Fitzgerald K A, Davies A, Russell A D
Welsh School of Pharmacy, University of Wales College of Cardiff, U.K.
FEMS Microbiol Lett. 1989 Aug;51(3):327-32. doi: 10.1016/0378-1097(89)90419-9.
Uptake of 14C-labelled chlorhexidine diacetate (14C-CHA) by wild-type and envelope mutant strains of Escherichia coli and Pseudomonas aeruginosa was very rapid. Maximum uptake was observed within a contact time of 20 s with no additional binding on increased contact, and was concentration-dependent. In contrast to this rapid binding of 14C-CHA, bactericidal studies revealed that the lethal activity of low concentrations of unlabelled CHA was slow, although higher concentrations had a rapid effect. Comparison of a wild-type strain with its envelope mutants indicated that there was little difference in 14C-CHA uptake, in minimal inhibitory concentrations or in bactericidal activity. Azolectin was found to be an effective neutralising agent of biguanide action, but in in vitro agar tests and in reducing or removing the amount of 14C-CHA taken up by the cells.
野生型和包膜突变型大肠杆菌及铜绿假单胞菌对14C标记的双醋酸氯己定（14C-CHA）的摄取非常迅速。在20秒的接触时间内观察到最大摄取量，延长接触时间没有额外的结合，且摄取量呈浓度依赖性。与14C-CHA的这种快速结合形成对比的是，杀菌研究表明低浓度未标记的CHA的致死活性缓慢，尽管高浓度有快速作用。野生型菌株与其包膜突变体的比较表明，14C-CHA摄取、最低抑菌浓度或杀菌活性方面几乎没有差异。发现卵磷脂是双胍作用的有效中和剂，但在体外琼脂试验中以及在减少或去除细胞摄取的14C-CHA量方面有效。
