Li Xiong, Xie Chen, Zha Shuai, Tam Wing Sze, Jiang Mingjun, Wong Ka-Leung
Department of Chemistry, Hong Kong Baptist University Kowloon, Hong Kong S.A.R., P. R. China.
Chempluschem. 2022 Aug 10;87(11):e202200184. doi: 10.1002/cplu.202200184.
Epstein-Barr virus (EBV) is a common human-infected virus related to many diseases and cancers. Recently, some peptides have been found to serve targeting and therapeutic roles by inhibiting EBNA1, an oncoprotein of the EBV. We herein report the conjugation of the EBNA1-targeting peptides and porphyrins which can bring synergistic effects by both introducing more specific treatments (photodynamic therapy) and improving the biocompatibility of the photosensitizer and the peptides. One of our compounds exhibited significant photo-cytotoxicity where the Lethal Concentration 50 (LC )=6.1 μM in EBV-positive cells. Besides, in vitro cell imaging and co-staining can also be achieved simultaneously and suggested the binding inside nucleus.
爱泼斯坦-巴尔病毒（EBV）是一种常见的人类感染病毒，与许多疾病和癌症有关。最近，人们发现一些肽通过抑制EBV的一种癌蛋白EBNA1发挥靶向和治疗作用。我们在此报告了EBNA1靶向肽与卟啉的缀合，通过引入更具特异性的治疗方法（光动力疗法）以及提高光敏剂和肽的生物相容性，二者可产生协同效应。我们的一种化合物表现出显著的光细胞毒性，在EBV阳性细胞中半数致死浓度（LC₅₀）=6.1 μM。此外，还可同时实现体外细胞成像和共染色，并表明其在细胞核内的结合。
