Novel Anti-Acanthamoebic Activities of Irosustat and STX140 and Their Nanoformulations

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dc.authoridSiddiqui, Ruqaiyyah/0000-0001-9646-6208
dc.authoridKhan, Naveed/0000-0001-7667-8553
dc.authorid/0000-0003-3255-9135
dc.authoridZareei, Seyed Omar/0000-0002-0212-2146
dc.authoridRawas-Qalaji, Mutasem/0000-0001-8890-3818
dc.authoridAnbar, Hanan/0000-0003-3691-2813
dc.authoridJagal, Jayalakshmi/0000-0002-8486-0926
dc.authorwosidKhan, Naveed/KCK-0156-2024
dc.authorwosidSiddiqui, Ruqaiyyah/AIF-2100-2022
dc.authorwosidKhan, Naveed/AAM-2892-2021
dc.contributor.authorSiddiqui, Ruqaiyyah
dc.contributor.authorRawas-Qalaji, Mutasem
dc.contributor.authorEl-Gamal, Mohammed I.
dc.contributor.authorSajeev, Sreedevi
dc.contributor.authorJagal, Jayalakshmi
dc.contributor.authorZaraei, Seyed-Omar
dc.contributor.authorSbenati, Rawan M.
dc.date.accessioned2024-05-19T14:38:46Z
dc.date.available2024-05-19T14:38:46Z
dc.date.issued2023
dc.departmentİstinye Üniversitesien_US
dc.description.abstractPathogenic Acanthamoeba produce keratitis and fatal granulomatous amoebic encephalitis. Treatment remains problematic and often ineffective, suggesting the need for the discovery of novel compounds. For the first time, here we evaluated the effects of the anticancer drugs Irosustat and STX140 alone, as well as their nanoformulations, against A. castellanii via amoebicidal, excystment, cytopathogenicity, and cytotoxicity assays. Nanoformulations of the compounds were successfully synthesized with high encapsulation efficiency of 94% and 82% for Irosustat and STX140, respectively. Nanoparticles formed were spherical in shape and had a unimodal narrow particle size distribution, mean of 145 and 244 nm with a polydispersity index of 0.3, and surface charge of -14 and -15 mV, respectively. Irosustat and STX140 exhibited a biphasic release profile with almost 100% drug released after 48 h. Notably, Irosustat significantly inhibited A. castellanii viability and amoebae-mediated cytopathogenicity and inhibited the phenotypic transformation of amoebae cysts into the trophozoite form, however their nanoformulations depicted limited effects against amoebae but exhibited minimal cytotoxicity when tested against human cells using lactate dehydrogenase release assays. Accordingly, both compounds have potential for further studies, with the hope of discovering novel anti-Acanthamoeba compounds, and potentially developing targeted therapy against infections of the central nervous system.en_US
dc.description.sponsorshipAmerican University of Sharjah; University of Sharjah, United Arab Emiratesen_US
dc.description.sponsorshipThe authors are grateful to the American University of Sharjah to support this work, as well as University of Sharjah, United Arab Emirates, for providing funds (operational funds of Drug Design and Discovery, Drug Delivery, as well as Virology and Parasitology research groups).en_US
dc.identifier.doi10.3390/antibiotics12030561
dc.identifier.issn2079-6382
dc.identifier.issue3en_US
dc.identifier.pmid36978428en_US
dc.identifier.scopus2-s2.0-85151363966en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.urihttps://doi.org10.3390/antibiotics12030561
dc.identifier.urihttps://hdl.handle.net/20.500.12713/4600
dc.identifier.volume12en_US
dc.identifier.wosWOS:000956946300001en_US
dc.identifier.wosqualityN/Aen_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherMdpien_US
dc.relation.ispartofAntibiotics-Baselen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.snmz20240519_kaen_US
dc.subjectAcanthamoeba Castellaniien_US
dc.subjectCns Infectionsen_US
dc.subjectFree-Living Amoebaeen_US
dc.subjectIrosustaten_US
dc.subjectPlga Nanoparticlesen_US
dc.subjectStx140en_US
dc.titleNovel Anti-Acanthamoebic Activities of Irosustat and STX140 and Their Nanoformulationsen_US
dc.typeArticleen_US

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