Lipofuscin granules accumulate in the retinal pigment epithelium (RPE) with age, especially in patients with visual diseases, including progressive age-related macular degeneration (AMD).
The spectral characteristics, binding constants with bovine (BSA) and human serum albumin (HSA) and lifetimes of fluorescence in PBS and EtOH solutions and in the presence of BSA in PBS were measured for novel indotricarbocyanine dyes bearing remote phosphonate groups. These parameters are close to those for indocyanine green (ICG) indicating that the Coulomb interaction does not play a significant role in complex formation, and the binding is determined by the interaction of the dye polymethine chain with albumin. The fluorescence lifetimes of the complexes with BSA strongly indicate the formation of complexes of two types with different lifetimes. The complex with a longer fluorescence lifetime (740-800 ps) and major contribution (up to 88%) is bound to the more hydrophobic site and that with a shorter fluorescence lifetime (300-340 ps) to the more hydrophilic site.
Controlled photoreduction of Pt(IV) prodrugs is a challenging
task
due to the possibility of targeted light-controlled activation of
anticancer agents without affecting healthy tissues. Also, a conjugation
of photosensitizers and clinically used platinum drugs into one Pt(IV)
prodrug allows combining photodynamic therapy and chemotherapy approaches
into one molecule. Herein, we designed the cisplatin-based Pt(IV)
prodrug Riboplatin with tetraacetylriboflavin in the axial position.
A novel Pt(IV) prodrug is able to act both as a photodynamic therapy
(PDT) agent through the conversion of ground-state 3O2 to excited-state 1O2 and as an agent
of photoactivated chemotherapy (PACT) through releasing of cisplatin
under gentle blue light irradiation, without the requirement of a
reducing agent. The light-induced behavior of Riboplatin was investigated
using an electrochemical sensor in MCF-7 tumor spheroids. Photocontrolled
cisplatin release and ROS generation were detected electrochemically
in real time. This appears to be the first confirmation of simultaneous
photoactivated release of anticancer drug cisplatin and ROS from a
dual-action Pt(IV) prodrug observed from the inside of living tumor
spheroids.
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