红霉素基因工程研究进展

红霉素是一类广谱大环内酯类抗生素 ,在临床上具有广泛的应用。近 10年来用基因工程方法对红霉素结构改造已经取得了很大的进展。通过基因工程不仅可以改造红霉素内酯环环的大小、环的骨架和环的侧链 ,而且可以对后修饰的羟基、糖基和甲基进行改造。迄今用基因工程方法合成的新的大环内酯环结构已超过 10 0种 ,所合成的各种红霉素类似物也有数十种 ,且经过基因改造的红霉素类似物都具有生物活性。但基因工程产物产量都普遍降低 ,抑菌活性也不理想 ,因此未来红霉素基因工程研究的重点应加强产量和高活性结构筛选的研究。

Progress in Erythromycin Genetic Engineering

Erythromycin is a broad spectrum macrolide antibiotic and clinically used widely. Great progresses have been made in changing erythromycin structures with genetic manipulation in recent 10 years. By means of genetic engineering, not only could the ring size, the ring backbone and the side chains of erythromycin aglycone be changed, but also the post-modified hydroxyl, glycosyl and methyl could be altered. Until now more than 100 types of novel macrolactones and tens of erythromycin analogs have been produced, and almost all of erythromycin analogs possess biological activity. However, the yield of the genetic products is commonly low, and the antibacterial activity is not satisfactory. So future researches on erythromycin genetic engineering should focus on the output of novel products and the selection of structures with high biological activity.;