A Smart Europium–Ruthenium Complex as Anticancer Prodrug: Controllable Drug Release and Real-Time Monitoring under Different Light Excitations

What is it about?

A unique, dual-function, photo-activatable anticancer prodrug, RuEuL, has been tailored that features a ruthenium(II) complex linked to a cyclen-europium chelate via a p-conjugated bridge. Under irradiation at 488 nm, the dark-inactive prodrug undergoes photodissociation, releasing the DNA-damaging ruthenium species. Under evaluation-window irradiation (lirr = one-photon 350 nm or two-photon 700 nm), the drug delivery process can be quantitatively monitored in real-time thanks to the long-lived red europium emission. Linear relationships between released drug concentration and ES-MS or luminescence responses are established. Finally, the efficiency of the new prodrug is demonstrated both in vitro on HeLa cells and in vivo by inhibiting tumours in BALB/c nude mice carrying SW480 xenografts. The results presented in this article also reveal the advantages of the dual-functional RuEuL anticancer prodrug over some existing ones and open the way for decisive improvements in multi-purpose prodrugs

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