The role of ceranib-2 and its nanoform on the decrease of telomerase levels in human non-small cell cancer

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dc.authoridIZGORDU, Dr. Huseyin/0000-0002-1377-2988
dc.authoridBAYRAKDAR, Alpaslan/0000-0001-7967-2245
dc.authoridCENGIZ, Mustafa/0000-0002-6925-8371
dc.contributor.authorCengiz, Mustafa
dc.contributor.authorSezer, Canan Vejselova
dc.contributor.authorGur, Bahri
dc.contributor.authorBayrakdar, Alpaslan
dc.contributor.authorIzgordu, Hueseyin
dc.contributor.authorAlanyali, Filiz
dc.contributor.authorOzic, Cem
dc.date.accessioned2024-12-24T19:24:42Z
dc.date.available2024-12-24T19:24:42Z
dc.date.issued2024
dc.departmentSiirt Üniversitesi
dc.description.abstractBackgroundCeranib-2, an acid ceramidase (AC) inhibitor, can inhibit cancer cell proliferation and tumor development. However, poor water solubility and low cellular bioavailability limit its efficacy in cancer treatment.Methods and resultsThis study aimed to investigate the cell death induced by ceranib-2 and its solid lipid nanoformulation (ceranib-2-SLN) produced by the hot homogenization technique and the synergistic relationship between ceramide and telomerase in vitro and in silico. Furthermore, this study proved the possible mechanism of ceranib-2-induced AC inhibition by in silico studies. The effective cytotoxic concentrations of ceranib-2, telomerase level, and changes in ceramide levels were measured by MTT colorimetric cytotoxicity assay, ELISA, and LC/MS/MS methods, respectively. TEM results showed that ceranib-2-SLN was 13-fold smaller than the size of ceranib-2. Ceranib-2 and ceranib-2-SLN had IC50 concentrations of 31.62 (+/- 2.1) and 27.69 (+/- 1.75) mu M in A549, and 48.79 (+/- 1.56) and 67.98 (+/- 2.33) in Beas-2B cells. These compounds simultaneously increased ceramide levels and decreased telomerase levels in A549 cells. Ceranib-2 increased telomerase levels while decreasing ceramide levels in Beas-2B cells. It was shown how the synergistic impact of ceranib-2-induced ceramide production and ceramide-induced telomerase level reduction on cytotoxicity in A549 cells.ConclusionsCeranib-2-SLN was discovered to be more cytotoxic on cancer cells than ceranib-2, suggesting that it could be a promising option for the development of a new anti-cancer agent.
dc.description.sponsorshipEskisehir Technical University Scientific Research Project Coordination Unit [21GAP109, 21GAP112]
dc.description.sponsorshipThis study was financially supported by Eskisehir Technical University Scientific Research Project Coordination Unit with the projects numbered 21GAP109 and 21GAP112.
dc.identifier.doi10.1007/s11033-024-09838-2
dc.identifier.issn0301-4851
dc.identifier.issn1573-4978
dc.identifier.issue1
dc.identifier.pmid39105852
dc.identifier.scopus2-s2.0-85200508752
dc.identifier.scopusqualityQ2
dc.identifier.urihttps://doi.org/10.1007/s11033-024-09838-2
dc.identifier.urihttps://hdl.handle.net/20.500.12604/6105
dc.identifier.volume51
dc.identifier.wosWOS:001285298000001
dc.identifier.wosqualityN/A
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherSpringer
dc.relation.ispartofMolecular Biology Reports
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.snmzKA_20241222
dc.subjectAcid ceramidase inhibition
dc.subjectCeramide
dc.subjectCytotoxicity
dc.subjectin silico
dc.subjectTelomerase
dc.titleThe role of ceranib-2 and its nanoform on the decrease of telomerase levels in human non-small cell cancer
dc.typeArticle

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