Endocrine Abstracts

Anthocyanidins are aglycons of anthocyanins, which are plant pigments responsible for floral and fruits color. Anthocyanidins possess beneficial pharmacological properties such as antioxidant, anti-inflammatory, anti-tumor and anti-diabetic. Anthocyanidins are contained in normal diet and might play role in food-drug interactions.

The aim of current study was to evaluate the effects of cyanidin, delphinidin, malvidin, pelargonidin and peonidin on the transcriptional activities of steroid and nuclear receptors.

The activities of glucocorticoid receptor (GR), androgen receptor (AR), estrogen receptor (ER), progesterone receptor (PR), thyroid receptor (TR), vitamin D receptor (VDR), pregnane X receptor (PXR), retinoic acid receptor (RAR) and retinoid X receptor (RXR) were assessed using either stably or transiently transfected luciferase gene reporter cell lines. The cytotoxicity assays and gene reporter assays were performed after the 24-h treatment of cells with increasing range of concentrations (10 nM – 50 μM) of tested anthocyanidins.

We found that some anthocyanidins in 50 μM concentration inhibited transcriptional activity of examined receptors. The inhibition down-to 49.4% for malvidin vs VDR, 49.3% for delphinidin vs RXR, 38.0% for malvidin vs RAR and 52.2% for pelargonidin vs PXR of maximal induction was observed.

Generally, certain tested anthocyanidins in the highest concentration inhibited transcriptional activity of studied receptors and none of the tested anthocyanidins in given concentration range caused significant induction of transcriptional activity of examined receptors.