Synthesis and DNA-binding affinities of monomodified berberines Original Research Article

Four new monomodified berberines have been synthesized in moderate to good yields starting from berberine and fully characterized by HRMS and 1H NMR. Spectrometric titration and ethidium bromide displacement experiments indicate that these berberine derivatives, especially the one having primary amino group, strongly bind with calf-thymus DNA, presumably via an intercalation mechanism.