In vitro Antimicrobial Activity Comparison of Linezolid, Tedizolid, Sutezolid and Delpazolid Against Slowly Growing Mycobacteria Isolated in Beijing, China.
In vitro Antimicrobial Activity Comparison of Linezolid, Tedizolid, Sutezolid and Delpazolid Against Slowly Growing Mycobacteria Isolated in Beijing, China.
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利奈唑胺、泰地唑胺、苏特唑胺和地帕唑胺对中国北京分离的缓慢生长分枝杆菌的体外抗菌活性比较
DOI：
10.2147/idr.s332835
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发表时间：
2021
影响因子：
3.9
通讯作者：
Huang H
中科院分区：
文献类型：
--
作者：
Yu X;Huo F;Wang F;Wen S;Jiang G;Xue Y;Dong L;Zhao L;Zhu R;Huang H
背景一些新型恶唑烷酮类化合物对慢生长分枝杆菌（SGM）的抑菌活性尚未得到很好的评价。方法对20株参比菌株和157株不同SGM菌株对4种恶唑烷酮类药物delpazolid、sutezolid、tedizolid和linezolid的体外敏感性进行评价。此外，还检测了利奈唑胺耐药与23srRNA、rplC、rplD突变的关系。结果Sutezolid对临床分离的胞内支原体抗菌活性最强，MIC50为2 μg/mL， MIC90为4 μg/mL。舒替唑胺对胞内支原体和鸟型支原体的mic通常比利奈唑胺低4- 8倍。实验分离的堪萨斯分枝杆菌对4种恶唑烷酮均敏感。根据多序列比对，本研究在M. avium细胞内发现了新的23srRNA突变（A2267C和A2266G）和rplD突变（Thr147Ala），这些突变可能参与了对利奈唑胺的抗性。结论本研究表明，舒替唑胺对胞内M.、鸟型M.和堪萨斯M.具有较强的体外抑制活性，为恶唑烷酮类药物治疗SGM感染的潜在临床应用提供了重要启示。
Background The antimicrobial activities of some new oxazolidinones against slowly growing mycobacteria (SGM) have never been well evaluated. Methods We evaluate the in vitro susceptibility of 20 reference strains and 157 clinical isolates, pertaining different SGM species, against four oxazolidinones, ie, delpazolid, sutezolid, tedizolid and linezolid. In addition, the association of linezolid resistance and mutations in 23srRNA, rplC, rplD were also tested. Results Sutezolid presented the strongest antimicrobial activity against the clinical isolates of M. intracellulare than the other oxazolidinones, with MIC50 at 2 μg/mL and MIC90 at 4 μg/mL. MICs of sutezolid were usually 4- to 8-fold lower than these of linezolid against M. intracellulare and M. avium. The tested isolates of M. kansasii were susceptible to all of the four oxazolidinones. According to the multiple sequence alignment, novel 23srRNA mutations (A2267C and A2266G) in M. intracellulare and rplD mutations (Thr147Ala) in M. avium were identified in this study which have plausible involvement in rendering resistance against linezolid. Conclusion This study showed that sutezolid harbors the strongest inhibitory activity against M. intracellulare, M. avium and M. kansasii in vitro, which provided important insights on the potential clinical application of oxazolidinones for treating SGM infections.