• Title/Summary/Keyword: .Antitumor activity

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Antitumor activity of Trichosanthes kirilowii

  • Ryu, Shi-Yong;Lee, Seung-Ho;Lee, Sang-Un;Lee, Chong-Ock;No, Zaesung;Ahn, Jong-Woong
    • Archives of Pharmacal Research
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    • v.17 no.5
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    • pp.348-353
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    • 1994
  • The activity fractionation upon the MeOH extract of the root of trichosanthes kirilowii led to the isolation of eight cucurbitane tritepense namely cucurbitacin .betha. (I), isocucurbitacin .betha.(II), cucurbitacin D(III), isocucurbitacin D(IV), 3-epi-isocucurbitacin .betha(V), dihydrocucurbitain .betha. (VI), dihydroisocucurgbitachin .betha. (VII) and dihydrocucurbitacin E (VIII), as active principles. All isolates were shown to exhibit significant cytotoxicity against cultured human tumor cells, including A-549, Sk-OV-3, Sk-MEL-2, XF-498 and HCT 15, with an exceptionally high potency.

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Isolation of Antitumor Agent from the Heartwood of Dalbergia odorifera (강진향(降眞香)의 항암활성 성분)

  • Park, Jong-Dae;Lee, You-Hui;Baek, Nam-In;Kim, Shin-Il;Ahn, Byung-Zun
    • Korean Journal of Pharmacognosy
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    • v.26 no.4
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    • pp.323-326
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    • 1995
  • Through bioassay-guided separation of the chemical constituents from the heartwood of Dalbergia odorifera, an 2'-O-methoxyisoliquiritigenin(1) was isolated as cytotoxic principle. 1 showed potent cytotoxic activity against the three kinds of human cancer cell lines (A-549, SK-MEL-2 and SK-OV-3) with similar activity to 5-Fluorouracil.

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Exogenous Natural Glycoprotein Multiple Mechanisms of Anti-tumor Activity

  • Yuan, Hong-Liang;Liu, Xiao-Lei;Dai, Qi-Chang;Song, Hui
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.4
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    • pp.1331-1336
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    • 2015
  • Natural glycoproteins can induce apoptosis of tumor cells and exert anti-tumor activity by immunomodulatory functions, cytotoxic and anti-inflammation effects, and inhibition of endothelial growth factor. Given their prospects as novel agents, sources of natural antitumor glycoproteins have attracted attention and new research directions in glycoprotein biology are gradually shifting to the direction of cancer treatment and prevention of neoplastic disease. In this review, we summarize the latest findings with regard to the tumor suppressor signature of glycoproteins and underlying regulatory mechanisms.

NMR Studies on Antitumor Drug Candidates, Berberine and Berberrubine

  • Jeon, Young-Wook;Jung, Jin-Won;Kang, Mi-ran;Chung, In-Kwon;Lee, Weon-tae
    • Bulletin of the Korean Chemical Society
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    • v.23 no.3
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    • pp.391-394
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    • 2002
  • Berberine and berberrubine, which display antitumor activity, have also demonstrated distinct enzyme-poisoning activities by stabilizing topoisomerase Ⅱ-DNA cleavable complexes. The protoberberine berberrubine differs in chemical structure with berberine at only one position, however, it shows a prominent activity difference from berberine. Solution structures of berberine and berberrubine determined by NMR spectroscopy are similar, however, the minor structural rearrangement has been observed near 19 methoxy or hydroxyl group. We suggest that the DNA cleavage activities of topoisomerase Ⅱ poisons could be correlated with both chemical environments and minor structural change together with hydrophobicity of interacting side chains of drugs with DNA molecule.

Synthesis, Cytotoxicity and Antitumor Activity of 2,3-Diarylcyclopent-2-ene-1-ones

  • Nam, Nguyen-Hai;Kim, Yong;You, Young-Jae;Hong, Dong-Ho;Kim, Hwan-Mook;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • v.25 no.5
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    • pp.600-607
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    • 2002
  • Two series of 2,3-diarylcyclopent-2-ene-1-ones including 2-aryl-3-(2,5-dihydroxyphenyl)cyclopent-2-ene-1-ones (2a∼2f) and 3-aryl-2-(3',4',5'-trimethoxyphenyl)cyclopent-2-ene-1-one (3a∼3j) were synthesized and evaluated for the cytotoxicity against three tumor cell lines; B16F10, HCT116 and A431. It was found that the 3,4,5-trimethoxy substituent was optimal for the bioactivity of compounds in series 2. Meanwhile, compounds in series 3 exhibited the most potent cytotoxicity with 3-aryl ring being 4-methoxyphenyl (compound 3f), (3-hydroxy-4-methoxy)phenyl (compound 3e), or (3-amino-4-methoxy)phenyl (compound 3j).

Study on Antitumor Activity of Bujeongyangeumtang(BJYET) (부정양음양(扶正養陰陽)의 항암활성(抗癌活性)에 관(關)한 연구(硏究)(I))

  • Song, Min-Ho;Choe, Bong-Gyun;Kim, Dong-Hee
    • Journal of Haehwa Medicine
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    • v.9 no.1
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    • pp.169-182
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    • 2000
  • To evaluate the antitumor activity and antimetastatic effects of Bujeongyangeumtang(BJYET), studies were done experimentally. The results were obtained as follows: 1. BJYET extracts exhibited a significant cytotoxicity against A549, SK-MEL-2, SK-OV-3 and B16-BL6 cell lines. 2. The T/C% was 118.2% in BJYET treated group in S-180 bearing ICR mice. 3. BJYET extracts exhibited inefficient adhesive effect of A549, B16-BL6 cell to complex extracellular matrix. 4. BJYET extracts showed a significant inhibition of lung metastasis of B16-BL6 cells in C57BL/6. 5. In vitro neovascularization assays, angiogenesis was significantly inhibited in BJYET treated group than control group. These results suggested that BJYET extracts might be usefully applied for prevention and treatment of cancer.

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Inhibitory Mechanism of a New Antitumor Agent DA125 on DNA Replication (새로운 항암제 DA-125의 유전자 복제 억제 기작)

  • 이상광;김도진;오유택;이상득;우은란;신차균
    • YAKHAK HOEJI
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    • v.43 no.5
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    • pp.623-628
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    • 1999
  • DA-125, a new antitumor agent, was compared with adriamycin, a known DNA intercalator, in terms of inhibitory mechanism of DNA replication by using replicating simian virus 40 (SV40) genome in vivo. In analyzing the SV40 DNA replication intermediates present in cells treated with DA-125, it was not observed to accumulate B-dimers of SV40 DNA which are prominent in adriamycin-treated cells. However, treatment with DA-125 induced dose-dependent formation of DNA-topoisomerase complex which is characteristic of topoisomerase poisons. In addition, DA-125 showed more efficient in inhibiting SV40 DNA replication than adriamycin. Therefore, on the basis of this observation, we suggest that DA-125, a derivative of adriamycin, inhibits DNA replication by blocking topoisomerase activity as a toposomerase poison although adriamycin blocks topoisomerase activity as a DNA intercalator.

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Studies on the Antitumor Activity of Some Crude Drugs (생약(生藥)의 항암성(抗癌性)에 관(關)한 연구(硏究))

  • Han, Dae-Suck;Chung, Bo-Sup;Kim, Young-Choong
    • Korean Journal of Pharmacognosy
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    • v.11 no.1
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    • pp.7-10
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    • 1980
  • Antitumor activity test was achieved with 20 crude drugs which are folkmedicine and recorded in Dong-eu-bo-gam. Three crude drugs showed above 60% effect on life span of mouse and 5 crude drugs showed under 50% effect. After death, body weight was decreased with 3 crude drugs and increased with most other crude drugs, which were tested in this study. The solid cancer tissue weight was decreased slightly with 4 crude drugs.

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Anti-Tumor Metastasis Activity by Extracts of Inonotus obliquus (차가버섯 추출물의 종양 전이 억제 효과)

  • Yoon, Taek-Joon;Moon, Won-Kook;Lee, Kwang-Ho
    • The Korean Journal of Food And Nutrition
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    • v.20 no.3
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    • pp.253-258
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    • 2007
  • In experimental lung metastasis of colon26-M3.1 carcinoma cells, we found that the prophylactic or therapeutic admini-stration of Inonotus obliquus extracts significantly inhibited lung metastasis. In an in vitro cytotoxicity analysis, the extracts did not affect colon26-M3.1 cell growth at concentrations up to 1000 ${\mu}g/m{\ell}$. Peritoneal macrophages that were stimulated with the extracts produced $TNF-{\alpha}$. These data suggest that Inonotus obliquus extract has antitumor activity to inhibit tumor metastasis, and its antitumor effects are partially associated with macrophages activation.

DMNQ S64 exerts antitumor activity on A549 cells via COX-2 inhibition

  • Park, Jeong-Ran;Lim, Eu-Soo;Lee, Seong-Deok;Kim, Sung-Hoon
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.208.1-208.1
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    • 2003
  • We synthesized naphthazarin derivatives from shikonin, a major compound from Lithospermum erythrorhion Sieb et ZUCC. Of derivatives, DMNQ S64, 2-or 6-(l-hydroxyiminoalkyl) effectively showed antitumor activity on A549, human lung cancer cells (IC$\sub$50/= 30 ${\mu}$M). It significantly inhibited prostaglandin E$_2$(IC$\sub$50/= 10 ${\mu}$M). We also confirmed it selectively downregulated the expression of cyclooxygenase 2(COX-2), while it didn't affect COX-1. The induction of apoptosis by DMNQ S64 is underway.

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