Synthesis and biological evaluation of 173-dicarboxylethyl-pyropheophorbide-a amide derivatives for photodynamic therapy |
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| Authors: | Wei Zhu Lai-Xing Wang Dan-Ye Chen Ying-Hua Gao Yi-Jia Yan Xiao-Feng Wu Mi Wang Yi-Ping Han Zhi-Long Chen |
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| Institution: | 1. Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai 201620, China;2. Shanghai Changhai Hospital, 200433, China;3. Shanghai Xianhui Pharmaceutical Co. Ltd., Shanghai 200433, China |
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| Abstract: | Three novel 173-dicarboxylethyl-pyropheophorbide-a amide derivatives as photosensitizers for photodynamic therapy (PDT) were synthesized from pyropheophorbide-a (Ppa). Their photophysical and photochemical properties, intracellular localization, photocytotoxicity in vitro and in vivo were investigated. All target compounds exhibited low cytotoxicity in the dark and remarkable photocytotoxicity against human esophageal cancer cells. Among them, 1a showed highest singlet oxygen quantum yield. Upon light activation, 1a exhibited significant photocytotoxicity. After PDT treatment, the growth of Eca-109 tumor in nude mice was significantly inhibited. Therefore, 1a is a powerful and promising antitumor photosensitizer for PDT. |
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| Keywords: | Photosensitizer Photodynamic therapy Chlorophyll Chlorin Tumor |
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