Precisely activating ferroptosis by Fe(II)-triggered drug release for enhanced cancer therapy

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In the year of FY2022, the development and optimization of iron(II)-responsive drug release system in vitro was mainly conducted. Several oxime ester models were designed and synthesized. The stability and reactivity towards Fe2+ in aqueous solutions were evaluated. The proposed reaction mechanism and reaction product for the Fe2+-activated release were confirmed by ESI-MS spectra. Fluorescent cyanine dye and tumor-targeting moiety cRGD were synthesized by following the reported work of our research group.My research also focused on the design and synthesis of novel reaction-based functional fluorescent sensors to detect the diseases-related tiny changes in biological specimens such as pH, and enzymes. Due to the poor water-solubility and easily aggregation of cyanine dyes in aqueous solutions which hamper their biocompatibility in biological application. I am trying to develop the water-soluble Near-infrared pH-responsive cyanine dyes through introduction of several sulfonate groups to the benzoindole moiety of cyanine dyes. The dyes containing two or three anionic groups exhibited better water-solubility even in aqueous solutions without surfactant or organic solvents. Interestingly, I found that the aggregation nanoparticle size of dye in aqueous solutions was changed dependent on pH values which is promising to be used for the improved EPR effect for targeted and specific tumor imaging in vivo models.Besides, some cell experiments about enzyme-responsive probes for the cooperations with other researcher were conducted in this year.