Azole and 5-nitroimidazole based nanoformulations are potential antiamoebic drug candidates against brain-eating amoebae

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dc.authoridSiddiqui, Ruqaiyyah/0000-0001-9646-6208
dc.authoridHussain, Kashif/0000-0001-7396-938X
dc.authoridKhan, Naveed/0000-0001-7667-8553
dc.authoridShah, Muhammad Raza/0000-0003-4978-3627
dc.authoridAkbar, Noor/0000-0002-8114-1969
dc.authorwosidHussain, Kashif/JDN-2995-2023
dc.authorwosidSiddiqui, Ruqaiyyah/AIF-2100-2022
dc.authorwosidKhan, Naveed/KCK-0156-2024
dc.authorwosidShah, Muhammad Raza/AAR-3981-2021
dc.authorwosidHussain, Kashif/GNP-3705-2022
dc.authorwosidKhan, Naveed/AAM-2892-2021
dc.contributor.authorAkbar, Noor
dc.contributor.authorHussain, Kashif
dc.contributor.authorKhalid, Maria
dc.contributor.authorSiddiqui, Ruqaiyyah
dc.contributor.authorShah, Muhammad Raza
dc.contributor.authorKhan, Naveed Ahmed
dc.date.accessioned2024-05-19T14:45:56Z
dc.date.available2024-05-19T14:45:56Z
dc.date.issued2023
dc.departmentİstinye Üniversitesien_US
dc.description.abstractAim Herein, the anti-parasitic activity of azoles (fluconazole and itraconazole) and 5-nitroimdazole (metronidazole) against the brain-eating amoebae: Naegleria fowleri and Balamuthia mandrillaris was elucidated. Methods and results Azoles and 5-nitroimidazole based nanoformulations were synthesized and characterized using a UV-visible spectrophotometer, atomic force microscopy, and fourier transform infrared spectroscopy. H-1-NMR, EI-MS, and ESI-MS were performed to determine their molecular mass and elucidate their structures. Their size, zeta potential, size distribution, and polydispersity index (PDI) were assessed. Amoebicidal assays revealed that all the drugs and their nanoformulations, (except itraconazole) presented significant anti-amoebic effects against B. mandrillaris, while all the treatments indicated notable amoebicidal properties against N. fowleri. Amoebicidal effects were radically enhanced upon conjugating the drugs with nanoparticles. The IC50 values for KM-38-AgNPs-F, KM-20-AgNPs-M, and KM-IF were 65.09, 91.27, and 72.19 mu g.mL-1, respectively, against B. mandrillaris. Whereas against N. fowleri, the IC50 values were: 71.85, 73.95, and 63.01 mu g.mL-1, respectively. Additionally, nanoformulations significantly reduced N. fowleri-mediated host cell death, while nanoformulations along with fluconazole and metronidazole considerably reduced Balamuthia-mediated human cell damage. Finally, all the tested drugs and their nanoformulations revealed limited cytotoxic activity against human cerebral microvascular endothelial cell (HBEC-5i) cells. Conclusion These compounds should be developed into novel chemotherapeutic options for use against these distressing infections due to free-living amoebae, as currently there are no effective treatments.en_US
dc.description.sponsorshipUniversity of Sharjah [2101110144, 2101110149]en_US
dc.description.sponsorshipAcknowledgement The University of Sharjah provided funding for this project [grant number: 2101110144 & 2101110149].en_US
dc.identifier.doi10.1093/jambio/lxad072
dc.identifier.issn1364-5072
dc.identifier.issn1365-2672
dc.identifier.issue4en_US
dc.identifier.pmid37024269en_US
dc.identifier.scopus2-s2.0-85153983470en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org10.1093/jambio/lxad072
dc.identifier.urihttps://hdl.handle.net/20.500.12713/5395
dc.identifier.volume134en_US
dc.identifier.wosWOS:000977090000002en_US
dc.identifier.wosqualityN/Aen_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherOxford Univ Pressen_US
dc.relation.ispartofJournal of Applied Microbiologyen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.snmz20240519_kaen_US
dc.subjectNaegleria Fowlerien_US
dc.subjectBalamuthia Mandrillarisen_US
dc.subjectFree-Living Amoebaeen_US
dc.subjectNanotechnologyen_US
dc.subjectCytotoxicityen_US
dc.subjectCns Pathogensen_US
dc.titleAzole and 5-nitroimidazole based nanoformulations are potential antiamoebic drug candidates against brain-eating amoebaeen_US
dc.typeArticleen_US

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