Abstract
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.
Keywords: Furocoumarins, Phototoxicity, DNA photodamage, Apoptosis
Letters in Drug Design & Discovery
Title: Synthesis and Photobiological Properties of Bromo- and Alkoxymethyl Furocoumarins
Volume: 5 Issue: 2
Author(s): Giampietro Viola, Marco Boccalini, Elena Fortunato, Francesco dall'Acqua and Stefano Chimichi
Affiliation:
Keywords: Furocoumarins, Phototoxicity, DNA photodamage, Apoptosis
Abstract: 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.
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Cite this article as:
Viola Giampietro, Boccalini Marco, Fortunato Elena, dall'Acqua Francesco and Chimichi Stefano, Synthesis and Photobiological Properties of Bromo- and Alkoxymethyl Furocoumarins, Letters in Drug Design & Discovery 2008; 5 (2) . https://dx.doi.org/10.2174/157018008783928481
DOI https://dx.doi.org/10.2174/157018008783928481 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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