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Title

Isobenzofuran-1(3H)-one derivatives: Amoebicidal activity and program cell death in Acanthamoeba castellanii Neff

AuthorsRodríguez-Expósito, Rubén L.; Reyes-Batlle, María; Sifaoui, Inés; Tejedor, David CSIC ORCID CVN ; García-Tellado, Fernando CSIC ORCID ; Piñero, José E.; Lorenzo-Morales, Jacob
KeywordsAcanthamoeba
Isobenzofuran-1(3H)-ones
PCD
Issue Date6-May-2022
PublisherElsevier
CitationBiomedicine & Pharmacotherapy 150, 113062 : 1-10 (2022)
AbstractThe genus Acanthamoeba is characterized by being a group of ubiquitous and free-living amoebae that inhabit a variety of environments. Generally, human infections by this parasite are associated with Acanthamoeba keratitis, especially in contact lens wearers, and with chronic but fatal granulomatous amoebic meningoencephalitis. Current treatments used for eradication of amoeba from infection sites represent a challenge for pharmacotherapy, due to the lack of effective treatment and the amoebae highly resistant to anti-amoebic drugs. In this study, we describe the results of the assessment of the IC50 of 10 isobenzofuran-1(3H)-one derivatives (QOET) against four Acanthamoeba strains. The compounds QOET-3 and QOET-9 were the selected derivatives with the lowest IC50 in A. castellanii Neff trophozoites (73.71 ± 0.25 and 69.99 ± 15.32 μM, respectively). Interestingly, analysis of the compound effects on the cell apoptosis-like features showed that both active molecules triggered programmed cell death (PCD) in A. castellanii Neff. The results obtained in this study highlights that isobenzofuranone derivatives could represent an interesting source for developing novel antiamoebic drugs.
Publisher version (URL)https://doi.org/10.1016/j.biopha.2022.113062
URIhttp://hdl.handle.net/10261/268990
DOI10.1016/j.biopha.2022.113062
ISSN0753-3322
Appears in Collections:(IPNA) Artículos




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