Downey Autumn S, Graczyk Thaddeus K, Sullivan David J
Department of Molecular Microbiology and Immunology, Johns Hopkins Bloomberg School of Public Health, Baltimore, MD 21205, USA.
J Antimicrob Chemother. 2009 Oct;64(4):751-4. doi: 10.1093/jac/dkp296. Epub 2009 Aug 18.
To assess the in vitro activity of the FDA-approved antihelminthic drug pyrvinium pamoate against Entamoeba histolytica and Giardia intestinalis.
A head-to-head comparison of a standard radiolabelled thymidine incorporation assay and the SYBR Green I-based fluorescence assay for determination of in vitro inhibition by pyrvinium and metronidazole was performed.
The 50% inhibitory concentration (IC(50)) for treatment of E. histolytica with pyrvinium was 4-5 microM for both assays compared with 1-2 microM for metronidazole. For pyrvinium treatment of G. intestinalis, an IC(50) of approximately 12 microM was determined by the radiolabelled thymidine assay alone, with maximum inhibition around 60%. In contrast, the IC(50) for metronidazole treatment using this assay was approximately 2 microM.
Pyrvinium is a potential gut lumen agent for treatment of intestinal amoebiasis, but possibly not for giardiasis. SYBR Green I is an alternative screening method for E. histolytica, but not G. intestinalis.
评估美国食品药品监督管理局（FDA）批准的抗蠕虫药物帕罗维铵对溶组织内阿米巴和肠道贾第虫的体外活性。
对标准放射性标记的胸苷掺入试验和基于SYBR Green I的荧光试验进行了直接比较，以测定帕罗维铵和甲硝唑的体外抑制作用。
两种试验中，帕罗维铵治疗溶组织内阿米巴的50%抑制浓度（IC50）均为4-5微摩尔，而甲硝唑为1-2微摩尔。仅通过放射性标记的胸苷试验测定，帕罗维铵治疗肠道贾第虫的IC50约为12微摩尔，最大抑制率约为60%。相比之下，使用该试验甲硝唑治疗的IC50约为2微摩尔。
帕罗维铵是治疗肠道阿米巴病的潜在肠腔药物，但可能不适用于贾第虫病。SYBR Green I是溶组织内阿米巴的一种替代筛选方法，但不适用于肠道贾第虫。
