Novel anti-Acanthamoebic properties of raloxifene sulfonate/sulfamate derivatives

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dc.authoridSiddiqui, Ruqaiyyah/0000-0001-9646-6208
dc.authoridKhan, Naveed/0000-0001-7667-8553
dc.authoridZareei, Seyed Omar/0000-0002-0212-2146
dc.authorwosidSiddiqui, Ruqaiyyah/AIF-2100-2022
dc.authorwosidKhan, Naveed/AAM-2892-2021
dc.authorwosidKhan, Naveed/KCK-0156-2024
dc.contributor.authorSiddiqui, Ruqaiyyah
dc.contributor.authorEl-Gamal, Mohammed I.
dc.contributor.authorSajeev, Sreedevi
dc.contributor.authorZaraei, Seyed-Omar
dc.contributor.authorKhan, Naveed Ahmed
dc.date.accessioned2024-05-19T14:38:47Z
dc.date.available2024-05-19T14:38:47Z
dc.date.issued2023
dc.departmentİstinye Üniversitesien_US
dc.description.abstractAcanthamoeba are known to cause a vision threatening eye infection typically due to contact lens wear, and an infection of the central nervous system. The ability of these amoebae to switch phenotypes, from an active trophozoite to a resistant cyst form is not well understood; the cyst stage is often resistant to chemotherapy, which is of concern given the rise of contact lens use and the ineffective disinfectants available, versus the cyst stage. Herein, for the first time, a range of raloxifene sulfonate/sulfamate derivatives which target nucleotide pyrophosphatase/phosphodiesterase enzymes, were assessed using amoebicidal and excystation tests versus the trophozoite and cyst stage of Acanthamoeba. Moreover, the potential for cytopathogenicity inhibition in amoebae was assessed. Each of the derivatives showed considerable anti-amoebic activity as well as the ability to suppress phenotypic switching (except for compound 1a). Selected raloxifene derivatives reduced Acanthamoeba-medi-ated host cell damage using lactate dehydrogenase assay. These findings suggest that pyrophosphatase/phosphodiesterase enzymes may be valuable targets against Acanthamoeba infections.en_US
dc.identifier.doi10.1016/j.molbiopara.2023.111582
dc.identifier.issn0166-6851
dc.identifier.issn1872-9428
dc.identifier.pmid37562558en_US
dc.identifier.scopus2-s2.0-85170221499en_US
dc.identifier.scopusqualityQ3en_US
dc.identifier.urihttps://doi.org10.1016/j.molbiopara.2023.111582
dc.identifier.urihttps://hdl.handle.net/20.500.12713/4603
dc.identifier.volume256en_US
dc.identifier.wosWOS:001072866600001en_US
dc.identifier.wosqualityN/Aen_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.relation.ispartofMolecular and Biochemical Parasitologyen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.snmz20240519_kaen_US
dc.subjectAcanthamoebaen_US
dc.subjectAnti-Amoebicen_US
dc.subjectCns Infectionsen_US
dc.subjectFree-Living Amoebaeen_US
dc.subjectRaloxifene Derivativesen_US
dc.titleNovel anti-Acanthamoebic properties of raloxifene sulfonate/sulfamate derivativesen_US
dc.typeArticleen_US

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