1 Ocak 2022 Dergi makalesi Açık Erişim

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

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    "creators": [
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        "affiliation": "Izmir Katip Celebi Univ, Fac Pharm, Dept Pharmaceut Toxicol, Izmir, Turkey", 
        "name": "Erguc, Elif Ince"
      }, 
      {
        "affiliation": "Ege Univ, Fac Pharm, Dept Pharmaceut Toxicol, Izmir, Turkey", 
        "name": "Sezer, Senem Ozcan"
      }, 
      {
        "affiliation": "Ege Univ, Fac Pharm, Dept Pharmaceut Toxicol, Izmir, Turkey", 
        "name": "Orhan, Hande Gurer"
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    "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.", 
    "doi": "10.4274/tjps.galenos.2021.85530", 
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    "journal": {
      "issue": "6", 
      "pages": "626-629", 
      "title": "TURKISH JOURNAL OF PHARMACEUTICAL SCIENCES", 
      "volume": "19"
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    "publication_date": "2022-01-01", 
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    "title": "Advantages and Disadvantages of Two In Vitro Assays in Evaluating Aromatase Activity: \"A Cell-Based and a Cell-Free Assay\""
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