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Several factors can increase the risk of cancer in an individual. About 50% of cancer cases can be prevented by adopting a healthy lifestyle, regular exercise, eating healthy, and following a modest cancer prevention diet. Epidemiological studies have consistently shown that populations with vegetable and fruit-rich diets have reduced the incidence of cancer. On the other hand, populations who have a diet rich in animal fat, red meat, junk food, or high calories are predisposed to cancer.
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  5. Predictive And Prognostic Markers
  6. Evaluating Flavonoids As Potential Aromatase Inhibitors For Breast Cancer Treatment: In Vitro Studies And In Silico Predictions

Evaluating flavonoids as potential aromatase inhibitors for breast cancer treatment: In vitro studies and in silico predictions

Jeong In Seo1, Jun Sang Yu1, Yonghui Zhang2

  • 1Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Republic of Korea.

Chemico-Biological Interactions
|February 25, 2024

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View abstract on PubMed

Summary
This summary is machine-generated.

Flavonoids show potential as aromatase inhibitors for breast cancer treatment. Several flavonoids demonstrated significant inhibitory activity and favorable drug-like properties, suggesting their development as novel therapeutics.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Aromatase inhibitors are crucial for hormone-dependent breast cancer treatment.
  • Flavonoids offer a promising alternative to current therapies with fewer side effects.

Purpose of the Study:

  • To investigate the in vitro aromatase (CYP19A1) inhibitory potential of 14 different flavonoids.
  • To evaluate the drug-likeness and pharmacokinetic properties of active flavonoids using in silico methods.

Main Methods:

  • In vitro screening of 14 flavonoids for aromatase inhibition.
  • In silico analysis including molecular docking, SwissADME, admetSAR, and QED for drug-likeness prediction.

Main Results:

  • Six flavonoids (pinocembrin, eriodictyol, naringenin, liquiritigenin, sakuranetin, and chrysin) showed IC50 values below 10 μM.
Keywords:
AromataseBreast cancerFlavonoidsInhibitors

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  • These active flavonoids exhibited favorable physicochemical properties and ADME profiles.
  • Conclusions:

    • Pinocembrin, eriodictyol, naringenin, liquiritigenin, sakuranetin, and chrysin are promising candidates for novel flavonoid-based aromatase inhibitors.
    • This research provides valuable insights for developing new breast cancer treatments.