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蛋白酶抑制剂对十二指肠贾第鞭毛虫和甲硝唑耐药阴道毛滴虫的活性。

The activity of protease inhibitors against Giardia duodenalis and metronidazole-resistant Trichomonas vaginalis.

作者信息

Dunn Linda A, Andrews Katherine T, McCarthy James S, Wright Janelle M, Skinner-Adams Tina S, Upcroft Peter, Upcroft Jacqueline A

机构信息

Molecular Genetics Laboratory, Queensland Institute of Medical Research, 300 Herston Road, Brisbane, Qld 4006, Australia.

出版信息

Int J Antimicrob Agents. 2007 Jan;29(1):98-102. doi: 10.1016/j.ijantimicag.2006.08.026. Epub 2006 Nov 29.

Abstract

Antiretroviral protease inhibitors were assessed in vitro for their activity against Giardia duodenalis and Trichomonas vaginalis. Kaletra (a co-formulation of ritonavir and lopinavir) was the most effective overall, with 50% effective drug concentrations (EC(50)) of 1.1-2.7 microM (ritonavir concentration) against G. duodenalis and 6.8-8 microM against metronidazole-sensitive and clinically metronidazole-resistant T. vaginalis. Minimal inhibitory concentrations were 2-2.5 microM and 10-50 microM for G. duodenalis and T. vaginalis, respectively. Within the range of human plasma concentrations for ritonavir, only G. duodenalis was inhibited. Lopinavir alone was less inhibitory than ritonavir but was associated with a blockage in cytokinesis of G. duodenalis trophozoites. Saquinavir was not effective. These findings are significant considering the association between human immunodeficiency virus and T. vaginalis, and between G. duodenalis and homosexual behaviour.

摘要

对抗逆转录病毒蛋白酶抑制剂进行了体外评估,以检测其对十二指肠贾第鞭毛虫和阴道毛滴虫的活性。克力芝(利托那韦和洛匹那韦的复方制剂)总体上最为有效,对十二指肠贾第鞭毛虫的50%有效药物浓度(EC50)为1.1 - 2.7微摩尔(利托那韦浓度),对甲硝唑敏感及临床上对甲硝唑耐药的阴道毛滴虫的EC50为6.8 - 8微摩尔。十二指肠贾第鞭毛虫和阴道毛滴虫的最低抑菌浓度分别为2 - 2.5微摩尔和10 - 50微摩尔。在利托那韦的人体血浆浓度范围内,仅十二指肠贾第鞭毛虫受到抑制。单独使用洛匹那韦的抑制作用比利托那韦小,但与十二指肠贾第鞭毛虫滋养体的胞质分裂受阻有关。沙奎那韦无效。考虑到人类免疫缺陷病毒与阴道毛滴虫以及十二指肠贾第鞭毛虫与同性恋行为之间的关联,这些发现具有重要意义。

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