研究目的
Investigating the therapeutic effects of stable and well-organized near-infrared platinum(II)-acetylide-based metallacycles mediated cancer phototherapy.
研究成果
The study presents the design of a new series of well-defined metallacycles (M1-M3) via the Pt-acetylide coordination with highly efficient photoconversion behavior for synergistic PDT/PTT. The metallacycles showed high stability and intense NIR absorption, and their absorption peaks were red-shifted compared with their corresponding precursors. In vitro studies demonstrated that M3-NPs showed excellent performance including high singlet oxygen generation and photothermal conversion efficiency, which facilitated the photoinduced cell damage and subsequently achieved the tumor ablation. The present study, as the first example of NIR-absorbing Pt-acetylide metallacycles, provided a valuable guideline for improving the stability and anticancer efficiency of metallacycles.
研究不足
The technical and application constraints of the experiments include the challenge of achieving highly-stable architectures with easily tunable optical properties for metallacycle using the coordination interaction. Potential areas for optimization include improving the NIR absorption and stability of metallacycles for deeper tissue penetration and efficient therapeutic efficacy.
1：Experimental Design and Method Selection:
The metallacycles (M1-M3) were prepared from the aza-BODIPY (1-3) and Pt1 in the presence of catalyst CuI through dehydrohalogenation reaction. The metallacycles were purified by silica column chromatography.
2：Sample Selection and Data Sources:
All synthetic intermediates and metallacycles were characterized by 1H NMR, 31P{1H} NMR, 19F NMR, matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF-MS).
3：List of Experimental Equipment and Materials:
Bruker Ultra Shield Plus 400MHz NMR instrument, Bruker autoflex matrix assisted laser desorption ionization time of flight mass spectrometer, Shimadzu UV-3600 UV-VIS-NIR spectrophotometer, Horiba Fluoromax-4 fluorescence spectrophotometer, HR-TEM, TEM (JEM-2100), Zetasizer Nanoseries (Nano ZS90), Power Wave XS/XS2 microplate spectrophotometer, Olympus IX81 laser scanning confocal microscope, NIR thermal imager (FLIR E40), VLP-2000 laser power meter.
4：Experimental Procedures and Operational Workflow:
The metallacycles were synthesized, characterized, and their photophysical properties were explored. M-NPs were prepared and their photodynamic and photothermal properties were investigated. In vitro and in vivo studies were conducted to evaluate the phototherapy efficiency.
5：Data Analysis Methods:
The data were analyzed using Gaussian 09 program for DFT calculation, xtb program for packing mode optimization, and various spectroscopic and imaging techniques for characterization.
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