Emissive nanoparticles from pyridinium-substituted tetraphenylethylene salts: imaging and selective cytotoxicity towards cancer cells in vitro and in vivo by varying counter anions

Chemotherapeutics specifically targeting cancer cells without damaging healthy cells is the long-awaited goal of cancer treatment. In this paper, a series of nanoparticles (NanoTPES 1–4) assembled from pyridinium-substituted tetraphenylethylene salts were synthesized and investigated both in vitro and in vivo for this purpose. By changing the counter anions, NanoTPES 1–4 exhibit tunable emission colors, sizes and surface charges. NanoTPES 2 and 3 with tetraphenyl borate and tetra(4-chlorophenyl) borate as the respective anions selectively imaged and targeted mitochondria in cancer cells. Accordingly, these two nanoparticles specifically kill cancer cells with minimal effect on normal cells. Such selective cytotoxicity was attributed to the change of membrane potential and inhibition of ATP synthesis in the mitochondria of cancer cells. Furthermore, both NanoTPES 2 and 3 exhibited efficient tumor accumulation and tumor growth inhibition in vivo, with negligible systemic toxicity.