| 초록 |
Herein, we developed a highly efficient mitochondria targeting antitumor theranostic prodrug that contain two molecules of drug 5’-deoxy-5-fluorouridine, and an apoptotic marker ethidium for self-monitoring intrinsic (mitochondrial) apoptosis after its activation in tumor cells. Theranostic was activated by endogenously produced mitochondrial-overexpressed H2O2 and release the drug 5’-deoxy-5-fluorouridine and apoptotic marker ethidium to the tumor site. The in vitro and in vivo drug release was monitored by observing the fluorescence changes of ethidium. Theranostic exhibited an enhanced cytotoxicity over commercial 5-fluorouracil leading to intrinsic apoptosis monitored by in situ generated ethidium. Enhanced expression of mitochondria-mediated apoptotic genes (NOXA, PUMA, BID, BAX, and BAK), Cyt C, Caspase-3 and -9, and cell surface death receptors was observed after theranostic activation in tumor cells. . |
