A Highly Luminescent Tetrahydrocurcumin IrIII Complex with Remarkable Photoactivated Anticancer Activity |
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Authors: | Dr Alessia Colombo Dr Mattia Fontani Prof Claudia Dragonetti Prof Dominique Roberto Prof J A Gareth Williams Dr Rossella Scotto di Perrotolo Dr Francesca Casagrande Dr Sara Barozzi Dr Simona Polo |
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Institution: | 1. Dipartimento di Chimica, dell'Università degli Studi di Milano, and UdR INSTM di Milano, via Golgi 19, 20133 Milan, Italy;2. Department of Chemistry, Durham University, Durham, DH1 3LE UK;3. IFOM, Fondazione Istituto FIRC di Oncologia Molecolare, Via Adamello 16, 20145 Milan, Italy |
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Abstract: | Curcumin has chemopreventative properties against a variety of tumours, but has poor bioavailability. Here, two new bis-cyclometallated iridium(III) complexes have been prepared, featuring the natural product curcumin (CUR) or its reduced form, tetrahydrocurcumin (THC), as bidentate, anionic O O-binding ligands. The iridium THC complex is highly luminescent in deoxygenated solution and efficiently generates singlet oxygen under aerated conditions, whereas in the CUR analogue, other non-radiative decay pathways are competitive. The complexes are rapidly taken up by a variety of human tumour cell lines from solutions of micromolar concentration. They show negligible cytotoxicity in the absence of irradiation. When briefly irradiated with visible light, Ir-THC becomes highly phototoxic, inducing rapid apoptosis within 2 h. The results show the high potential of such complexes as sensitizers in photodynamic therapy (PDT). |
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Keywords: | anticancer agents curcumin imaging agents iridium natural products photodynamic therapy tetrahydrocurcumin |
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