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A Photoisomerizable Zinc (II) Complex Inhibits Microtubule Polymerization for Photoactive Therapy |
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| Authors: | Fengshu Cao Haobing Wang Nong Lu Prof. Pingyu Zhang Prof. Huaiyi Huang |
| Affiliation: | 1. College of Chemistry and Environmental Engineering, Shenzhen University, Shenzhen, 518060 China School of Pharmaceutical Science (Shenzhen), Shenzhen campus of Sun Yat-sen University, No.66, Gongchang Road, Shenzhen, 518107 China These authors contributed equally to this work.;2. College of Chemistry and Environmental Engineering, Shenzhen University, Shenzhen, 518060 China These authors contributed equally to this work.;3. College of Chemistry and Environmental Engineering, Shenzhen University, Shenzhen, 518060 China;4. School of Pharmaceutical Science (Shenzhen), Shenzhen campus of Sun Yat-sen University, No.66, Gongchang Road, Shenzhen, 518107 China |
| Abstract: | The photoisomerization-induced cytotoxicity in photopharmacology provides a unique pathway for phototherapy because it is independent of endogenous oxygen. In this study, we developed a biosafe photoisomerizable zinc(II) complex ( Zn1 ), which releases its trans ligand ( trans -L1 ) after being irradiated with blue light. This causes the complex to undergo photoisomerization and produce the toxic cis product ( cis -L1 ) and generate singlet oxygen (1O2). The resulting series of events caused impressive phototoxicity in hypoxic A431 skin cancer cells, as well as in a tumor model in vivo. Interestingly, Zn1 was able to inhibit tumor microtubule polymerization, while still showing good biocompatibility and biosafety in vivo. This photoisomerizable zinc(II) complex provides a novel strategy for addressing the oxygen-dependent limitation of traditional photodynamic therapy. |
| Keywords: | Metals in Medicine Microtubule Inhibition Photoactive Therapy Photoisomerization Zinc(II) Complex |