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

Debelec-Butuner, Bilge; Ozturk, Mert Burak; Tag, Ozgur; Akgun, Ismail Hakki; Yetik-Anacak, Gunay; Bedir, Erdal; Korkmaz, Kemal Sami


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  <identifier identifierType="URL">https://aperta.ulakbim.gov.tr/record/33299</identifier>
  <creators>
    <creator>
      <creatorName>Debelec-Butuner, Bilge</creatorName>
      <givenName>Bilge</givenName>
      <familyName>Debelec-Butuner</familyName>
      <affiliation>Ege Univ, Fac Pharm, Dept Pharmaceut Biotechnol, Izmir, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Ozturk, Mert Burak</creatorName>
      <givenName>Mert Burak</givenName>
      <familyName>Ozturk</familyName>
    </creator>
    <creator>
      <creatorName>Tag, Ozgur</creatorName>
      <givenName>Ozgur</givenName>
      <familyName>Tag</familyName>
      <affiliation>Ege Univ, Grad Sch Nat &amp; Appl Sci, Dept Chem, Izmir, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Akgun, Ismail Hakki</creatorName>
      <givenName>Ismail Hakki</givenName>
      <familyName>Akgun</familyName>
      <affiliation>Ege Univ, Fac Engn, Dept Bioengn, Izmir, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Yetik-Anacak, Gunay</creatorName>
      <givenName>Gunay</givenName>
      <familyName>Yetik-Anacak</familyName>
      <affiliation>Ege Univ, Fac Pharm, Dept Pharmacol, Izmir, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Bedir, Erdal</creatorName>
      <givenName>Erdal</givenName>
      <familyName>Bedir</familyName>
    </creator>
    <creator>
      <creatorName>Korkmaz, Kemal Sami</creatorName>
      <givenName>Kemal Sami</givenName>
      <familyName>Korkmaz</familyName>
      <affiliation>Ege Univ, Fac Engn, Dept Bioengn, Canc Biol Lab, Izmir, Turkey</affiliation>
    </creator>
  </creators>
  <titles>
    <title>Cycloartane-Type Sapogenol Derivatives Inhibit Nf Kappa B Activation As Chemopreventive Strategy For Inflammation-Induced Prostate Carcinogenesis</title>
  </titles>
  <publisher>Aperta</publisher>
  <publicationYear>2018</publicationYear>
  <dates>
    <date dateType="Issued">2018-01-01</date>
  </dates>
  <resourceType resourceTypeGeneral="Text">Journal article</resourceType>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://aperta.ulakbim.gov.tr/record/33299</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsIdenticalTo">10.1016/j.steroids.2018.04.005</relatedIdentifier>
  </relatedIdentifiers>
  <rightsList>
    <rights rightsURI="http://www.opendefinition.org/licenses/cc-by">Creative Commons Attribution</rights>
    <rights rightsURI="info:eu-repo/semantics/openAccess">Open Access</rights>
  </rightsList>
  <descriptions>
    <description descriptionType="Abstract">Chronic 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 kappa 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 kappa B signaling leading the repression of NF kappa 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 kappa B signaling pathway.</description>
  </descriptions>
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