• Title/Summary/Keyword: and Antitumor activity

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Studies on the Synthesis and In Vitro Antitumor Activity of the Isoquinolone Derviatives

  • Cheon, Seung-Hoon;Lee, Joon-Yeol;Chung, Byung-Ho;Choi, Bo-Gil;Cho, Won-Jea;Kim, Tae-Sung
    • Archives of Pharmacal Research
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    • v.22 no.2
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    • pp.179-183
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    • 1999
  • 3-Arylisoquinolin-1(2H)-ones (2) are possible bioisosteres of the $5-[4^{l}-(piperidinomethyl)phenyl]-2<$,3-dihydroimidazo[2,1-$\alpha$]isoquinoline (1) which is in clinical evaluation for the treatment of cancer. Structure-activity relationship studies of 3-arylisoquinolin-1(2H)-ones. (2) led to the synthesis of 3-arylquinolin-2(1H)-ones (3). A number of 3-phenyl substituted quinolin-2(1H)-ones were synthesized and tested for their in vitro antitumor activity against four different human tumor cell lines and 3-phenyl-N-benzyl-3,4-dihydroquinolin-2(1H)-one (12) showed the most potent activity.

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Studies on Antitumor Activity and Antimicrobial Activity of Coriolus Versicolor(Fr.)Quel and Ganoderma Lucidum (Fr.)Karst (구름버섯과 영지버섯의 항암효과에 관한 연구)

  • Kim Sung-Hun;Cha Eun-Jung;Hwang Young-Jeong
    • Korean Journal of Human Ecology
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    • v.7 no.3
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    • pp.49-58
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    • 2004
  • The purpose of the study was to verify if or not as funtional food by estimating antitumor activity and antimicrobial activity of Coriolus versicolor(Fr.)Quel and Ganoderma Lucidum (Fr.)Karst. 1. The contents of moisture. crude fiber and crude protein of GL were higher $(18.28\%,\;10.3\%,\;78.4\%)$ than that of CV, but the content of crude lipid GL was higher than that of CV. 2. Inhibitory effects of on the growth of AGS human gastric adenocarcinoma cells and HT-29 human colon adenocarcinoma cell were increased by increasing of concentration in added methanol extracts of CV and GL. 3. Antimicrobial activity on Escherichia col1; Staphylococcus aureus, Salmonella typhimurium existed methanol extracts of CV. Therefore. it is suggested that CV is worth as functional food.

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Studies on Constituents of the Higher Fungi of Korea (XLVI) -Antitumor Components Extracted from the Cultured Mycelia of Lyophyllum decastes-

  • Kim, Hye-Ryoung;Shim, Mi-Ja;Kim, Jung-Woo;Kim, Ha-Won;Lee, Chong-Ock;Choi, Eung-Chil;Kim, Byong-Kak
    • 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.

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Cytotoxic and Apoptotic Activites of Echinomycin Derivative (Echinomycin-7) on P388 Murine Leukemia Cells

  • Jeon, Hyang;Kim, Sung-Su;Kim, Yoon-Suk;Park, Yil-Sung;Kim, Yong-Hae;Choi, Sun-Ju;Kim, Soo-Kie;Kim, Tae-Ue
    • 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.

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Effects of the Antitumor Component, F-D-P, Isolated from Elfvingia applanata on the Immune Response

  • Kim, Young-So;Ryu, Ku-Hyun;Mo, Young-Keun;Lee, Chong-Kil;Han, Seong-Sun
    • 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.

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Biological Evaluation of Korean Medicinal Plants (III)

  • Woo, Won-Sick;Lee, Eun-Bang;Han, Byung-Hoon
    • Archives of Pharmacal Research
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    • v.2 no.2
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    • pp.127-131
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    • 1979
  • The extracts of sixty Korean plants were evaluated for their biological activities such as antitumor activities against Sarcoma 180, Leukemia SN-36 and Ehrlich ascites carcinoma, antimicrobial activities and behavioral observation in mice. The results are tabulate.

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Antitumor Activity of Bifidobacterium adolesentis ATCC-15703 against Sarcoma 180 in Mice (마우스에서 Sarcoma-180에 대한 Bifidobacterium adolesentis ATCC-15703의 항암 효과)

  • Kim, Gyung-Tae;Bae, Hyoung-suk;Baek, Young-Jin;Lee, Hyung-Hoan
    • Microbiology and Biotechnology Letters
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    • v.22 no.3
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    • pp.322-328
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    • 1994
  • Antitumor and immunoadjuvant activities of Bifidobacterium adolesentis ATCC-15703 were investigated against the ascites and solid forms of tumor induced by Sarcoma 180(S-180) in ICR mice. When 100 $\mu$g of the bacterium was intraperitonealy administered in the mice, the survival rate(T/C %) of the mice was 132% for 50 days after the inoculation of S-180, however the increment of their body weights was suppressed. When the 100 $\mu$g was subcutaneously adminis- tratered at the right grion, the suppresion rate of the tumor growth on the 21st day after inoculation of S-180 were 62.3%. Complete supression of the tumor growth was observed from 2 out of 8 test mice. The bacterium itself appeared to have noncytotoxic substance against the S-180 in vitro. The bacteria] administration markedly enhanced the activity of peritoneal macrophages. The num- ber of peritoneal macrophages at one day after the administration of the 100 $\mu$g increased about 8 times as much as that of the control, and the highest activity of acid phosphatase appeared at 2 days.

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Antitumor Activity of Fermented Antler on Sarcoma 180 in Mice (복수암 생쥐에 대한 발효녹용의 항암작용)

  • Kim, Dong-Hyun;Han, Sang-Bum;Yu, Ki-Ung;Kim, Yu-Suk;Han, Myung-Joo
    • YAKHAK HOEJI
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    • v.38 no.6
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    • pp.795-799
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    • 1994
  • Some components and antitumor effect of antler and fermented antler with Bacillus P-92 were determined. By fermenting the antler with Bacillus P-92, the amount of free amino acids, polypeptides and other compounds were increased. The free amino acid of the fermented antler was 6-fold higher than those of the untreated antler. Sarcoma 180 cells were intraperitoneally implanted into ICR mice to determine the effect of fermented antler and untreated antler on life span prolongation. The life span of ICR mouse treated with antler and fermented antler were prolonged to 24.4% and 39.2%(p<0.05), and survival rates were 22% and 33%, respectively. In addition, the induction of neutrophil was 2.3-fold and 3.4-fold, respectively.

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Antitumor Activity of Gamdutang Aqua-Acupuncture Solution (감두약침액의 암세포 성장 저해 효과)

  • 조경희;한상훈;임종국;손윤희;이임태;남경수
    • Journal of Life Science
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    • v.9 no.6
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    • pp.677-683
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    • 1999
  • Gamdutang aqua-acupuncture solution (GAS), Gamdutang water-extracted solution (GWS) and Dae-Gamdutang aqua-acupuncture solution (DGAS) were prepared and tested for antitumor activities. It was shown to possess considerable toxicity toward various tumor cell lines. Concentration of 5 $\times$ and 10$\times$ of GAS resulted in more than 70% inhibition of growth in Ehrlich ascites tumor cells (EATC), Hepa1c1c7 and A549. GAS at concentrations of 5$\times$ and 10$\times$ revealed more than 60% inhibition in HeLa. GWS showed more than 50% inhibition of growth with EATC and HeLa at concentrations of 5$\times$ and 10$\times$, respectively. Toxicity assay with GWS in Hepa1c1c7 and A549 revealed that more than 80% inhibition of growth at the concentration of 5$\times$ and 10$\times$. In morphological study, the number of cells were decreased, and the shape of cells was round-form in EATC, Hepa1c1c7, A549, HeLa with GAS.

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Antitumor activity of Bacillus subtilis SW-1 isolated from Jeotgal (젓갈에서 분리한 Bacillus subtilis SW-1의 항암활성)

  • 박종기;조용운;최영우;정영기;갈상완
    • 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.