-Ho
    • The Journal of Internal Korean Medicine
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    • v.21 no.2
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    • pp.251-257
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    • 2000
  • To clarifiy the activating effects of Buthus martensi Karsch(BMK) on tumor promotion in two-stage carcinogenesis in mice was investigated. In vivo system, BMK was seen to gave an inhibitory activity on TPA-induced mouse ear edema. In addition, the BMK was proved to have antitumor-promoting activity in two-stage mouse skin carcinogenesis induced by DMBA and two-stage mouse lung carcinogenesis induced by 4-NQO as a initiator plus TPA and glycerol as a promoter. Moreover, BMK significantly exhibited an cytolytic effect in HepG2 cells and showed significant antitumor activity against Sarcoma-180 bearing mice by oral administration. These results suggest that BMK could be effective in adjuvant chemotherapy for human cancer.

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Isolation and Evaluation of an Antitumor Constituent from Pyrolae Herba (녹수초의 항암활성물질의 분리 및 항암력 평가)

  • Bae, Ki-Hwan;Kim, Hwan-Mook;Lee, Sang-Myung
    • YAKHAK HOEJI
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    • v.40 no.2
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    • pp.225-229
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    • 1996
  • The cytotoixic effect of Pylorae Herba (Pyrola japonica Klenze) against L1210 and K-562 cells was studied in vitro. The methanolic extract of Pylorae Radix was add ed to the culture of L1210 cells and K-562 cells for the cytotoxic activity and the ED50 values of hexane, ethylacetate, buthanol and water fractions from methanolic extract were determined using MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazoliumbromide) assay. The active constituent isolated by bioassay guided fractionation followed by purification gave rise to a yellow needle crystal and was clarified to be chimaphilline by the comparison with the published data. The average life spans with it were not prolonged significantly on tumor growth in hybrid female mouse (BDF1-KIST) inoculated subcutaneously with P388 cells.

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Boron Trifluoride Etherate on Silica-A Modified Lewis Acid Reagent (VII). Antitumor Activity of Cannabigerol Against Human Oral Epitheloid Carcinoma Cells

  • Baek, Seung-Hwa;Kim, Young-Ok;Kwag, Jung-Suk;Choi, Kyw-Eun;Jung, Woo-Young;Han, Du-Seok
    • Archives of Pharmacal Research
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    • v.21 no.3
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    • pp.353-356
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    • 1998
  • Geraniol (1), olivetol (2), cannabinoids (3 and 4) and 5-fluorouracil (5) were tested for their growth inhibitory effects against human oral epitheloid carcinoma cell lines (KB) and NIH 3T3 fibrobalsts using two different 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay and sulforhodamine B protein (SRB) assay. Cannabigerol (3) exhibited the highest growth-inhibitory activity against the cancer cell lines.

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Development of Anticancer Agents from Korean Medicinal Plants (Part 8). - Cytotoxic Activity of Taraxaci Herba Extract against Human Skin Melanoma Cells - (한국산 생약으로부터 항암물질의 개발(제 8보) - 포공령 추출물이 인체 피부흑색종세포에 미치는 세포독성작용 -)

  • Oh, In-Kio;Yoo, Eun-Ah;Han, Du-Seok;Kang, Kil-Ung;Baek, Seung-Hwa
    • Korean Journal of Pharmacognosy
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    • v.29 no.3
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    • pp.198-203
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    • 1998
  • In the present study, we have evaluated cytotoxic effects of Taraxaci herba extract on human skin melanoma cells. The light microscopic study showed morphological changes of the treated cells. Disruptions in cell organelles were determined by calorimetric methods: MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide), NR (Neutral red) and SRB (Sulforhodamine B protein) assay. These results suggest that Taraxaci herba retains a potential antitumor activity.

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