Phenylephrine Enhances the Mitogenic Effect of S-Allyl-L-cysteine on Primary Cultured Hepatocytes through Protein Kinase C-Induced B-Raf Phosphorylation

Biol Pharm Bull. 2024;47(9):1565-1574. doi: 10.1248/bpb.b24-00157.

Abstract

The co-mitogenic effects of the α1-adrenoceptor agonist phenylephrine on S-allyl-L-cysteine (SAC)-induced hepatocyte proliferation were examined in primary cultures of adult rat hepatocytes. The combination of phenylephrine (10-10-10-6 M) and SAC (10-6 M) exhibited a significant dose-dependent increase in the number of hepatocyte nuclei and viable cells compared to SAC alone. This combination also increased the progression of hepatocyte nuclei into the S-phase. The potentiating effect of phenylephrine on SAC-induced cell proliferation was counteracted by prazosin (an α1-adrenergic receptor antagonist) and GF109203X (selective protein kinase C (PKC) inhibitor). In addition, PMA (direct PKC activator) potentiated the proliferative effects of SAC similarly to phenylephrine. In essence, these findings suggest that PKC activity plays a crucial role in enhancing SAC-induced cell proliferation. Moreover, the effects of phenylephrine on SAC-induced Ras activity, Raf phosphorylation, and extracellular signal-regulated kinase 2 (ERK2) phosphorylation were investigated. Phenylephrine (or PMA) in combination with SAC did not augment Ras activity, but further increased ERK2 phosphorylation and its upstream B-Raf phosphorylation. These results indicate that PKC activation, triggered by stimulating adrenergic α1 receptors, further amplifies SAC-induced cell proliferation through enhanced ERK2 phosphorylation via increased B-Raf-specific phosphorylation in primary cultured hepatocytes.

Keywords: B-Raf; S-allyl-L-cysteine (SAC); cell proliferation; cross-talk; protein kinase C (PKC); α1-adrenergic agonist.

MeSH terms

  • Adrenergic alpha-1 Receptor Agonists* / pharmacology
  • Adrenergic alpha-1 Receptor Antagonists / pharmacology
  • Animals
  • Cell Proliferation* / drug effects
  • Cells, Cultured
  • Cysteine* / analogs & derivatives
  • Cysteine* / pharmacology
  • Drug Synergism
  • Hepatocytes* / drug effects
  • Hepatocytes* / metabolism
  • Indoles / pharmacology
  • Male
  • Maleimides / pharmacology
  • Mitogen-Activated Protein Kinase 1 / metabolism
  • Mitogens / pharmacology
  • Phenylephrine* / pharmacology
  • Phosphorylation / drug effects
  • Prazosin / pharmacology
  • Protein Kinase C* / metabolism
  • Proto-Oncogene Proteins B-raf* / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Tetradecanoylphorbol Acetate / analogs & derivatives
  • Tetradecanoylphorbol Acetate / pharmacology

Substances

  • Phenylephrine
  • Protein Kinase C
  • Cysteine
  • Adrenergic alpha-1 Receptor Agonists
  • S-allylcysteine
  • Proto-Oncogene Proteins B-raf
  • Prazosin
  • Tetradecanoylphorbol Acetate
  • Mitogen-Activated Protein Kinase 1
  • Maleimides
  • Indoles
  • Adrenergic alpha-1 Receptor Antagonists
  • bisindolylmaleimide I
  • Mitogens