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Radiolabeling and in vitro evaluation of a new 5-fluorouracil derivative with cell culture studies

Ilem-Ozdemir, Derya; Atlihan-Gundogdu, Evren; Ekinci, Meliha; Halay, Erkan; Ay, Kadir; Karayildirim, Tamer; Asikoglu, Makbule


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  <identifier identifierType="URL">https://aperta.ulakbim.gov.tr/record/67797</identifier>
  <creators>
    <creator>
      <creatorName>Ilem-Ozdemir, Derya</creatorName>
      <givenName>Derya</givenName>
      <familyName>Ilem-Ozdemir</familyName>
      <affiliation>Ege Univ, Fac Pharm, Dept Radiopharm, Bornova, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Atlihan-Gundogdu, Evren</creatorName>
      <givenName>Evren</givenName>
      <familyName>Atlihan-Gundogdu</familyName>
      <affiliation>Ege Univ, Fac Pharm, Dept Radiopharm, Bornova, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Ekinci, Meliha</creatorName>
      <givenName>Meliha</givenName>
      <familyName>Ekinci</familyName>
      <affiliation>Ege Univ, Fac Pharm, Dept Radiopharm, Bornova, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Halay, Erkan</creatorName>
      <givenName>Erkan</givenName>
      <familyName>Halay</familyName>
      <affiliation>Usak Univ, Sci Anal &amp; Technol Applicat &amp; Res Ctr, Usak, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Ay, Kadir</creatorName>
      <givenName>Kadir</givenName>
      <familyName>Ay</familyName>
      <affiliation>Manisa Celal Bayar Univ, Fac Art &amp; Sci, Dept Chem, Manisa, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Karayildirim, Tamer</creatorName>
      <givenName>Tamer</givenName>
      <familyName>Karayildirim</familyName>
      <affiliation>Ege Univ, Fac Sci, Dept Chem, Bornova, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Asikoglu, Makbule</creatorName>
      <givenName>Makbule</givenName>
      <familyName>Asikoglu</familyName>
      <affiliation>Ege Univ, Fac Pharm, Dept Radiopharm, Bornova, Turkey</affiliation>
    </creator>
  </creators>
  <titles>
    <title>Radiolabeling And In Vitro Evaluation Of A New 5-Fluorouracil Derivative With Cell Culture Studies</title>
  </titles>
  <publisher>Aperta</publisher>
  <publicationYear>2019</publicationYear>
  <dates>
    <date dateType="Issued">2019-01-01</date>
  </dates>
  <resourceType resourceTypeGeneral="Text">Journal article</resourceType>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://aperta.ulakbim.gov.tr/record/67797</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsIdenticalTo">10.1002/jlcr.3804</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">The clinical impact and accessibility of Tc-99m tracers for cancer diagnosis would be greatly enhanced by the availability of a new, simple, and easy labeling process and radiopharmaceuticals. 5-Fluorouracil is an antitumor drug, which has played an important role for the treatment of breast carcinoma. In the present study, a new derivative of 5-Fluorouracil was synthesized as (1-[{1 '-(1 ''-deoxy-2 '',3 '':4 '',5 ''-di-O-isopropylidene-beta-D-fructopyranose-1 ''-yl)-1 ' H-1 ',2 ', 3 '-triazol-4 '-yl}methyl]-5-fluorouracil) (E) and radiolabeled with Tc-99m. It was analyzed by radio thin layer chromatography for quality control and stability. The radiolabeled complex was subjected to in vitro cell-binding studies to determine healthy and cancer cell affinity using HaCaT and MCF-7 cells, respectively. In addition, in vitro cytotoxicity studies of compound E were performed with HaCaT and MCF-5 cells. The radiochemical purity of the [Tc-99m]TcE was found to be higher than 90% at room temperature up to 6 hours. The radiolabeled complex showed higher specific binding to MCF-7 cells than HaCaT cells. IC50 values of E were found 31.5 +/- 3.4 mu M and 20.7 +/- 2.77 mu M for MCF-7 and HaCaT cells, respectively. The results demonstrated the potential of a new radiolabeled E with Tc-99m has selective for breast cancer cells.</description>
  </descriptions>
</resource>
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