Cancer‐Targeting Functionalization of Selenium‐Containing Ruthenium Conjugate with Tumor Microenvironment‐Responsive Property to Enhance Theranostic Effects. Issue 13 (5th February 2018) - Zhao, Zhennan
Abstract: 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. Abstract : Selenium against cancer : We demonstrate the rational design and synthesis of a selenium‐containing conjugate that could selectively recognize cancer cells to demonstrate enhanced theranostic effects and nullify the systemic toxicity. The protonation process of Ru II conjugate in tumor acidic microenvironment causes ligand substitution, resulting in release of an activated metallodrug that triggers apoptosis in tumor tissue.