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Pharmaceuticals 2017, 10(2), 41; doi:10.3390/ph10020041

Biotinylated Chlorin and Its Zinc and Indium Complexes: Synthesis and In Vitro Biological Evaluation for Photodynamic Therapy

Department of Chemistry and Physics, Purdue University Northwest, 1401 S US Hwy 421, Westville, IN 46391, USA
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Author to whom correspondence should be addressed.
Academic Editor: Francois Dufrasne
Received: 27 December 2016 / Revised: 15 March 2017 / Accepted: 27 March 2017 / Published: 15 April 2017
(This article belongs to the Special Issue Metal-Based Drugs)
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Abstract

The synthesis and characterization of biotinylated chlorin photosensitizer and the corresponding zinc and indium complexes are described for potential applications in photodynamic therapy (PDT) for cancer. Phototoxicity of the biotin-chlorin conjugate and the metallated complexes was determined in colon carcinoma CT26 cell lines known to overexpress biotin (Vit B7) receptors. Cell survival assay indicated that the biotinylated chlorin and indium complex showed increased cell growth inhibition than the zinc complex and the starting chlorin (methyl pheophorbide). Fluorescence microcopy studies revealed the generation of apoptotic cells upon light irradiation of colon cells treated with the indium complex. Targeting biotin receptors in cancer cells can improve specificity of photosensitizers for PDT applications. View Full-Text
Keywords: photodynamic therapy; PDT; chlorin-biotin conjugate; zinc chlorin-biotin complex; indium chlorin-biotin complex; vitamin-targeted cancer therapeutics photodynamic therapy; PDT; chlorin-biotin conjugate; zinc chlorin-biotin complex; indium chlorin-biotin complex; vitamin-targeted cancer therapeutics
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Isaac-Lam, M.F.; Hammonds, D.M. Biotinylated Chlorin and Its Zinc and Indium Complexes: Synthesis and In Vitro Biological Evaluation for Photodynamic Therapy. Pharmaceuticals 2017, 10, 41.

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