Volume 61, Issue 45 e202212689
Research Article

Organogold(III) Complexes Display Conditional Photoactivities: Evolving From Photodynamic into Photoactivated Chemotherapy in Response to O2 Consumption for Robust Cancer Therapy

Yunli Luo

Yunli Luo

Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006 P. R. China

Search for more papers by this author
Dr. Bei Cao

Dr. Bei Cao

Warshel Institute for Computational Biology, and General Education Division, The Chinese University of Hong Kong, Shenzhen, 518172 P. R. China

Search for more papers by this author
Mingjie Zhong

Mingjie Zhong

Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006 P. R. China

Search for more papers by this author
Moyi Liu

Moyi Liu

Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006 P. R. China

Search for more papers by this author
Dr. Xiaolin Xiong

Dr. Xiaolin Xiong

Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006 P. R. China

Search for more papers by this author
Prof. Dr. Taotao Zou

Corresponding Author

Prof. Dr. Taotao Zou

Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006 P. R. China

Search for more papers by this author
First published: 15 September 2022
Citations: 23

Graphical Abstract

Oxygen-dependent photo-reactivity for robust tumor therapy: A PDT-to-PACT evolving photo-reactivity with response to oxygen-consumption was found in cyclometalated gold(III)-alkyne complexes, leading to potent cytotoxicity towards cancer cells, strong anti-angiogenesis in zebrafish, and efficient suppression of mouse tumor xenografts.

Abstract

Photodynamic therapy (PDT) is a spatiotemporally controllable, powerful approach in combating cancers but suffers from low activity under hypoxia, whereas photoactivated chemotherapy (PACT) operates in an O2-independent manner but compromises the ability to harness O2 for potent photosensitization. Herein we report that cyclometalated gold(III)-alkyne complexes display a PDT-to-PACT evolving photoactivity for efficient cancer treatment. On the one hand, the gold(III) complexes can act as dual photosensitizers and substrates, leading to conditional PDT activity in oxygenated condition that progresses to highly efficient PACT (ϕ up to 0.63) when O2 is depleted in solution and under cellular environment. On the other hand, the conditional PDT-to-PACT reactivity can be triggered by external photosensitizers in a similar manner in vitro and in vivo, giving additional tumor-selectivity and/or deep tissue penetration by red-light irradiation that leads to robust anticancer efficacy.

Conflict of interest

The authors declare no conflict of interest.

Data Availability Statement

The data that support the findings of this study are available from the corresponding author upon reasonable request.

The full text of this article hosted at iucr.org is unavailable due to technical difficulties.