Effects of icariin on cGMP-specific PDE5 and cAMP-specific PDE4 activities

Asian J Androl. 2003 Mar;5(1):15-8.

Abstract

Aim: To clarify the mechanism of the therapeutic action of icariin on erectile dysfunction (ED).

Methods: PDE5 was isolated from the human platelet and PDE4 from the rat liver tissue using the FPLC system (Pharmacia, Milton Keynes, UK) and the Mono Q column. The inhibitory effects of icariin on PDE5 and PDE4 activities were investigated by the two-step radioisotope procedure with [(3)H]-cGMP/[(3)H]-cAMP. Papaverine served as the control drug.

Results: Icariin and papaverine showed dose-dependent inhibitory effects on PDE5 and PDE4 activities. The IC(50) of Icariin and papaverine on PDE5 were 0.432 micromol/L and 0.680 micromol/L, respectively and those on PDE4, 73.50 micromol/L and 3.07 micromol/L, respectively. The potencies of selectivity of icariin and papaverine on PDE5 (PDE4/PDE5 of IC(50)) were 167.67 times and 4.54 times, respectively.

Conclusion: Icariin is a cGMP-specific PDE5 inhibitor that may be developed into an oral effective agent for the treatment of ED.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3',5'-Cyclic-AMP Phosphodiesterases / antagonists & inhibitors
  • 3',5'-Cyclic-AMP Phosphodiesterases / metabolism
  • 3',5'-Cyclic-GMP Phosphodiesterases / antagonists & inhibitors
  • 3',5'-Cyclic-GMP Phosphodiesterases / metabolism*
  • Animals
  • Cyclic AMP / metabolism
  • Cyclic GMP / metabolism
  • Cyclic Nucleotide Phosphodiesterases, Type 4
  • Cyclic Nucleotide Phosphodiesterases, Type 5
  • Dose-Response Relationship, Drug
  • Drugs, Chinese Herbal / pharmacology*
  • Flavonoids / pharmacology*
  • Humans
  • In Vitro Techniques
  • Male
  • Papaverine / pharmacology
  • Penile Erection / drug effects*
  • Penile Erection / physiology
  • Phosphodiesterase Inhibitors / pharmacology
  • Rats
  • Tritium

Substances

  • Drugs, Chinese Herbal
  • Flavonoids
  • Phosphodiesterase Inhibitors
  • Tritium
  • Papaverine
  • Cyclic AMP
  • 3',5'-Cyclic-AMP Phosphodiesterases
  • Cyclic Nucleotide Phosphodiesterases, Type 4
  • 3',5'-Cyclic-GMP Phosphodiesterases
  • Cyclic Nucleotide Phosphodiesterases, Type 5
  • PDE5A protein, human
  • Pde5a protein, rat
  • Cyclic GMP
  • icariin