Aromatase (CYP19) inhibition by biflavonoids obtained from the branches of Garcinia gardneriana (Clusiaceae)
| Autor: | Valdir Cechinel-Filho, Amélia T. Henriques, Sérgio Augusto de Loreto Bordignon, Cristiane Matté, Angelica Maria Recalde-Gil, Juliana Salton, Luiz Carlos Klein-Júnior |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
chemistry.chemical_classification
Biflavonoids Postmenopausal women Garcinia gardneriana biology Aromatase Inhibitors Plant Extracts 010405 organic chemistry Clusiaceae Pharmacology biology.organism_classification 01 natural sciences General Biochemistry Genetics and Molecular Biology In vitro 0104 chemical sciences 03 medical and health sciences 0302 clinical medicine Enzyme chemistry 030220 oncology & carcinogenesis Sense (molecular biology) biology.protein Aromatase Garcinia |
| Zdroj: | Zeitschrift für Naturforschung C. 74:279-282 |
| ISSN: | 1865-7125 0939-5075 |
| Popis: | Overexpression of aromatase in breast cancer cells may substantially influence its progression and maintenance. In this sense, the inhibition of aromatase is a key target for the treatment of breast cancer in postmenopausal women. Although several flavonoids had already demonstrated the capacity of inhibiting aromatase activity, the role of biflavonoids as aromatase inhibitors is poorly studied. In this work, the biflavonoids isolated from Garcinia gardneriana, morelloflavone (1), Gb-2a (2) and Gb-2a-7-O-glucose (3) were submitted to in vitro assay to evaluate the aromatase modulatory effect. As results, it was demonstrated that all biflavonoids were able to inhibit the enzyme, with IC50 values ranging from 1.35 to 7.67 μM. This demonstrates that biflavonoids are an important source of scaffolds for the development of new aromatase inhibitors, focusing on the development of new anticancer agents. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|