Synthesis And Biological Evaluation Of Axially Modificated RGD Targeting Silicon Phthalocyanine

As a noninvasive binary therapy for the treatment of cancer, photodynamic therapy(PDT) has get more attention and the photosensitizer has played a core role in the system.The silicon photosensitizer was cased more and more careful because of the unique advantage.The article designed a series of photosensitizers (SPD-PQ,SPD-COOH,SPD-RGD,SPD-Linker-RGD,SPD-(Linker)2-RGD,SPD-Glu,(Linker)2-RGD) for evaluating their abilities in the PDT by the way of spectrum, Mtt and so on. Then on this basis, we evaluating the best compound SPD-Glu-(Linker)2-RGD) in living body imaging. In terms of spectrum, The UV-Vis spectra of Pcs in DMSO were typical of those for nonaggregated Pcs and all showing a soret band at 354 nm, two vibronic bands at approximately 610 nm-650 nm and a Q-band at 678 nm. It suggested that the axial substituents do not exert significant effects on the Pcs ? system. It had the highest Singlet oxygen quantum yield(??=0.39),the higher fluorescence quantum((?F=0.15) and the lowest fluorescence lifetime(3.14 ns) which was making for biotherapy. In terms of solution, Every photosensitizers(Pcs) had good dissolution in DMSO(R2=0.9992?0.9998). In 10% Triton X-100 and 1% cremophor EL, the Q-band spectrum of SPD-Glu-(Linker)2-RGD had recovered completely. In terms of bioevaluation, SPD-Glu-(Linker)2-RGD has the highest cytotoxic ability (IC50=17.54 nM). And the compound was enriched in the tumor in some degree, which will be a promising photosensitizer in the future.