1 Ocak 2022 Dergi makalesi Açık Erişim

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

Citation Style Language JSON

{
  "DOI": "10.4274/tjps.galenos.2021.85530", 
  "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.", 
  "author": [
    {
      "family": "Erguc", 
      "given": " Elif Ince"
    }, 
    {
      "family": "Sezer", 
      "given": " Senem Ozcan"
    }, 
    {
      "family": "Orhan", 
      "given": " Hande Gurer"
    }
  ], 
  "container_title": "TURKISH JOURNAL OF PHARMACEUTICAL SCIENCES", 
  "id": "258893", 
  "issue": "6", 
  "issued": {
    "date-parts": [
      [
        2022, 
        1, 
        1
      ]
    ]
  }, 
  "page": "626-629", 
  "title": "Advantages and Disadvantages of Two In Vitro Assays in Evaluating Aromatase Activity: \"A Cell-Based and a Cell-Free Assay\"", 
  "type": "article-journal", 
  "volume": "19"
}