Počet záznamů: 1

Interaction of N-(2-hydroxypropyl)methacrylamide copolymer-doxorubicin conjugates with human liver microsomal cytochromes P450: comparison with free doxorubicin

  1. 1.
    0366452 - UMCH-V 2012 RIV US eng J - Článek v odborném periodiku
    Mašek, V. - Anzenbacherová, E. - Etrych, Tomáš - Strohalm, Jiří - Ulbrich, Karel - Anzenbacher, P.
    Interaction of N-(2-hydroxypropyl)methacrylamide copolymer-doxorubicin conjugates with human liver microsomal cytochromes P450: comparison with free doxorubicin.
    Drug Metabolism and Disposition. Roč. 39, č. 9 (2011), s. 1704-1710 ISSN 0090-9556
    Grant CEP: GA AV ČR KAN200200651
    Výzkumný záměr: CEZ:AV0Z40500505
    Klíčová slova: targeted drug delivery * nanomedicine * supramolecular chemistry
    Kód oboru RIV: FR - Farmakologie a lékárnická chemie
    Impakt faktor: 3.733, rok: 2011

    Interaction of nine forms of human hepatic cytochromes P450 (CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4) with two N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer-based doxorubicin (DOX) conjugates designed for passive tumor targeting was studied using pooled human microsomes. The compounds used in this study were two high-molecular-weight HPMA copolymers bearing doxorubicin attached to the polymeric carrier by 1) hydrazone bond enabling intracellular pH-controlled drug release or 2) amide bond through enzymatically cleavable tetrapeptide GlyPheLeuGly spacer. The extent of inhibition of enzymatic activities of the cytochrome P450 forms studied was negligible with the exception of CYP2B6 and was apparently caused by DOX as no inhibition was observed with polymers alone, and the extent of inhibition by the complex corresponded to this of the free DOX at the same concentration.
    Trvalý link: http://hdl.handle.net/11104/0201441