Liang Hong-Yu, Jiang Ying, Song Zhi-Bing, Namulinda Tabbisa, Chen Pei-Ran, Chen Zhi-Long, Yan Yi-Jia
Department of Pharmaceutical Science & Technology, Donghua University, Shanghai 201620, China.
Department of Pharmacy, Huadong Hospital, Fudan University, Shanghai 200040, China.
ACS Med Chem Lett. 2024 Jun 27;15(7):1109-1117. doi: 10.1021/acsmedchemlett.4c00202. eCollection 2024 Jul 11.
To discover effective photosensitizers for photodynamic therapy (PDT), a series of new -tetraphenyltetrabenzoporphyrin (-PhTBP) derivatives were designed, prepared, and characterized. All -PhTBPs own two characteristic absorption bands in the range of 450-500 and 600-700 nm and have the ability to generate singlet oxygen upon photoexcitation. Most of the -PhTBPs demonstrated high photoactivity, among which compounds I, I, I, and I induced apoptosis and also exhibited excellent photodynamic activities . Nonetheless, the liver organs of the I and I-PDT groups showed clear calcifications, whereas the liver tissues of the other PDT groups showed no calcification. It was indicated that compared to phenolic -PhTBPs, glycol -PhTBPs exhibited superior biological safety in mice. According to comprehensive evaluations, -PhTBP I displayed excellent photodynamic antitumor efficacy and biological safety and can be regarded as a promising antitumor drug candidate.
为了发现用于光动力疗法（PDT）的有效光敏剂，设计、制备并表征了一系列新型的-四苯基四苯并卟啉（-PhTBP）衍生物。所有的-PhTBPs在450-500和600-700nm范围内都有两个特征吸收带，并且在光激发时具有产生单线态氧的能力。大多数-PhTBPs表现出高光活性，其中化合物I、I、I和I诱导细胞凋亡并且还表现出优异的光动力活性。然而，I和I-PDT组的肝脏器官显示出明显的钙化，而其他PDT组的肝脏组织未显示钙化。结果表明，与酚类-PhTBPs相比，二醇-PhTBPs在小鼠中表现出更高的生物安全性。根据综合评价，-PhTBP I表现出优异的光动力抗肿瘤疗效和生物安全性，可以被视为一种有前途的抗肿瘤药物候选物。
