| 氯霉素的糖基化修饰及其抗菌活性研究 |
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| 引用本文： | 杨桂华,房俊强,张厚程,杜宇国,于广利.氯霉素的糖基化修饰及其抗菌活性研究[J].中国海洋大学学报(自然科学版),2007,37(3):423-426,452. |
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| 作者姓名： | 杨桂华 房俊强 张厚程 杜宇国 于广利 |
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| 作者单位： | 中国海洋大学海洋药物与食品研究所,山东,青岛,266003;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;中国科学院生态环境研究中心,北京,100085 |
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| 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。
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| 关 键 词： | 氯霉素 糖基化 抗菌活性 |
| 文章编号： | 1672-5174（2007）03-423-05 |
| 修稿时间： | 2006-06-302006-10-18 |
Study on the Antibacterial Activity of Glycosylchloramphenicol Analogues |
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| YANG Gui-Hua,FANG Jun-Qiang,ZHANG Hou-Cheng,DU Yu-Guo,YU Guang-Li.Study on the Antibacterial Activity of Glycosylchloramphenicol Analogues[J].Periodical of Ocean University of China,2007,37(3):423-426,452. |
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| Authors: | YANG Gui-Hua FANG Jun-Qiang ZHANG Hou-Cheng DU Yu-Guo YU Guang-Li |
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| Abstract: | 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. |
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| Keywords: | Chloramphenicol glycosylation antibacterial activity |
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