• Title/Summary/Keyword: Antitumor agent

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Studies on the Hemolytic Mechanism of Antitumor Platinum Complex (항암성 백금화합물의 용혈독성기전에 관한 연구)

  • 최병기;박영숙;정세영
    • Environmental Analysis Health and Toxicology
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    • v.8 no.3_4
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    • pp.33-41
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    • 1993
  • This study was designed to determine the hemolytic mechanism of antitumor agent tetraphosphine platinum (II) complex (RC-1), which was synthesized recently. Erythrocytes treated with RC-1 showed concentration and time dependent lipid peroxydation, methemoglobin synthesis and hemolysis. And also treatment of radical scavengers showed the inhibitory effect of hemolysis and the decrease of malondialdehyde levels in RC-1 treated erythrocytes. So, the mechanism of hemolysis was considered to be the generation of free radicals, methemoglobin synthesis and the lipid peroxidation of phospholipid which composed of erythrocyte membrane.

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Efficient Synthesis of 2-Substituted 2,3-Dihydro-4-quinolones as Potential Intermediates for 2-Substituted 1,2,3,4-Tetrahydro-4-quinolone Antitumor Agents

  • Choi Sun;Jung Keumn-Yeo;Ryu Jae-Sang
    • Archives of Pharmacal Research
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    • v.29 no.5
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    • pp.369-374
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    • 2006
  • An efficient method for the synthesis of optically active 2-substituted 2,3-dihydro-4-quinolones has been developed. The key features include the introduction of a chiral side chain and the construction of quinolone skeleton by Mitsunobu alkylation and hydroarylation, respectively.

Total Synthesis of New Apicidin Derivatives as Potent Antitumor Agents

  • kim, hyung-Kyo;Jin, Cheng-Hua;Han, Jeong-Whan;Lee, Hyang-Woo;Lee, Yin-Won;Zee, Ok-Pyo;Jung, Young-Hoon
    • 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)

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DESIGN, SYNTHESIS AND IN VITRO EVALUATION OF APIO ANALOGUE OF NEPLANOCIN A

  • Moon, Hyung-Ryong;Lee, Jeong-Ah;Yoo, Byul-Nae;Shin, Dae-Hong;Jeong, Lak-Shin
    • 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)

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Reproductive Toxicity of DA-125, A New Anthracycline Anticancer Agent: Teratogenicity Study in Rabbits (새로운 안트라사이클린계 항암제 DA-125의 생식독성연구: 토끼 최기형시험)

  • 정문구;김종춘;한상섭;노정구
    • Biomolecules & Therapeutics
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    • v.3 no.1
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    • pp.47-53
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    • 1995
  • DA-125, a new anthracycline antitumor antibiotic, was administered at dose levels of 0, 0.2, 0.6 and 1.8 mg/kg/day intravenously to pregnant New Zealand White rabbits from day 6 through 18 of gestation. The does were subjected to the caesarean section on day 28 of gestation. Effects of test agent on general toxicity of does and embryonic development of F1 fetuses were examined. At 1.8 mg/kg, the organ weight for ovary of does was significantly decreased. The decrease in the number of corpus lutea, implantations and litter size, and the increase in the rate of resorptions were also observed. In addition, various types of external, visceral and skeletal malformations occurred in fetuses at an incidence of 7.7, 7.7 and 20.6%, respectively. The results show that the no effect dose levels (NOELs) of DA-125 are 0.6 mg/kg/day for does and F1 fetuses.

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Antitumor Agent from the Rhizome of Anemarrhena asphodeloides (지모(知母)의 항암활성성분에 관한 연구)

  • Lee, Seung-Ho;Ryu, Shi-Yong;Choi, Sang-Un;No, Zae-Sung;Kim, Sung-Ki;Lee, Chong-Ock;Ahn, Jong-Woong
    • Korean Journal of Pharmacognosy
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    • v.26 no.1
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    • pp.47-50
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    • 1995
  • EtOAc soluble part of MeOH extract of Anemarrhena asphodeloides rhizome was evaluated for the cytotoxicity against the five kinds of human tumor cell lines (A-549, SK-OV-3, SK-MEL-2, XF498 and HCT15) in vitro. Bioassay-guided fractionation of EtOAc soluble part led to the isolation of active compound which was identified as timosaponin A-III showed potent cytotoxic activity, but its genin, sarsasapogenin, did not show cell growth inhibition.

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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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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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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.

Antitumor Activity of Health Food-C22 (건강식품 C-22의 항암 효과)

  • Jin, Wen-Yi;Yoo, Jae-Kuk;Park, Byeong-Wook;Chen, Quan-Cheng;Bae, Ki-Hwan
    • Korean Journal of Pharmacognosy
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    • v.39 no.3
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    • pp.237-240
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    • 2008
  • C-22 is one of health food made in Han Kook Shin Yak. For studying its antitumor activity, the 50% ethanol extract from C-22 was tested on BDF1 mice bearing LLC tumor cell by Teruhiro’s method. The samples were intraperitoneally injected to mice once a day with a daily dose of 50, 100, and 200 mg/kg for 14 consecutive days. Taxol was used as positive control with a dose of 50 mg/kg. As a result, the C-22's extracts dose dependently inhibited the tumor volume with the IRTV values of 28.7, 46.7, 58.9% and the IRTW values of 28.1, 46.0, 57.8% in 50, 100, and 200 mg/kg, respectively, while the Taxol showed antitumor activity with IRTV and IRTW values of 68.5 and 67.3% in 50 mg/kg. No loss of body weight was observed at any samples. This data suggested that the C-22's antitumor activity was enough to use as a cancer chemopreventive agent, and it will be used for preventing cancer as health food.