Chlorin e6-Biotin Conjugates for Tumor-Targeting Photodynamic Therapy |
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| Authors: | Wei Liu Xingqun Ma Yingying Jin Jie Zhang Yang Li Yuxia Tang Yong Song Shouju Wang |
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| Affiliation: | 1.Lab of Molecular Imaging, Department of Radiology, the First Affiliated Hospital of Nanjing Medical University, Nanjing 210000, China; (W.L.); (Y.J.); (J.Z.); (Y.L.);2.Department of Oncology, Nanjing Baiyi Hospital, Jinling Clinical College of Nanjing Medical University, Nanjing 210000, China;3.Department of Respiratory and Critical Care Medicine, Jinling Clinical College of Nanjing Medical University, Nanjing 210000, China |
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| Abstract: | To improve the tumor-targeting efficacy of photodynamic therapy, biotin was conjugated with chlorin e6 to develop a new tumor-targeting photosensitizer, Ce6-biotin. The Ce6-biotin had good water solubility and low aggregation. The singlet-oxygen generation rate of Ce6-biotin was slightly increased compared to Ce6. Flow cytometry and confocal laser scanning microscopy results confirmed Ce6-biotin had higher binding affinity toward biotin-receptor-positive HeLa human cervical carcinoma cells than its precursor, Ce6. Due to the BR-targeting ability of Ce6-biotin, it exhibited stronger cytotoxicity to HeLa cells upon laser irradiation. The IC50 against HeLa cells of Ce6-biotin and Ce6 were 1.28 µM and 2.31 µM, respectively. Furthermore, both Ce6-biotin and Ce6 showed minimal dark toxicity. The selectively enhanced therapeutic efficacy and low dark toxicity suggest that Ce6-biotin is a promising PS for BR-positive-tumor-targeting photodynamic therapy. |
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| Keywords: | biotin photosensitizer chlorin e6 photodynamic therapy |
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