Cancer-Targeting Functionalization of Selenium-Containing Ruthenium Conjugate with Tumor Microenvironment-Responsive Property to Enhance Theranostic Effects.
A mutifunctional ruthenium-based conjugate Ru-BSe was designed and synthesized. The Ru complex with favorable bioimaging function was covalently linked with a cancer-targeted molecule that could be effectively internalized by the tumor to realize enhanced theranostic effects. The pH-response of the Ru conjugate in tumor acidic microenvironment causes ligand substitution and release of therapeutic complex. This activated complex remains inert to the reducing biomolecule-glutathione and terminally locates in mitochondria, in which it triggers oxidative stress, and activates intrinsic apoptosis. Real-time monitoring reveals that this Ru conjugate could selectively accumulate in tumor tissue in vivo, which significantly suppresses tumor progression and alleviate the damage to normal organs, realizing the precise cancer theranosis.
['Zhao|Zhennan|Z|', 'Gao|Pan|P|', 'You|Yuanyuan|Y|', 'Chen|Tianfeng|T|http://orcid.org/0000-0001-6953-1342']
D000970:Antineoplastic Agents D017209:Apoptosis D006801:Humans D008024:Ligands D008928:Mitochondria D012428:Ruthenium D012643:Selenium D015398:Signal Transduction D000068936:Theranostic Nanomedicine D059016:Tumor Microenvironment
microenvironment theranosis cancer targeting selenium tumor-responsive