1 Ocak 2022 Dergi makalesi Açık Erişim

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

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  <dc:creator>Erguc, Elif Ince</dc:creator>
  <dc:creator>Sezer, Senem Ozcan</dc:creator>
  <dc:creator>Orhan, Hande Gurer</dc:creator>
  <dc:date>2022-01-01</dc:date>
  <dc:description>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.</dc:description>
  <dc:identifier>https://aperta.ulakbim.gov.trrecord/258893</dc:identifier>
  <dc:identifier>oai:aperta.ulakbim.gov.tr:258893</dc:identifier>
  <dc:rights>info:eu-repo/semantics/openAccess</dc:rights>
  <dc:rights>http://www.opendefinition.org/licenses/cc-by</dc:rights>
  <dc:source>TURKISH JOURNAL OF PHARMACEUTICAL SCIENCES 19(6) 626-629</dc:source>
  <dc:title>Advantages and Disadvantages of Two In Vitro Assays in Evaluating Aromatase Activity: "A Cell-Based and a Cell-Free Assay"</dc:title>
  <dc:type>info:eu-repo/semantics/article</dc:type>
  <dc:type>publication-article</dc:type>
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