Electro-optical fluorescence studies on the DNA binding of medically active drugs.
By measuring the transient changes in each of the polarized components of fluorescence during the application of a pulsed electric field to a solution of macromolecules, a method has been developed for evaluating the binding characteristics of fluorescent chemotherapeutic agents to DNA. It is shown that whereas quinacrine and berberine intercalate the DNA helix, hydroxystilbamidine does not. Furthermore, measurements on both the native and the diol-epoxide forms of benzo(a)pyrene show that the former is consistent with an intercalation type of binding, whilst the latter appears to be more inclined to the major DNA axis and may possibly be associated with the external helical grooves. The significance of these findings is discussed.
D015123:7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide; D001564:Benzo(a)pyrene; D001580:Benzopyrenes / Q000378:metabolism; D001599:Berberine / Q000378:metabolism; D002273:Carcinogens; D004247:DNA / Q000378:metabolism*; D005454:Fluorescence Polarization; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D011796:Quinacrine / Q000378:metabolism; D013266:Stilbamidines / Q000378:metabolism
D001580:Benzopyrenes; D002273:Carcinogens; D004364:Pharmaceutical Preparations; D013266:Stilbamidines; D001599:Berberine; D001564:Benzo(a)pyrene; C100274:hydroxystilbamidine; D015123:7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide; D004247:DNA; D011796:Quinacrine