Synthesis and Photobiological Properties of Bromo- and Alkoxymethyl Furocoumarins

Bromo- and alkoxymethyl-furocoumarins were synthesized and evaluated for their ability to photoinduce cell death in human tumoral cell culture. Bromo substituted compounds resulted to be the most phototoxic compounds giving rise to a significant induction of apoptosis at 24 h from irradiation as demonstrated by a remarkable percentage of Annexin- V positive cells. The DNA photocleavaging properties of these derivatives were investigated using plasmid DNA as model. The results indicate that bromo derivatives induce significant photodamage to DNA. In particular, the effect is strongly evidenced after treatment of photosensitized DNA by two base excision repair enzymes, Fpg and Endo III.