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肺炎链球菌野生型和耐药突变体中celiptium的摄取与细胞毒性之间的关系。

Relationship between the uptake and cytotoxicity of celiptium in wild type and resistant mutants of the bacterium Streptococcus pneumoniae.

作者信息

Sautereau A M, Tocanne J F, Trombe M C

出版信息

Biochem Biophys Res Commun. 1987 Jun 15;145(2):927-33. doi: 10.1016/0006-291x(87)91054-0.

Abstract

Celiptium, a cationic and amphiphilic drug currently employed in cancer chemotherapy, was found to be accumulated against its concentration gradient by the bacterium Streptococcus pneumoniae. Accumulation was reduced in Celiptium resistant amiA mutants which were also observed to have reduced electric transmembrane potentials delta psi. This suggested a relationship between Celiptium toxicity and accumulation in S. pneumoniae, and indicated a delta psi - driven uptake in a manner reminiscent of that observed for other lipophilic cations such as tetraphenylphosphonium.

摘要

塞利铂,一种目前用于癌症化疗的阳离子两亲性药物,被发现可被肺炎链球菌逆浓度梯度积累。在对塞利铂耐药的amiA突变体中积累减少,这些突变体也被观察到具有降低的跨膜电位δψ。这表明塞利铂毒性与在肺炎链球菌中的积累之间存在关联,并表明以类似于其他亲脂性阳离子如四苯基鏻所观察到的方式由δψ驱动摄取。

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