Details

Autor(en) / Beteiligte

• Rodríguez-Expósito, Rubén L.
• Reyes-Batlle, María
• Sifaoui, Ines
• Tejedor, David
• García-Tellado, Fernando
• Piñero, José E.
• Lorenzo-Morales, Jacob

Titel

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

Ist Teil von

• Biomedicine & pharmacotherapy, 2022-06, Vol.150, p.113062-113062, Article 113062

Ort / Verlag

France: Elsevier Masson SAS

Erscheinungsjahr

2022

Link zum Volltext

Quelle

EZB Electronic Journals Library

Beschreibungen/Notizen

• The 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. [Display omitted] •Isobenzofuran-1(3H)-one derivatives (QOET) were active against Acanthamoeba spp.•QOET-3 and QOET-9 presented the lowest IC50 values in A. castellanii Neff.•QOET-3 and QOET-9 did not show cytotoxic effect against murine macrophages.•QOET-3 and QOET-9 induced programmed cell death in Acanthamoeba castellanii Neff.