氯霉素的糖基化修饰及其抗菌活性研究  

Study on the Antibacterial Activity of Glycosylchloramphenicol Analogues

作　　者：杨桂华[1] 房俊强[2] 张厚程[2] 杜宇国[3] 于广利[1] 

机构地区：[1]中国海洋大学海洋药物与食品研究所,山东青岛266003 [2]山东大学生命科学院微生物技术国家重点实验室,山东济南250100 [3]中国科学院生态环境研究中心,北京100085

出　　处：《中国海洋大学学报（自然科学版）》2007年第3期423-426,452,共5页Periodical of Ocean University of China

摘　　要：制备5种氯霉素糖基化衍生物,并对这些衍生物的抑菌活性和安全性进行初步测试。实验结果表明:1)氯霉素被糖基化后水溶性得到了明显提高;2)氯霉素糖基化衍生物时未产生抗菌活性,但经相关糖苷酶水解后,可重新表现出抗菌活性;3)小鼠急毒试验证明,氯霉素糖基化衍生物的毒副作用与原药相比显著降低。该项研究对于设计和合成类氯霉素前药开辟了新领域。Five glycosylated chloramphenicol derivatives were synthesized in this study. Their antibacterial activities and safety were investigated. The results showed that： 1 ） The water-solubility of the glycosylated analogues were remarkably improved compared to the original chloramphenicol; 2） Though the glycosylated derivatives showed no antibacterial activity, the antibacterial activity was observed when hydrolyzed by some corresponding specific glycosidase; 3） The mouse acute toxicity test showed that the toxicity and the side effects were deeply reduced compared to the original chloramphenicol. This investigation may open a new field in the design and sythesis of shloramphenicol-like prodrugs.

关 键 词：氯霉素 糖基化 抗菌活性 

分 类 号：S482.28[农业科学—农药学]