Acta poloniae pharmaceutica 2010-01-01

Inhibition of DNA topoisomerases I and II by G3 PAMAM-NH2 dendrimer-modified digoxin and proscillaridin A conjugates in a cell free system.

Katarzyna Winnicka, Anna Bielawska, Krzysztof Bielawski

Index: Acta Pol. Pharm. 67(6) , 630-4, (2010)

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Abstract

Two modified glycosides--digoxin and proscillaridin A conjugated to a generation 3 of polyamidoamine dendrimer (G3 PAMAM-NH2) were evaluated as DNA topoisomerase II inhibitors. The ability of these compounds (PAMAM-Dig and PAMAM-Prosc) to inhibit topoisomerase I and II activity was quantified by measuring the action on supercoiled DNA substrate as a function of increasing concentration of the test compounds by the use of agarose gel electrophoresis. The obtained results suggest that a conjugation of the modified glycosides with G3 PAMAM-NH2 significantly improved the ability of the parent compounds to an inhibition of DNA topoisomerases.