摘要
抗生素发现"黄金时代"的结束以及日趋严重的抗生素耐药性问题给我们留下一个戏剧性的、缺乏新型药物来防治耐药病原体感染的难题。这使得从现有非抗生素药物中筛查抗菌活性药物成为一种新尝试。近期研究表明:美国食品药品监督管理局(FDA)批准的、本来用于治疗高血钙的药物硝酸镓具有良好的抗菌活性。不同于其他抗生素,镓的药理性质依靠化学拟态,它可以在目标酶分子中取代铁,从而干扰、扰乱细菌含铁蛋白的功能及细菌代谢,无论是在体外实验还是在体内实验中,镓对多种病原体,包括多重耐药病原体都表现出杀菌活性。因此一些含镓制剂有望被开发成有潜力的非传统抗菌药物,帮助治疗多重耐药细菌感染。
The end of the ＂golden age＂ of antibiotic discovery along with the growing antibiotic resistance left us a dramatic shortage of new drugs to prevent and cure drug-resistant pathogens. This makes it a new alternative approach to screen antibacterial activity from existing non-antimicrobial drugs. Recent studies show that gallium nitrate, a compound approved for treatment of hypercalcemia by US FDA, has potent antibacterial activities. Unlike classical antibiotics, the pharmacological property of gallium lies on its chemical mimicry, which can cause malfunction and disruption of enzymes using iron as a co-factor, and thus interfere with bacterial metabolism. Gallium has shown bactericidal activity against many pathogens, including multidrug-resistant ones, both in vitro and in vivo. Some gallium-containing regimens are expected to be developed as non-traditional and potentially effective anti- infective agents that help combat multidrug-resistant bacterial infections.
作者
吕毅华
李昕
刘周
李家斌
王岱
薛云新
赵西林
Lu Yi-hua;Li Xin;Liu Zhou;Li Jia-binz;,;Wang Dai;Xue Yun-xin(State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, Xiamen University, Xiamen 361102;Department of Infectious Diseases, First Affiliated Hospital of Anhui Medical University, Hefei 230022;Aihui Bacterial Drug Resistance Surveillance Center, Hefei 230022;Department of Infectious Diseases, Chaohu Hospital Affiliated to Anhui Medical University, Chaohu 238000)
出处
《中国抗生素杂志》
CAS
CSCD
2018年第4期394-400,共7页
Chinese Journal of Antibiotics
基金
国家自然科学基金(No.81673242、No.81473251、No.31741006、No.31370166和No.81301474)
福建省自然科学基金(No.2014J01139和No.2015J01345)
厦门大学校长基金(No.20720160060)
关键词
镓
抗菌
多重耐药病原菌
Gallium
Antibacterial
Multidrug-resistant pathogens
