Correlation between in vitro cyclic adenosine monophosphate phosphodiesterase inhibition and in vivo anti-inflammatory effect

We tested the hypothesis that topical adenosine monophosphate phosphodieste rase (cAMP PDE) inhibitors are anti-inflammatory, These can be shown by a c orrelation between PDE inhibitory and anti-inflammatory function of a serie s of known PDE inhibitors, The effect of various cAMP PDE inhibitors on PDE s isolated from HaCaT cells was first investigated. These compounds were th en tested as anti-irritants against topical 8% Balsam of Peru, A direct cor relation was observed between the in vitro EC50 values for PDE inhibition a nd the in vivo anti-inflammatory potential with a correlation coefficient o f r = 0.79. These results stress the value of PDE inhibitors as anti-inflam matory agents in topical use, and also demonstrate that the in vitro PDE as say can be used to predict in vivo anti-inflammatory potential. Copyright ( C) 2000 S. Karger AG, Basel.