刺孢霉素族抗生素的研究进展

Progress in calicheamicins

刺孢霉素(Calicheamicins,CLM)是一族既有广谱抗菌活性又能强效杀伤多种肿瘤细胞的抗生素,从结构上属于烯炔类抗肿瘤抗生素。自从1987年被发现至今,CLM就以其独特的化学结构、优越的生物学活性受到研究者的关注。其杀伤癌细胞的机制是与DNA双螺旋上的小沟结合,通过Bergman环化产生自由基,从而夺取DNA骨架上的氢原子,引起DNA断裂,杀伤肿瘤细胞。近年来科研人员利用单克隆抗体免疫偶联CLM,极大地拓展了CLM在临床上的应用范围。现综述刺孢霉素族抗生素的研究进展和应用前景。

Calicheamicins （CLM） is a family of broad-spectrum antibacterial agents which also has potent antitumor activities. It belongs to enediyne antitumor antibiotics based on the chemistry structure. Ever since the initial reports of CLM in 1987, researchers have been devoting increasing attention to CLM because of its unique chemistry structure and extremely superior biology activity. CLM binds at the DNA minor grooves, followed by capturing hydrogen atoms on DNA framework through Bergman cycle reaction,subsequent double-strand DNA breaking, and finally tumor cells death. Recently, the clinical applications of CLM are greatly extended because of using monoclonal antibody-based immuno-conjugates. The progress on CLM research was reviewed.