Nucleus‐targeted organoiridium‐albumin conjugate for photoactivated cancer therapy

: A highly phosphorescent organoiridium‐albumin conjugate (Ir1‐HSA) was synthesized by reacting an organo‐iridium complex (Ir1) containing a pendant maleimide with human serum albumin. The phosphorescence of the Ir1‐HSA conjugate is much stronger than the parent iridium complex. Real‐time cellular imaging shows that the conjugate mainly accumulates in the nucleus of cancer cells. The long phosphorescence lifetime and high 1O2 quantum yield of Ir1‐HSA make it a strong candidate for photoactivated cancer therapy. Ir1‐HSA shows remarkable photocytotoxicty in a range of cancer cell lines and tumor spheroids (IC50; 0.8‐5 μM) with an excellent photo‐cytotoxicity index (C50 (dark) / IC50 (light) = 40‐60) while remaining non‐toxic to normal cells and normal‐cell spheroids, even after photo‐irradiation. This organoiridium‐albumin photosensitizer has potential for application in both photoactivated therapy and nucleus staining.

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