In vitro activity of pyrvinium pamoate against Entamoeba histolytica and Giardia intestinalis using radiolabelled thymidine incorporation and an SYBR Green I-based fluorescence assay

Autumn S. Downey, Thaddeus K. Graczyk, David J Sullivan

Research output: Contribution to journalArticle

Abstract

Objectives: To assess the in vitro activity of the FDA-approved antihelminthic drug pyrvinium pamoate against Entamoeba histolytica and Giardia intestinalis. Methods: 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. Results: The 50% inhibitory concentration (IC50) for treatment of E. histolytica with pyrvinium was 4-5 μM for both assays compared with 1-2 μM for metronidazole. For pyrvinium treatment of G. intestinalis, an IC50 of ∼12 μM was determined by the radiolabelled thymidine assay alone, with maximum inhibition around 60%. In contrast, the IC50 for metronidazole treatment using this assay was ∼2 μM. Conclusions: 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.

Original languageEnglish (US)
Pages (from-to)751-754
Number of pages4
JournalThe Journal of antimicrobial chemotherapy
Volume64
Issue number4
DOIs
StatePublished - 2009

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Giardia lamblia
Entamoeba histolytica
Thymidine
Fluorescence
Inhibitory Concentration 50
Metronidazole
Amoebic Dysentery
Giardiasis
In Vitro Techniques
pyrvinium
SYBR Green I
Pharmaceutical Preparations

Keywords

  • Drug
  • Drug assay
  • Protozoan

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)
  • Infectious Diseases

Cite this

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title = "In vitro activity of pyrvinium pamoate against Entamoeba histolytica and Giardia intestinalis using radiolabelled thymidine incorporation and an SYBR Green I-based fluorescence assay",
abstract = "Objectives: To assess the in vitro activity of the FDA-approved antihelminthic drug pyrvinium pamoate against Entamoeba histolytica and Giardia intestinalis. Methods: 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. Results: The 50{\%} inhibitory concentration (IC50) for treatment of E. histolytica with pyrvinium was 4-5 μM for both assays compared with 1-2 μM for metronidazole. For pyrvinium treatment of G. intestinalis, an IC50 of ∼12 μM was determined by the radiolabelled thymidine assay alone, with maximum inhibition around 60{\%}. In contrast, the IC50 for metronidazole treatment using this assay was ∼2 μM. Conclusions: 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.",
keywords = "Drug, Drug assay, Protozoan",
author = "Downey, {Autumn S.} and Graczyk, {Thaddeus K.} and Sullivan, {David J}",
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AU - Downey, Autumn S.

AU - Graczyk, Thaddeus K.

AU - Sullivan, David J

PY - 2009

Y1 - 2009

N2 - Objectives: To assess the in vitro activity of the FDA-approved antihelminthic drug pyrvinium pamoate against Entamoeba histolytica and Giardia intestinalis. Methods: 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. Results: The 50% inhibitory concentration (IC50) for treatment of E. histolytica with pyrvinium was 4-5 μM for both assays compared with 1-2 μM for metronidazole. For pyrvinium treatment of G. intestinalis, an IC50 of ∼12 μM was determined by the radiolabelled thymidine assay alone, with maximum inhibition around 60%. In contrast, the IC50 for metronidazole treatment using this assay was ∼2 μM. Conclusions: 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.

AB - Objectives: To assess the in vitro activity of the FDA-approved antihelminthic drug pyrvinium pamoate against Entamoeba histolytica and Giardia intestinalis. Methods: 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. Results: The 50% inhibitory concentration (IC50) for treatment of E. histolytica with pyrvinium was 4-5 μM for both assays compared with 1-2 μM for metronidazole. For pyrvinium treatment of G. intestinalis, an IC50 of ∼12 μM was determined by the radiolabelled thymidine assay alone, with maximum inhibition around 60%. In contrast, the IC50 for metronidazole treatment using this assay was ∼2 μM. Conclusions: 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.

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