Flavonoids as Prospective Aromatase Inhibitors in Breast Cancer Prevention/ Therapy

Curr Mol Pharmacol. 2021;14(6):1112-1124. doi: 10.2174/1874467214666210210123709.

Abstract

Flavonoids have been shown to target aromatase, suppressing the transformed cells' proliferation and growth. Such experimental data further promoted the usage of flavonoids as an aromatase inhibitor and helps prevent cancer, specifically breast and lung cancer. Conversely, flavonoids have certain limitations like low absorption, potency, and some side effects in addition to their tremendous advantages. The pharmacokinetics and toxicity of flavonoids are now being addressed by using advanced nanotechnological approaches. This review discusses the comprehensive aromatase signaling pathway in normal and cancer cells. It also draws attention to how do flavonoids modulate aromatase signaling pathways. Also, different flavonoid groups inhibiting aromatase activities are discussed and listed in the Table comprising flavonoids group, cancer type, clinical trials, IC50, and the assay employed. Moreover, nanoparticles-mediated improvement in the pharmacokinetics and toxicity issues of flavonoids in targeting aromatase are also deliberated. In conclusion, flavonoids act as a potential anticancer agent via targeting aromatase. Besides, nanotechnological approaches are useful in addressing the pharmacokinetics and toxicity of flavonoids.

Keywords: Aromatase; cancer.; flavonoids; medicinal and aromatic plants; nano-composites; nanotechnology.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • Antineoplastic Agents* / therapeutic use
  • Aromatase Inhibitors / pharmacology
  • Aromatase Inhibitors / therapeutic use
  • Breast Neoplasms* / drug therapy
  • Breast Neoplasms* / prevention & control
  • Female
  • Flavonoids / pharmacology
  • Flavonoids / therapeutic use
  • Humans
  • Prospective Studies

Substances

  • Antineoplastic Agents
  • Aromatase Inhibitors
  • Flavonoids