Aromatase (CYP19) inhibition by biflavonoids obtained from the branches of Garcinia gardneriana (Clusiaceae)
-
Angelica Maria Recalde-Gil
,
Juliana Salton
Abstract
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.
Acknowledgments
This work was supported by The National Council for Scientific and Technological Development (CNPq) and Fundação de Amparo à Pesquisa do Estado do Rio Grande do Sul (FAPERGS), Brazil. LCKJ, JS, VCF and ATH thank CNPq for the fellowships.
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Articles in the same Issue
- Frontmatter
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- The chemistry of social insects
- The critical role of primer pheromones in maintaining insect sociality
- Sexual attraction: a review of bumblebee male pheromones
- (3R,6E)-nerolidol, a fertility-related volatile secreted by the queens of higher termites (Termitidae: Syntermitinae)
- Regular Articles
- Evaluation of anti-adipogenic active homoisoflavonoids from Portulaca oleracea
- Structure elucidation and antimicrobial activities of five compounds from Artemisia integrifolia L
- Aromatase (CYP19) inhibition by biflavonoids obtained from the branches of Garcinia gardneriana (Clusiaceae)
Articles in the same Issue
- Frontmatter
- Special Section Articles
- The chemistry of social insects
- The critical role of primer pheromones in maintaining insect sociality
- Sexual attraction: a review of bumblebee male pheromones
- (3R,6E)-nerolidol, a fertility-related volatile secreted by the queens of higher termites (Termitidae: Syntermitinae)
- Regular Articles
- Evaluation of anti-adipogenic active homoisoflavonoids from Portulaca oleracea
- Structure elucidation and antimicrobial activities of five compounds from Artemisia integrifolia L
- Aromatase (CYP19) inhibition by biflavonoids obtained from the branches of Garcinia gardneriana (Clusiaceae)
