Src kinase inhibitory activity of black chokeberry and bilberry fruits

Edible berries such as the fruits of black chokeberry (Aronia melanocarpa (Michx.) Elliott.) and bilberry (Vaccinium myrtillus L.) are considered to be rich in polyphenols, which are nowadays attracting great interest due to their promising health benefits. The aim of our study was to investigate their inhibitory properties on Src kinase activity, as this enzyme plays an important role in multiple cellular processes and is activated in both cancer and inflammatory cells. In the hydroethanolic fruit extracts, 5.0 – 5.9% of total polyphenols were determined spectrophotometrically, including high amounts of hydroxycinnamic acid derivatives. HPLC analysis revealed that the black chokeberry and bilberry extracts contained 2.05 mg/g and

2.54 mg/g of chlorogenic acid, respectively. Using a time-resolved fluorescence resonance energy transfer (TR-FRET) assay, the extracts studied were found to have comparable inhibitory effects on Src kinase, with IC₅₀ values of 366 µg/mL and 369 µg/mL, respectively. The results also indicated that chlorogenic acid contributes significantly to the observed effect (IC₅₀ 122 µg/mL). In addition, both fruit extracts exhibited antioxidant activity by scavenging NO radicals with IC₅₀ values of 158 µg/mL (black chokeberry) and 352 µg/mL (bilberry). Our study demonstrated, for the first time, that black chokeberry and bilberry fruits are able to affect Src kinase activity, which could be beneficial in the prevention of cancer and inflammation- related diseases.

 

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Publication History

Article published online:
16 November 2023