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一种新型共轭苯乙烯基酮对新型隐球菌中H(+)-ATP酶介导的质子泵浦的抑制作用。

Inhibition of H(+)-ATPase-mediated proton pumping in Cryptococcus neoformans by a novel conjugated styryl ketone.

作者信息

Manavathu E K, Dimmock J R, Vashishtha S C, Chandrasekar P H

机构信息

Division of Infectious Diseases, Department of Internal Medicine, 427 Lande Building, Wayne State University, 550 E. Canfield, Detroit, MI 48201, USA.

出版信息

J Antimicrob Chemother. 2001 Apr;47(4):491-4. doi: 10.1093/jac/47.4.491.

Abstract

We investigated the in vitro susceptibility of clinical isolates of Cryptococcus neoformans to the novel conjugated styryl ketone NC1175 by broth microdilution. The MIC(90) and the MFC of NC1175 for C. neoformans were 1 and 2 mg/L, respectively. NC1175 at low concentrations (1-4 mg/L) completely inhibited the glucose-induced acidification of the external medium caused by the extrusion of intracellular protons mediated by the plasma membrane located H(+)-ATPase. These data suggest that NC1175 is a fungicidal agent for C. neoformans and its possible cellular target(s) include the H(+)-ATPase.

摘要

我们通过肉汤微量稀释法研究了新型共轭苯乙烯基酮NC1175对新生隐球菌临床分离株的体外敏感性。NC1175对新生隐球菌的MIC(90)和MFC分别为1 mg/L和2 mg/L。低浓度(1-4 mg/L)的NC1175完全抑制了由位于质膜的H(+)-ATP酶介导的细胞内质子外排所引起的葡萄糖诱导的细胞外培养基酸化。这些数据表明,NC1175是一种针对新生隐球菌的杀真菌剂,其可能的细胞靶点包括H(+)-ATP酶。

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