國家衛生研究院 NHRI:Item 3990099045/2841
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    题名: Dual inhibition of topoisomerase I and tubulin polymerization by BPR0Y007, a novel cytotoxic agent
    作者: Chang, JY;Hsieh, HP;Pan, WY;Liou, JP;Bey, SJ;Chen, LT;Liu, JF;Song, JS
    贡献者: National Institute of Cancer Research;Division of Biotechnology and Pharmaceutical Research
    摘要: Through the screening of DNA topoisomerase I (Top I) inhibitors, a new cytotoxic agent, BPR0Y007 [2,5-bis(4-hydroxy-3-methoxybenzylidene)cyclopentanone], was identified. BPR0Y007 was less potent than camptothecin (CPT) in the inhibition of Top I in vitro. Also, in vitro data showed that BPR0Y007 induces DNA cleavage in the presence of Top I at micromolar concentrations, with a cleavage specificity similar to that of CPT. High concentrations of BPR0Y007 did not produce detectable DNA unwinding, suggesting that BPR0Y007 is not a DNA intercalator. However, BPR0Y007 displaced Hoechst 33342 dye, suggesting that BPR0Y007 binds to DNA at the Hoechst 33342 binding site. Furthermore, BPR0Y007 generated protein-linked DNA breaks in a cell-based study. Cell cycle analysis demonstrated that the cell cycle effect of BPR0Y007 differs from that of CPT. Cells accumulated in the S-phase when treated with high concentrations of CPT, whereas cells accumulated gradually in the G(2)/M phase when treated with increasing concentrations of BPR0Y007. Further studies showed that BPR0Y007 inhibits tubulin polymerization in vivo and in vitro, and induces apoptosis in a concentration-dependent manner. No cross-resistance with BPR0Y007 was observed in CPT-, VP-16-, or vincristine-resistant cell lines. The IC50 of BPR0Y007 for various human cancer cell lines ranged from I to 8 M Taken together, these results suggest that BPR0Y007 acts on both Top I and tubulin. Given its unique biochemical mechanisms of action, BPR0Y007 warrants exploration as an antitumor compound. (C) 2003 Elsevier Science Inc. All rights reserved.
    关键词: Pharmacology & Pharmacy
    日期: 2003-06-15
    關聯: Biochemical Pharmacology. 2003 Jun;65(12):2009-2019.
    Link to: http://dx.doi.org/10.1016/S0006-2952(03)00197-7
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0006-2952&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000183588900011
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=0037716242
    显示于类别:[陳立宗] 期刊論文
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    [張俊彥] 期刊論文

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