The weak immunosuppressant cyclosporine D as well as the immunologically inactive cyclosporine H are potent inhibitors in vivo of phorbol ester TPA-induced biological effects in mouse skin and of Ca2+/calmodulin dependent EF-2 phosphorylation in vitro

Biochem Biophys Res Commun. 1988 Jan 29;150(2):545-51. doi: 10.1016/0006-291x(88)90428-7.

Abstract

Various biological effects induced by the tumor promoting phorbol ester TPA in mouse skin are comparably suppressed by the immunologically inactive cyclosporine H (CsH) and by the strongly immunosuppressive cyclosporine A (CsA). These effects inhibited include the development of edema, stimulation of alkaline phosphatase activity, DNA and protein synthesis, as well as tumor promotion. Furthermore, CsH, like CsA, inhibits the Ca2+/calmodulin-dependent phosphorylation of the elongation factor 2 (EF-2) in vitro and the TPA-induced increases in the amount of EF-2 in vivo. Similar observations were made using the weak immunosuppressant CsD. We conclude from these results that the ability of cyclosporines to act as immunosuppressants and their ability to inhibit TPA-effects are based on two different mechanisms of action. Inhibition of TPA-effects may involve suppression of calmodulin-dependent processes, such as augmentation and phosphorylation of EF-2.

Publication types

  • Comparative Study

MeSH terms

  • Alkaline Phosphatase / metabolism
  • Animals
  • Cyclosporine*
  • Cyclosporins / pharmacology*
  • Cytosol / metabolism
  • DNA Replication / drug effects
  • Mice
  • Peptide Elongation Factor 2
  • Peptide Elongation Factors / metabolism*
  • Phosphorylation
  • Protein Biosynthesis
  • Protein Kinases / metabolism*
  • Skin / drug effects
  • Skin / metabolism*
  • Structure-Activity Relationship
  • Tetradecanoylphorbol Acetate / pharmacology*

Substances

  • Cyclosporins
  • Peptide Elongation Factor 2
  • Peptide Elongation Factors
  • Cyclosporine
  • cyclosporin D
  • Protein Kinases
  • Alkaline Phosphatase
  • cyclosporin H
  • Tetradecanoylphorbol Acetate