한빛사논문
Le Tu 1+, Chonglu Li 1+, Xiaoxing Xiong 2+, Ji Hyeon Kim 3+, Qian Li 4, Longcan Mei 1, Junrong Li 1, Shuang Liu 5, Jong Seung Kim 3, Yao Sun 1
1National Key Laboratory of Green Pesticide, College of Chemistry, Central China Normal University, Wuhan, 430079, China.
2Department of Neurosurgery, Renmin Hospital of Wuhan University, Wuhan, 430060, China.
3Department of Chemistry, Korea University, Seoul, 02841, Korea.
4Key Laboratory of Optic-electric Sensing and Analytical Chemistry for Life Science, Qingdao University of Science & Technology, Qingdao, 266100, China.
5School of Materials Science and Engineering, Wuhan University of Technology, Wuhan, 430070, China.
+ These authors contributed equally to this work.
CORRESPONDING AUTHORS : Prof. Jong Seung Kim, Prof. Yao Sun
Abstract
Although metallacycle-based supramolecular photosensitizers (PSs) have attracted increasing attention in biomedicine, their clinical translation is still hindered by their inherent dark toxicity. Herein, we report what to our knowledge is the first example of a molecular engineering approach to building blocks of metallacycles for constructing a series of supramolecular PSs (RuA-RuD), with the aim of simultaneously reducing dark toxicity and enhancing phototoxicity, and consequently obtaining high phototoxicity indexes (PI). Detailed in vitro investigations demonstrate that RuA-RuD display high cancer cellular uptake and remarkable antitumor activity even under hypoxic conditions. Notably, RuD exhibited no dark toxicity and displayed the highest PI value (≈406). Theoretical calculations verified that RuD has the largest steric hindrance and the lowest singlet-triplet energy gap (ΔEST , 0.61 eV). Further in vivo studies confirmed that RuD allows safe and effective phototherapy against A549 tumors.
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