1 Ocak 2022 Dergi makalesi Açık Erişim

Erguc, Elif Ince; Sezer, Senem Ozcan; Orhan, Hande Gurer

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  <identifier identifierType="URL">https://aperta.ulakbim.gov.tr/record/258893</identifier>
  <creators>
    <creator>
      <creatorName>Erguc, Elif Ince</creatorName>
      <givenName>Elif Ince</givenName>
      <familyName>Erguc</familyName>
      <affiliation>Izmir Katip Celebi Univ, Fac Pharm, Dept Pharmaceut Toxicol, Izmir, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Sezer, Senem Ozcan</creatorName>
      <givenName>Senem Ozcan</givenName>
      <familyName>Sezer</familyName>
      <affiliation>Ege Univ, Fac Pharm, Dept Pharmaceut Toxicol, Izmir, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Orhan, Hande Gurer</creatorName>
      <givenName>Hande Gurer</givenName>
      <familyName>Orhan</familyName>
      <affiliation>Ege Univ, Fac Pharm, Dept Pharmaceut Toxicol, Izmir, Turkey</affiliation>
    </creator>
  </creators>
  <titles>
    <title>Advantages And Disadvantages Of Two In Vitro Assays In Evaluating Aromatase Activity: "A Cell-Based And A Cell-Free Assay"</title>
  </titles>
  <publisher>Aperta</publisher>
  <publicationYear>2022</publicationYear>
  <dates>
    <date dateType="Issued">2022-01-01</date>
  </dates>
  <resourceType resourceTypeGeneral="Text">Journal article</resourceType>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://aperta.ulakbim.gov.tr/record/258893</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsIdenticalTo">10.4274/tjps.galenos.2021.85530</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">Objectives: Aromatase is an enzyme that catalyzes the conversion of androgens to estrogens. While inhibition of aromatase is a useful approach for treating breast cancer, it may also have toxicological consequences due to its endocrine disrupting/modulating effect. In this study, sensitivity and performance of two in vitro assays-a cell free and a cell -based-for evaluating aromatase activity were investigated by testing known aromatase inhibitors and partial validation of the methods was performed. Advantages and disadvantages of these methods are also discussed.Materials and Methods: Aromatase activity was evaluated via two in vitro models; direct measurement with a cell-free assay using a fluorescent substrate and recombinant human enzyme and indirect evaluation with a cell-based assay where cell proliferation was determined in estrogen receptor positive human breast cancer cells (MCF-7 BUS) in the absence of estrogen and the presence of testosterone.Results: In the cell-free direct measurement assay, reference compounds ketoconazole and aminoglutethimide have been shown to inhibit the aromatase enzyme with half-maximal inhibitory concentration (IC50) values concordant with literature. In cell-based indirect measurement assay, only ketoconazole dose-dependently inhibited cell proliferation with 3.47 x 10-7 M IC50. Inter-assay and intra-assay reproducibility of both methods was found to be within acceptable deviation levels.Conclusion: Both methods can be successfully applied. However, to evaluate the potential aromatase activity of the novel compounds in vitro, it seems better to perform both the cell-based and the cell-free assays that allows low-moderate biotransformation and eliminate cytotoxicity potential, respectively.</description>
  </descriptions>
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