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

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.

• Authors: Z C Xin, E K Kim, C S Lin, W J Liu, L Tian, Y M Yuan, J Fu
• Journal: Asian journal of andrology (Asian J Androl) Vol. 5 Issue 1 Pg. 15-8 (Mar 2003) ISSN: 1008-682X [Print] China
• PMID: 12646997 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 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

Topics

• 3',5'-Cyclic-AMP Phosphodiesterases (antagonists & inhibitors, metabolism)
• 3',5'-Cyclic-GMP Phosphodiesterases (antagonists & inhibitors, 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, physiology)
• Phosphodiesterase Inhibitors (pharmacology)
• Rats
• Tritium