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盐霉素(salinomycin)是由白色链霉菌(Streptomyces albus)产生的一元羧酸聚醚类抗生素,具有较强的抗革兰氏阳性菌和杀灭球虫的作用,而且对环境污染也较低;此外,还能特异性地抑制多种肿瘤细胞及肿瘤干细胞的生长,具有多重作用靶点,有望成为抗肿瘤的特效药。为提高盐霉素的产量,人们采用传统诱变技术和现代分子遗传学手段,对盐霉素产生菌进行了改造,获得了高产菌株;同时,通过对盐霉素化学结构进行修饰或者通过药物载体和联合用药等,增强了其活性和靶向性、减少了毒副作用。本文对盐霉素产生菌的改造策略、药物靶向性提高和活性优化等研究进展进行综述,并对今后的研究热点进行展望。
Salinomycin is a monocarboxylic acid polyether antibiotic produced by Streptomyces albus with a strong resistance to Gram-positive bacteria and coccidiosis, as well as low environmental pollution ; In addition, it can also specifically inhibit the growth of a variety of tumor cells and cancer stem cells, with multiple targets, is expected to become anti-tumor drug. In order to improve the yield of salinomycin, the traditional method of mutagenesis and modern molecular genetics were used to transform salinomycin-producing bacterium to obtain high-yielding strain. At the same time, by modifying the chemical structure of salinomycin, Carrier and combination therapy, etc., to enhance its activity and targeting, reducing the side effects. This article reviews the research progress of salinomycin producing strains, such as the strategy of drug-targeted improvement and activity optimization, and prospects the research hot spots in the future.