ABSTRACT
In the current study, six ferrocenylseleno-dopamine derivatives with different structural parameters were designed. Among these derivatives, F4b, containing two ferrocene units and a tertiary amine, showed in vitro anticancer activity with IC50 = 2.4 ± 0.4 µM for MGC-803 cells, and its in vivo studies suggested effective antitumor activity in mice bearing an MGC-803 tumor xenograft. Mechanistic study revealed that the cytotoxicity of these ferrocenylseleno-dopamine derivatives is mainly related to the Fenton-like reaction under physiological conditions, and the tertiary amine in F4b can facilitate the H2O2 decomposition to generate toxic ËOH which induces apoptosis through CDK-2 inactivation.
ABSTRACT
By taking advantage of the efficient Förster resonance energy transfer (FRET) between near-infrared (NIR)-responsive lanthanide-doped upconversion nanoparticles (UCNPs) and Fenton reagent ferrocenyl compounds (Fc), a series of Fc-UCNPs was designed by functionalizing NaYF4:Yb,Tm nanoparticles with Fc1-Fc5 via surface-coordination chemistry. Fc-UCNP-Lipo nanosystems were then constructed by encapsulating Fc-UCNP inside liposomes for efficient delivery. Fc-UCNP can effectively release ·OH via a NIR-promoted Fenton-like reaction. In vitro and in vivo studies of Fc1-UCNP-Lipo confirmed the preferential accumulation in a tumor site followed by an enhanced uptake of cancer cells. After cellular internalization, the released Fc1-UCNP can effectively promote ·OH generation for tumor growth suppression. Such a Fc1-UCNP-Lipo nanosystem exhibits advantages such as easy fabrication, low drug dosage, and no ferrous ion release.
Subject(s)
Antineoplastic Agents/therapeutic use , Ferrous Compounds/therapeutic use , Metal Nanoparticles/therapeutic use , Metallocenes/therapeutic use , Neoplasms/drug therapy , Animals , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/radiation effects , Cell Line, Tumor , Drug Carriers/chemistry , Female , Ferrous Compounds/chemistry , Ferrous Compounds/radiation effects , Humans , Infrared Rays , Liposomes/chemistry , Metal Nanoparticles/chemistry , Metal Nanoparticles/radiation effects , Metallocenes/chemistry , Metallocenes/radiation effects , Mice, Inbred BALB C , Neoplasms/pathology , Terbium/chemistry , Terbium/radiation effects , Xenograft Model Antitumor Assays , Yttrium/chemistry , Yttrium/radiation effectsABSTRACT
The modulation of luminescence via external stimuli such as temperature, mechanical stress, hydrostatic pressure, as well as electric and/or magnetic fields, has witnessed great progress, enabled the disclosure of new principles and energy transfer pathways, and widened applications. However, investigations on the luminescence modulation of lanthanide ions doped in semiconductors via an applied electric field are still absent. Herein, for the first time, we have demonstrated the in situ, real-time, and reversible modulation of the luminescence of Eu3+ doped in SnO2 nanocrystals by manipulating the recombination rate of photo-generated electrons and holes, and the accompanied energy transfer mode in terms of linear and quasi-sinusoidal, from semiconductor to lanthanide ions. Following the same principle, the modulation of near infrared responsive Er3+ in SnO2 and the visible luminescence of perovskite nanocrystals is further realized. This study offers extra methodologies for luminescence modulation, in addition to those already reported for ferro- and/or piezoelectric-hosted luminescent materials.
