非抗菌活性红霉素衍生物研究进展  

Recent developments in erythromycin derivatives with non-antibacterial activity

作　　者：孙俊[1,2] 赵红卫[1] 张为革[2] 

机构地区：[1]河南省人民医院药学部,河南郑州450003 [2]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2015年第8期660-668,共9页Journal of Shenyang Pharmaceutical University

基　　金：国家自然科学基金资助项目(30973614)

摘　　要：目的综述非抗菌活性红霉素衍生物的研究进展。方法依据国内外近期公开发表的40篇文献,对非抗菌活性红霉素衍生物的研究进展进行分类、归纳与总结。结果长期以来,红霉素及其衍生物作为抗菌药物被广泛使用。在临床实践中人们发现,该类化合物还具有一些新的生物活性,例如促进消化道运动、抗炎/免疫调节、抗寄生虫、抗肿瘤、拮抗黄体生成素释放激素、以及抑制磷酸二酯酶-3等活性。为提高新活性降低其抗菌作用,已经设计、合成了多种类型的新结构红霉素衍生物。结论利用红霉素衍生物的新活性研制、开发新药已经成为研究热点。Objective To review the recent developments in erythromycin derivatives with non-antibacterial activity. Methods According to forty of the published papers and patents, the recent developments in erythro- mycin derivatives with non-antibacterial activity were classified and summarized. Results Erythromycin and its derivatives had been extensively used in the treatment of bacterial infections for decades, however, indica- ted that they also have some new bioactivities. Such as motiline-like activity, anti-inflammatory and/or im- munomodulatory activity, antiparasitic activity, antitumor activity, luteinizing hormone-releasing hormone in- hibitory activity, and phosphodiesterase-3 inhibitory activity. In order to maximize these new activities of e- rythromycin while attenuate its antibacterial activity, several series of novel erythromycin derivatives had been designed and synthesized. Conclusions The research and development of erythromycin derivatives with new bioactivities have gradually become an important part of erythromycin derivatives research, which pos- sess a good prospect.

关 键 词：红霉素 衍生物 非抗菌活性 构效关系 

分 类 号：R914[医药卫生—药物化学]