论文部分内容阅读
现阶段,应用较为广泛的一种广谱抗生素便是氟喹诺酮类药物,在世界的抗生素类的药物市场上它占了大概18%的比重。氟喹诺酮类药物不仅能够迅速的杀菌,同时还有一个规模较大的衍生物库,为药物的换代更新创造了有利条件。然而,此类衍生物在代谢的过程、杀菌速度方面对蛋白合成的依赖性及对氧的需求各不相同。根据药物作用之后细菌分子遗传层面所表现出来的应答特点我们能够分析出不同的衍生物的深层次的作用体制,能够为研制疗效更好的新型的喹诺酮类药物创造条件。活性氧簇、染色体的片段化、细菌程序性的死亡、霉素-抗霉素的系统及SOS应答等新的机制在某种程度上参与了喹诺酮类药物杀菌的过程。笔者在本文中着重分析了喹诺酮作用的“二步特征”。引入这一特征不仅能够更好的理解各种喹诺酮类药物所具有的杀菌特点,同时还有利于新型喹诺酮类药物的研发。
At this stage, a widely used broad-spectrum antibiotic is fluoroquinolone, accounting for about 18% of the world’s antibiotic-based drugs market. Fluoroquinolones can not only sterilize rapidly, but also have a large library of derivatives that provide favorable conditions for drug replacement. However, the dependence of such derivatives on protein synthesis and on the oxygen demand in the metabolic process, the rate of sterilization, varies. According to the response characteristics of the molecular level of bacteria after drug action, we can analyze the deep-level action mechanism of different derivatives, which can create the conditions for the development of new quinolone drugs with better therapeutic effects. New mechanisms, such as reactive oxygen species (ROS), fragmentation of chromosomes, bacterial programmed death, systemic and SOS responses to mycotoxin and antimycin, are somewhat involved in the disinfection of quinolones. In this paper, the author focuses on the analysis of quinolone’s “two-step characteristics”. The introduction of this feature not only provides a better understanding of the bactericidal properties of various quinolones, but also facilitates the development of novel quinolones.