No abstract

In this study, for the first time, CuFeS nanocrystals were successfully prepared through a facile noninjection-based synthetic strategy, by reacting Cu and Fe precursors with dodecanethiol in a 1-octadecene solvent. This one-pot noninjection strategy features easy handling, large-scale production, and high synthetic reproducibility. Following hyaluronic acid (HA) encapsulation, CuFeS nanocrystals coated with HA (CuFeS@HA) not only readily dispersed in water and showed improved biocompatibility but also possessed a tumor-specific targeting ability of cancer cells bearing the cluster determinant 44 (CD44) receptors. The encapsulated CuFeS@HA showed broad optical absorbance from the visible to the near-infrared (NIR) region and high photothermal conversion efficiencies of about 74.2%. They can, therefore, be utilized for the photothermal ablation of cancer cells with NIR light irradiation. In addition, toxicity studies in vitro (B16F1 and HeLa) and in vivo (zebrafish embryos), as well as in vitro blood compatibility studies, indicated that CuFeS@HA show low cytotoxicity at the doses required for photothermal therapy. More importantly, CuFeS@HA can be used as delivery vehicles for chemotherapy cisplatin(IV) prodrug forming CuFeS@HA-Pt(IV). Their release profile revealed pH- and glutathione-mediated drug release from CuFeS@HA-Pt(IV), which may minimize the side effects of the drug to normal tissues during therapy. Subsequent in vitro experiments confirmed that the use of CuFeS@HA-Pt(IV) provides an enhanced and synergistic therapeutic effect compared to that from the use of either chemotherapy or photothermal therapy alone.

In this work, manganese‐doped carbon quantum dots (Mn‐CQDs) have been synthesized through a one‐pot hydrothermal method by using waste green tea. The Mn2+ dopants were introduced to impart magnetic resonance capability. Upon optimization of the experimental conditions, magnetofluorescent Mn‐CQDs exhibit an excitation‐dependent blue emission. The abundant functional groups on Mn‐CQDs not only promote water solubility but also allow straightforward functionalization with amine groups. The amine‐terminated Mn‐CQDs were then subsequently conjugated to folic acid (FA) and chlorin e6 (Ce6) to obtain the Mn‐CQDs@FA/Ce6 magnetofluorescent photodynamic therapy (PDT) agent. in vitro studies using three different cells indicated specific targeting of Mn‐CQDs@FA/Ce6 to the overexpressing folate receptor human epithelial carcinoma cell line (HeLa) cancer cells. Furthermore, Mn‐CQDs@FA/Ce6 enhanced magnetic resonance imaging (MRI) signal with an r2/r1 ratio of 5.77. Favorably, by using the Mn‐CQDs@FA delivery system, active Ce6 can reach the cellular interior while its red fluorescence (FL) and reactive oxygen species generation can be retained, as has been verified by confocal microscopy. in vitro cell viability studies verified the biocompatibility of Mn‐CQDs@FA/Ce6 nanohybrid with no significant toxicity up to 500 ppm while PDT treatment with 5 min irradiation (671 nm, 1 W cm−2) was effective in killing >90% of cells. The light‐triggered Mn‐CQDs@FA/Ce6 multifunctional hybrid can serve as a dual‐modal FL/MRI probe and as an efficient PDT agent to detect and eradicate cancer cells remotely.

Af acile route to Pt II complexes doubly functionalized with bioactive molecules through ab ipyridine-type ligand is described. Initially, ligands L EE (containing two ethacrynic acid units), L EF (ethacrynic acid + flurbiprofen) and L EB (ethacrynic acid + biotin) were obtained in moderate to good yields from 2,2'-bipyridine-4,4'-dicarboxylicacid. Subsequent reaction of the ligands with [PtCl 2 (DMSO) 2 ]a fforded complexes [PtCl 2 (L EE)] (2), [PtCl 2 (L EF)] (3)a nd [PtCl 2 (L EB)] (4)i n high yields. All compounds were fully characterizedb ya nalytical and spectroscopic methods. Complexes 2-4 are highly stable in water/DMSOs olutiona t3 7 8Ca fter 72 h, whereas progressive release of the bioactive fragments was detected in ac ell culture medium. The compounds were assessed for their in vitro antiproliferativea ctivity towards tumorigenic A2780, A2780cisR and Y79 cells and non-tumourigenic HEK293 cells. In particular,t he combinationo fe thacrynic acid and flurbiprofen in 3 overcomes cisplatin-based resistance andp rovides strongc ancerc ell selectivity.E nzyme inhibition assays on human GST P1 and human COX-2 and cross-experiments with complex 1,a nalogous to 2-4 but lackingb io-groups, revealed ac lear synergy between the Pt II frame andt he bioactive organic components.

No abstract