一种基于在癌细胞中过表达的半胱氨酸激活的新型血卟啉衍生物类光敏剂。
A novel photosensitizer based on hypocrellin B activated by cysteine over-expressed in cancer cells.
机构信息
Department of Applied Chemistry, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama 223-8522, Japan.
出版信息
Org Biomol Chem. 2024 Sep 11;22(35):7187-7193. doi: 10.1039/d4ob01288g.
L-Cysteine (Cys)-activatable photosensitizer 3 was designed and synthesized based on hypocrellin B (1). Cys is a novel tumor-associated biomarker. 3 exhibited negligible photosensitizing ability without Cys. However, when 1 was released from 3 by reaction with Cys, the photosensitizing activity was restored. Furthermore, 3 showed selective and effective photo-cytotoxicity against only cancer cells such as HeLa and A549 cells that highly express Cys when irradiated with 660 nm light, which is inside the phototherapeutic window.
基于竹红菌素 B（1）设计并合成了半胱氨酸（Cys）激活型光动力剂 3。Cys 是一种新型的肿瘤相关生物标志物。3 在没有 Cys 的情况下几乎没有光敏能力。然而，当 3 与 Cys 反应释放 1 时，光敏活性得到恢复。此外，当用 660nm 光照射时，3 对高表达 Cys 的癌细胞（如 HeLa 和 A549 细胞）表现出选择性和有效的光细胞毒性，这一光疗窗口内。
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