Cycloartane-type sapogenol derivatives inhibit NF?B activation as chemopreventive strategy for inflammation-induced prostate carcinogenesis

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dc.contributor.authorDebeleç-Bütüner B.
dc.contributor.authorÖztürk M.B.
dc.contributor.authorTağ Ö.
dc.contributor.authorAkgün İ.H.
dc.contributor.authorYetik-Anacak G.
dc.contributor.authorBedir E.
dc.contributor.authorKorkmaz K.S.
dc.date.accessioned2019-10-27T08:02:01Z
dc.date.available2019-10-27T08:02:01Z
dc.date.issued2018
dc.departmentEge Üniversitesien_US
dc.description.abstractChronic inflammation is associated to 25% of cancer cases according to epidemiological data. Therefore, inhibition of inflammation-induced carcinogenesis can be an efficient therapeutic approach for cancer chemoprevention in drug development studies. It is also determined that anti-inflammatory drugs reduce cancer incidence. Cell culture-based in vitro screening methods are used as a fast and efficient method to investigate the biological activities of the biomolecules. In addition, saponins are molecules that are isolated from natural sources and are known to have potential for tumor inhibition. Studies on the preparation of analogues of cycloartane-type sapogenols (9,19-cyclolanostanes) have so far been limited. Therefore we have decided to direct our efforts toward the exploration of new anti-tumor agents prepared from cycloastragenol and its production artifact astragenol. The semi-synthetic derivatives were prepared mainly by oxidation, condensation, alkylation, acylation, and elimination reactions. After preliminary studies, five sapogenol analogues, two of which were new compounds (2 and 3), were selected and screened for their inhibitory activity on cell viability and NF?B signaling pathway activity in LNCaP prostate cancer cells. We found that the astragenol derivatives 1 and 2 as well as cycloastragenol derivatives 3, 4, and 5 exhibited strong inhibitory activity on NF?B signaling leading the repression of NF?B transcriptional activation and suppressed cell proliferation. The results suggested that these molecules might have significant potential for chemoprevention of prostate carcinogenesis induced by inflammatory NF?B signaling pathway. © 2018 Elsevier Inc.en_US
dc.description.sponsorship113Z078en_US
dc.description.sponsorshipThis work was supported by Turkish Scientific and Technological Research Council (TUBITAK) with the project number 113Z078 to BDB. Appendix A --en_US
dc.identifier.doi10.1016/j.steroids.2018.04.005en_US
dc.identifier.endpage20en_US
dc.identifier.issn0039-128X
dc.identifier.pmid29678446en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.startpage9en_US
dc.identifier.urihttps://doi.org/10.1016/j.steroids.2018.04.005
dc.identifier.urihttps://hdl.handle.net/11454/25109
dc.identifier.volume135en_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherElsevier Inc.en_US
dc.relation.ispartofSteroidsen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectAstragenolen_US
dc.subjectCycloastragenolen_US
dc.subjectInflammation-induced carcinogenesisen_US
dc.subjectNF?Ben_US
dc.subjectProstate cancer chemopreventionen_US
dc.subjectSemi-synthesisen_US
dc.titleCycloartane-type sapogenol derivatives inhibit NF?B activation as chemopreventive strategy for inflammation-induced prostate carcinogenesisen_US
dc.typeArticleen_US

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