以苯硼酸为载体的前药及其类似物的研究进展

Research progress on prodrugs and their analogues containing phenylboronic acid carriers

ROS是机体重要的信号分子,对机体的代谢过程中起着重要的作用。研究发现,在癌症、炎症和神经退行性疾病等疾病组织出现了ROS异常升高的现象。这一现象为治疗以上相关疾病提供了靶点,ROS型敏感型前药应运而生,近年来将苯硼酸基团作为载体引入原药中设计ROS敏感型前药成为基于ROS开发新药的有效途径。本文作者对近年来开发出含苯硼酸结构的前药的设计思路及药效进行综述,所涉及的药物包括传统的化疗药物,生物小分子以及光动力疗法的光敏剂。以上药物均有良好的疗效,但此类前药也面临一些问题。本文作者探讨了这类前药连接臂的选择、合成方法以及释放效果等相关问题。希望为设计更好更合理含苯硼酸结构的前药和提出新的思路。

Objective ROS are important signaling molecules and play an important role in the metabolic processes of the body.It has been found that abnormal elevation of ROS occurs in tissues when people suffering from cancer,inflammation and neurodegenerative diseases.This phenomenon provides a target for the treatment of the above related diseases,and thus ROS-sensitive prodrugs have emerged.In recent years,the introduction of phenylboronic acid moiety as a carrier into medicine structures to design ROS-sensitive prodrugs has been proved to be an effective way.In this paper,the design concepts and efficacies of the phenylboronic acid-containing prodrugs developed in recent years are summarized,including traditional chemotherapeutic drugs,bio-small molecules,and photosensitizers for photodynamic therapy.Although above mentioned medicines have good efficacy,such prodrugs also face some problems.Moreover,the selection of linker arms,synthesis methods and release effects of these prodrugs are discussed.We hope this paper can provide reference for the design of more effective phenylboronic acid-containing prodrugs.