English  |  正體中文  |  简体中文  |  Items with full text/Total items : 17109/19415 (88%)
Visitors : 2696665      Online Users : 434
RC Version 7.0 © Powered By DSPACE, MIT. Enhanced by NTU Library IR team.
Scope Tips:
  • please add "double quotation mark" for query phrases to get precise results
  • please goto advance search for comprehansive author search
  • Adv. Search
    HomeLoginUploadHelpAboutAdminister Goto mobile version
    Please use this identifier to cite or link to this item: http://ir.cnu.edu.tw/handle/310902800/30961

    標題: Synthesis and Antitumor Properties of BQC-Glucuronide, a Camptothecin Prodrug for Selective Tumor Activation
    作者: Prijovich, Zeljko M.
    Burnouf, Pierre-Alain
    Chou, Hua-Cheng
    Huang, Ping-Ting
    Chen, Kai-Chuan
    Cheng, Tian-Lu
    Leu, Yu-Lin
    Roffler, Steve R.
    貢獻者: Acad Sinica, Inst Biomed Sci, Acad Rd
    Natl Yang Ming Univ, Taiwan Int Grad Program Mol Med
    Acad Sinica, Acad Rd
    Kaohsiung Med Univ, Fac Biomed Sci & Environm Biol
    Chia Nan Univ
    關鍵字: camptothecin
    targeted therapy
    albumin influence
    日期: 2016-04
    上傳時間: 2018-01-18 11:38:46 (UTC+8)
    出版者: Amer Chemical Soc
    摘要: Major limitations of camptothecin anticancer drugs (toxicity, nonselectivity, water insolubility, inactivation by human serum albumin) may be improved by creating glucuronide prodrugs that rely on beta-glucuronidase for their activation. We found that the camptothecin derivative 5,6dihydro-4H-benzo [de] quinoline-camptothecin (BQC) displays greater cytotoxicity against cancer cells than the clinically used Norma tissue camptothecin derivatives SN-38 and topotecan even in the presence of human serum albumin. We synthesized the prodrug BQC-glucuronide (BQC-G), which was 4000 times more water soluble and 20-40 times less cytotoxic than BQC. Importantly, even in the presence of human serum albumin, BQC-G was efficiently hydrolyzed by beta-glucuronidase and produced greater cytotoxicity (IC50 = 13 nM) than camptothecin, 9-aminocamptothecin, SN-38, or topotecan (IC50 > 3000, 1370, 48, and 28 nM, respectively). BQC-G treatment of mice bearing human colon cancer xenografts with naturally or artificially elevated beta-glucuronidase activity produced significant antitumor activity, showing that BQC-G is a potent prodrug suitable for selective intratumoral drug activation.
    Appears in Collections:[藥學系(所)] 期刊論文

    Files in This Item:

    File Description SizeFormat

    All items in CNU IR are protected by copyright, with all rights reserved.

    DSpace Software Copyright © 2002-2004  MIT &  Hewlett-Packard  /   Enhanced by   NTU Library IR team Copyright ©   - Feedback