Welcome to THE ZOU LAB

News in the Lab

Moyi's paper entitled "Photoactivation of Boronic Acid-Prodrugs via a Phenyl Radical Mechanism: Iridium(III) Anticancer Complex as an Example" has been accepted by JACS. Well done!

April 17, 2023

Boronic acid (or ester) is a well-known temporary masking group for developing anticancer prodrugs responsive to tumoral ROS, but their clinic application is largely hampered by the low activation efficiency. Herein, we report a robust photoactivation approach that can spatiotemporally convert boronic acid-caged iridium(III) complex IrBA into bioactive IrNH2 under hypoxic tumor microenvironments. Mechanistic studies show that the phenyl boronic acid moiety in IrBA is in equilibrium with phenyl boronate anion that can be photo-oxidized to generate phenyl radical, a highly reactive species that is capable of rapidly capturing O2 at extremely low concentrations (down to 0.02%). As a result, while IrBA could hardly be activated by intrinsic ROS in cancer cells, upon light irradiation, the prodrug is efficiently converted into IrNH2 even in limited O2 supply, along with direct damage to mitochondrial DNA and potent antitumor activities in hypoxic 2D monolayer cells, 3D tumor spheroids, and mouse-bearing tumor xenografts. Of note, the photoactivation approach could be extended to intermolecular photocatalytic activation by external photosensitizers with red absorption and to activate prodrugs of clinic compound, thus offering a general approach for activation of anti-cancer organoboron prodrugs.

A review paper entitled "Modulating the Chemical Reactivity of Gold Complexes in Living Systems: From Concept to Biomedical Applications" was accepted in Acc. Chem. Res. Congrates to Jiang jia and Xiaolin.

Apr-10-2023

This paper summarizes our recent series works on stimuli-activatable gold prodrugs. It is hoped that this account will spur the creation of better approaches to advance gold complexes closer to clinical application.

Yunli's paper on conditionally activatable anticancer gold complexes was accepted for publication in Angew. Chem. Congrats!

Sep 16, 2022