前药
化学
光敏剂
癌细胞
体内
组合化学
癌症
核黄素
血桂碱
原位
癌症治疗
光动力疗法
荧光
生物物理学
生物化学
癌症研究
药理学
立体化学
生物碱
光化学
有机化学
内科学
生物技术
量子力学
物理
医学
生物
作者
Xin Yang,Limin Ma,Hongwei Shao,Zikai Zhou,Lang Xia,Mengyu Yao,Guowen Luo,Stefano Scoditti,Emilia Sicilia,Gloria Mazzone,Meng Gao,Ben Zhong Tang
标识
DOI:10.1021/acs.jmedchem.2c01262
摘要
Cancer therapies usually suffer from poor targeting ability and serious side effects. Photoactivatable cancer therapy has the significant advantage of a high spatiotemporal resolution, but most photoactivatable prodrugs require decoration with stoichiometric photocleavable groups, which are only responsive to ultraviolet irradiation and suffer from low reaction efficiency. To tackle these challenges, we herein propose a photoactivation strategy with biogenic riboflavin as the photosensitizer to promote the in situ transformation of noncytotoxic dihydroalkaloid prodrugs dihydrochelerythrine (DHCHE), dihydrosanguinarine (DHSAN), and dihydronitidine (DHNIT) into anticancer alkaloid drugs chelerythrine (CHE), sanguinarine (SAN), and nitidine (NIT), respectively, which can efficiently kill cancer cells and inhibit in vivo tumor growth. Meanwhile, the photoactivatable transformation can be in situ monitored by green-to-red fluorescence conversion, which will contribute to easy controlling of the therapeutic dose. The proposed photoactivatable transformation mechanism was also explored by density functional theory (DFT) calculations. We believe this riboflavin-promoted and imaging-guided photoactivation strategy is promising for precise cancer therapy.
科研通智能强力驱动
Strongly Powered by AbleSci AI