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Evaluating the Antiparasitic Activity of Novel BPZ Derivatives Against Toxoplasma gondii

Prevalence studies revealed that one-third of the human population is chronically infected with Toxoplasma gondii. Presently, such infections are without medical treatment that effectively eradicates the parasite once it is in its latent form. Moreover, the therapeutics used to treat acute infection...

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Detalles Bibliográficos
Autores principales: Hatton, Olivia, Stitzlein, Lea, Dudley, Richard W., Charvat, Robert A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7466062/
https://www.ncbi.nlm.nih.gov/pubmed/32751616
http://dx.doi.org/10.3390/microorganisms8081159
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author Hatton, Olivia
Stitzlein, Lea
Dudley, Richard W.
Charvat, Robert A.
author_facet Hatton, Olivia
Stitzlein, Lea
Dudley, Richard W.
Charvat, Robert A.
author_sort Hatton, Olivia
collection PubMed
description Prevalence studies revealed that one-third of the human population is chronically infected with Toxoplasma gondii. Presently, such infections are without medical treatment that effectively eradicates the parasite once it is in its latent form. Moreover, the therapeutics used to treat acute infections are poorly tolerated by patients and also cause the parasite to convert into long-lasting tissue cysts. Hence, there is a dire need for compounds with antiparasitic activity against all forms of T. gondii. This study examines the antiparasitic capacity of nine novel bisphenol Z (BPZ) derivatives to determine whether they possessed any activity that prevented T. gondii replication. To begin assessing the efficacy of the novel derivatives, parasites were treated with increasing concentrations of the compounds, then doubling assays and MitoTracker staining were performed. Three of the nine compounds demonstrated strong inhibitory activity, i.e., parasite replication significantly decreased with higher concentrations. Additionally, many of the treated parasites exhibited decreases in fluorescent signaling and disruption of mitochondrial morphology. These findings suggest that bisphenol Z compounds disrupt mitochondrial function to inhibit parasite replication and may provide a foundation for the development of new and effective treatment modalities against T. gondii.
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spelling pubmed-74660622020-09-14 Evaluating the Antiparasitic Activity of Novel BPZ Derivatives Against Toxoplasma gondii Hatton, Olivia Stitzlein, Lea Dudley, Richard W. Charvat, Robert A. Microorganisms Communication Prevalence studies revealed that one-third of the human population is chronically infected with Toxoplasma gondii. Presently, such infections are without medical treatment that effectively eradicates the parasite once it is in its latent form. Moreover, the therapeutics used to treat acute infections are poorly tolerated by patients and also cause the parasite to convert into long-lasting tissue cysts. Hence, there is a dire need for compounds with antiparasitic activity against all forms of T. gondii. This study examines the antiparasitic capacity of nine novel bisphenol Z (BPZ) derivatives to determine whether they possessed any activity that prevented T. gondii replication. To begin assessing the efficacy of the novel derivatives, parasites were treated with increasing concentrations of the compounds, then doubling assays and MitoTracker staining were performed. Three of the nine compounds demonstrated strong inhibitory activity, i.e., parasite replication significantly decreased with higher concentrations. Additionally, many of the treated parasites exhibited decreases in fluorescent signaling and disruption of mitochondrial morphology. These findings suggest that bisphenol Z compounds disrupt mitochondrial function to inhibit parasite replication and may provide a foundation for the development of new and effective treatment modalities against T. gondii. MDPI 2020-07-30 /pmc/articles/PMC7466062/ /pubmed/32751616 http://dx.doi.org/10.3390/microorganisms8081159 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Communication
Hatton, Olivia
Stitzlein, Lea
Dudley, Richard W.
Charvat, Robert A.
Evaluating the Antiparasitic Activity of Novel BPZ Derivatives Against Toxoplasma gondii
title Evaluating the Antiparasitic Activity of Novel BPZ Derivatives Against Toxoplasma gondii
title_full Evaluating the Antiparasitic Activity of Novel BPZ Derivatives Against Toxoplasma gondii
title_fullStr Evaluating the Antiparasitic Activity of Novel BPZ Derivatives Against Toxoplasma gondii
title_full_unstemmed Evaluating the Antiparasitic Activity of Novel BPZ Derivatives Against Toxoplasma gondii
title_short Evaluating the Antiparasitic Activity of Novel BPZ Derivatives Against Toxoplasma gondii
title_sort evaluating the antiparasitic activity of novel bpz derivatives against toxoplasma gondii
topic Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7466062/
https://www.ncbi.nlm.nih.gov/pubmed/32751616
http://dx.doi.org/10.3390/microorganisms8081159
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