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1.
Chem Commun (Camb) ; 58(45): 6546-6549, 2022 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-35579558

RESUMEN

Novel NIR-II Ru(II) polypyridyl fluorophore Ru-1 dots for synergistic chemo-photothermal therapy against 4T1 tumors were designed and synthesized. Guided by in vivo NIR-II fluorescence imaging, the synergistic therapeutic efficacy, intracellular delivery, and biodistribution of the Ru-1 dots were precisely tracked in real-time.


Asunto(s)
Nanopartículas , Rutenio , Línea Celular Tumoral , Colorantes Fluorescentes , Fototerapia/métodos , Terapia Fototérmica , Distribución Tisular
2.
J Med Chem ; 65(3): 2225-2237, 2022 02 10.
Artículo en Inglés | MEDLINE | ID: mdl-34994554

RESUMEN

The clinical success of cisplatin ushered in a new era of the application of metallodrugs. When it comes to practice, however, drug resistance, tumor recurrence, and drug systemic toxicity make it implausible to completely heal the patients. Herein, we successfully transform an electron acceptor [1, 2, 5]thiadiazolo[3,4-g]quinoxaline into a novel second near-infrared (NIR-II) fluorophore H7. After PEGylation and chelation, HL-PEG2k exhibits a wavelength bathochromic shift, enhanced photothermal conversion efficiency (41.77%), and an antineoplastic effect against glioma. Its potential for in vivo tumor tracking and image-guided chemo-photothermal therapy is explored. High levels of uptake and high-resolution NIR-II imaging results are thereafter obtained. The hyperthermia effect could disrupt the lysosomal membranes, which in turn aggravate the mitochondria dysfunction, arrest the cell cycle in the G2 phase, and finally lead to cancer cell apoptosis. HL-PEG2k displays a superior biocompatibility and thus can be a potential theranostic platform to combat the growth and recurrence of tumors.


Asunto(s)
Complejos de Coordinación/química , Rayos Infrarrojos , Rutenio/química , Apoptosis/efectos de los fármacos , Materiales Biocompatibles/química , Materiales Biocompatibles/farmacología , Materiales Biocompatibles/uso terapéutico , Línea Celular Tumoral , Complejos de Coordinación/farmacología , Complejos de Coordinación/uso terapéutico , Diseño de Fármacos , Colorantes Fluorescentes/química , Colorantes Fluorescentes/farmacología , Colorantes Fluorescentes/uso terapéutico , Puntos de Control de la Fase G2 del Ciclo Celular/efectos de los fármacos , Humanos , Hipertermia Inducida , Neoplasias/diagnóstico por imagen , Neoplasias/tratamiento farmacológico , Neoplasias/terapia , Fenazinas/química , Terapia Fototérmica/métodos , Polietilenglicoles/química , Teoría Cuántica , Espectroscopía Infrarroja Corta
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