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- Title
Lignin Nanoparticles Deliver Novel Thymine Biomimetic Photo-Adducts with Antimelanoma Activity.
- Authors
Gabellone, Sofia; Piccinino, Davide; Filippi, Silvia; Castrignanò, Tiziana; Zippilli, Claudio; Del Buono, Davide; Saladino, Raffaele
- Abstract
We report here the synthesis of novel thymine biomimetic photo-adducts bearing an alkane spacer between nucleobases and characterized by antimelanoma activity against two mutated cancer cell lines overexpressing human Topoisomerase 1 (TOP1), namely SKMEL28 and RPMI7951. Among them, Dewar Valence photo-adducts showed a selectivity index higher than the corresponding pyrimidine-(6-4)-pyrimidone and cyclobutane counterpart and were characterized by the highest affinity towards TOP1/DNA complex as evaluated by molecular docking analysis. The antimelanoma activity of novel photo-adducts was retained after loading into UV photo-protective lignin nanoparticles as stabilizing agent and efficient drug delivery system. Overall, these results support a combined antimelanoma and UV sunscreen strategy involving the use of photo-protective lignin nanoparticles for the controlled release of thymine dimers on the skin followed by their sacrificial transformation into photo-adducts and successive inhibition of melanoma and alert of cellular UV machinery repair pathways.
- Subjects
CYCLOBUTANE; THYMINE; LIGNINS; DNA adducts; EXCIPIENTS; DRUG delivery systems; NANOPARTICLES
- Publication
International Journal of Molecular Sciences, 2022, Vol 23, Issue 2, p915
- ISSN
1661-6596
- Publication type
Article
- DOI
10.3390/ijms23020915