Citrus Flavanones as Anti-Breast Cancer Agents: A Review and in Silico Study Targeting Aromatase

Area of Science:

• Biochemistry
• Pharmacology
• Oncology

Background:

• Breast cancer is a prevalent malignancy, often estrogen-dependent, making aromatase a key therapeutic target.
• Aromatase inhibitors are crucial in breast cancer treatment, but drug resistance necessitates novel therapeutic strategies.
• Flavonoids, particularly flavanones from citrus fruits, possess aromatase-inhibitory properties.

Purpose of the Study:

• To review aromatase function, its role in breast cancer, current inhibitors, and resistance mechanisms.
• To explore flavonoids, focusing on flavanones from citrus fruits and their anti-aromatase activity.
• To evaluate citrus flavanones' interaction with aromatase using molecular docking and virtual pharmacokinetic analyses.

Main Methods:

• Literature review on aromatase, breast cancer, inhibitors, and flavonoids.
• Analysis of citrus fruit flavanone composition and anti-aromatase activity.
• In silico molecular docking and virtual pharmacokinetic (ADME) evaluations of citrus flavanones against aromatase.

Main Results:

• Flavanones exhibit significant aromatase inhibition, with citrus fruits being a rich source.
• In silico analysis indicated strong binding affinities between certain citrus flavanones and aromatase.
• Pinocembrin, a flavanone aglycone, showed potential as an anti-aromatase agent based on docking and pharmacokinetic predictions.

Conclusions:

• Citrus flavanones represent a promising class of natural compounds for breast cancer therapy.
• Pinocembrin warrants further research for its potential as a novel aromatase inhibitor.
• In silico methods can effectively screen natural compounds for therapeutic potential against aromatase.