In Vitro Inhibition of Phosphodiesterase 3B (PDE 3B) by Anthocyanin-Rich Fruit Juice Extracts and Selected Anthocyanins

Int J Mol Sci. 2020 Sep 21;21(18):6934. doi: 10.3390/ijms21186934.

Abstract

Phosphodiesterases (PDEs) are essential enzymes for the regulation of pathways mediated by cyclic adenosine monophosphate (cAMP). Secondary plant compounds like anthocyanins (ACs) can inhibit PDE activity and, consequently, may be beneficial for lipid metabolism. This study investigated 18 AC-rich juice extracts and pure reference compounds from red fruits for potential inhibitory effects on PDE 3B activity. Extracts were obtained through adsorption on Amberlite® XAD 7 resin. Based on this screening, the chokeberry, blueberry, pomegranate, and cranberry extracts were active, with half maximal inhibitory concentrations (IC50) ranging from 163 ± 3 µg/mL to 180 ± 3 µg/mL. The ACs in these extracts, peonidin-3-glucoside and cyanidin-3-arabinoside, were the most active single compounds (IC50 = 56 ± 20 µg/mL, 108 ± 6 µg/mL). All extracts comprised high amounts of phenolic compounds, as determined by the Folin-Ciocalteu assay, ranging from 39.8 ± 1.5 to 73.5 ± 4.8 g gallic acid equivalents (GAE)/100 g extract. Pomegranate and chokeberry extracts exhibited the largest amounts of polyphenols (72.3 ± 0.7 g GAE/100 g, 70.6 ± 4.1 g GAE/100 g, respectively). Overall, our results showed that fruit juice extracts and their ACs can inhibit PDE activity. Any potential health benefits in vivo will be investigated in the future.

Keywords: Folin-Ciocalteu; HPLC-ESI-MSn; anthocyanins; cyclic adenosine monophosphate; inhibition; phosphodiesterase; red fruit juice.

MeSH terms

  • Anthocyanins* / chemistry
  • Anthocyanins* / pharmacology
  • Cyclic Nucleotide Phosphodiesterases, Type 3 / metabolism*
  • Fruit / chemistry*
  • Fruit and Vegetable Juices*
  • HT29 Cells
  • Humans
  • Phosphodiesterase 3 Inhibitors* / chemistry
  • Phosphodiesterase 3 Inhibitors* / pharmacology
  • Plant Extracts / chemistry*

Substances

  • Anthocyanins
  • Phosphodiesterase 3 Inhibitors
  • Plant Extracts
  • Cyclic Nucleotide Phosphodiesterases, Type 3
  • PDE3B protein, human