Synthesis and Biological Activity of Raltitrexed-Carrier Conjugates

    March 2010 in “ Acta Biochimica Polonica ”
    Monika Jagiello, Urszula Kańska, Dmitry Nevozhay, Janusz Boratyński
    TLDR Raltitrexed conjugates are less potent than the free drug but more effective at high concentrations.
    The study synthesized raltitrexed (RTX) conjugates with lysozyme, bovine serum albumin (BSA), and dextran T40 to assess their cytotoxicity and cell cycle effects compared to the free drug. The conjugation process involved transforming RTX into an anhydride and reacting it with carriers at various pH levels, achieving maximum yield at pH 10. In vitro tests on SW707, LoVo, and A549 cell lines showed that the conjugates had significantly higher IC(50) values than the free drug, indicating lower potency. However, at high concentrations (1000 and 10000 ng/ml), dextran and albumin-based conjugates were more cytotoxic than the free drug. RTX primarily blocked the cell cycle in the G(0)-G(1) and S phases, increasing apoptosis, while the conjugates blocked the S phase and reduced the G(0)-G(1) phase cell percentage.
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