Targeting pathogenic Acanthamoeba castellanii using DNA minor groove binding agents

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dc.authorscopusidRuqaiyyah Siddiqui / 18635417000
dc.authorscopusidNaveed Ahmed Khan / 58685542900
dc.authorwosidRuqaiyyah Siddiqui / AIF-2100-2022
dc.authorwosidNaveed Ahmed Khan / GWD-0187-2022
dc.contributor.authorAlniss, Hasan Y.
dc.contributor.authorSajeev, Sreedevi
dc.contributor.authorSiddiqui, Ruqaiyyah
dc.contributor.authorDaalah, Meshal
dc.contributor.authorAlawfi, Bader S.
dc.contributor.authorAl-Jubeh, Hadeel M.
dc.contributor.authorRavi, Anil
dc.contributor.authorKhan, Naveed Ahmed
dc.date.accessioned2025-06-18T12:09:47Z
dc.date.available2025-06-18T12:09:47Z
dc.date.issued2024
dc.departmentİstinye Üniversitesi, Tıp Fakültesi, Cerrahi Tıp Bilimleri Bölümü
dc.description.abstractDNA minor groove binders exhibit a high degree of sequence specificity and have a variety of biological actions including antiviral, anticancer, antibacterial, and anti-protozoal properties. Since it is the location of non-covalent interactions, the minor groove of double helical B-DNA is gaining significant interest as therapeutic targets. For the purpose of this investigation, the synthesis of five novel DNA minor groove binding agents was accomplished and antiparasitic efficacies were determined against Acanthamoeba castellanii of the T4 genotype in vitro. Using amoebicidal assays, the results revealed that all inhibitors tested showed significant killing of amoebae (P < 0.05). Pre-treatment of amoebae with DNA minor groove binders inhibited parasite-mediated human cell death by measuring lactate dehydrogenase release using cytopathogenicity assays. Cytotoxicity assays revealed minimal effects on human cells. As phenotypic switching leads to infection recurrence, assays revealed that inhibitors blocked amoebae phenotypic transformation. These are promising findings and suggest that DNA minor groove binders may hold promise for further research in the effective eradication of pathogenic A. castellanii.
dc.identifier.citationAlniss, H. Y., Sajeev, S., Siddiqui, R., Daalah, M., Alawfi, B. S., Al-Jubeh, H. M., ... & Khan, N. A. (2024). Targeting pathogenic Acanthamoeba castellanii using DNA minor groove binding agents. Acta Tropica, 260, 107451.
dc.identifier.doi10.1016/j.actatropica.2024.107451
dc.identifier.endpage6
dc.identifier.issn0001-706X
dc.identifier.issn1873-6254
dc.identifier.pmid39510437
dc.identifier.scopus2-s2.0-85208969266
dc.identifier.scopusqualityQ2
dc.identifier.startpage1
dc.identifier.urihttp://dx.doi.org/10.1016/j.actatropica.2024.107451
dc.identifier.urihttps://hdl.handle.net/20.500.12713/7313
dc.identifier.volume260
dc.identifier.wosWOS:001361387900001
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.institutionauthorSiddiqui, Ruqaiyyah
dc.institutionauthorKhan, Naveed Ahmed
dc.institutionauthoridRuqaiyyah Siddiqui / 0000-0001-9646-6208
dc.institutionauthoridNaveed Ahmed Khan / 0000-0001-7667-8553
dc.language.isoen
dc.publisherElsevier b.v.
dc.relation.ispartofActa tropica
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectAcanthamoeba
dc.subjectCytopathogenicity
dc.subjectCytotoxicity
dc.subjectDNA Minor Groove Binders (MGBs)
dc.subjectParasites
dc.subjectTreatment
dc.titleTargeting pathogenic Acanthamoeba castellanii using DNA minor groove binding agents
dc.typeArticle

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