Positive Health Online

Abstract

ALBERT and colleagues, Institute of Pharmaceutical Chemistry, University of Frankfurt, D-60439 Frankfurt, Germany, found that hyperforin is a dual inhibitor of cyclo-oxygenase 1 and 5-lipoxygenase.

Background

5-lipoxygenase (5-LO) and cyclo-oxyghenase (COX) are key enzymes in the formation of pro-inflammatory eicosanoids. The aim of this study was to determine if the main fat-soluble component of St John’s Wort (Hypericum perforatum), hyperforin, can suppress the activity of these enzymes.

Methodology

The activities of 5-LO and COX were measured in freshly isolated human polymorphonuclear leukocytes stimulated with the calcium-ionophore A23187.

Results

Hyperforin inhibited the activity of 5-LO with IC(50) values of about 1-2 micromolar. It also inhibited isolated 5-LO. The effective doses are comparable to the well-known 5-LO inhibitor zileuton (IC(50) = 0.5-1 micromolar). Hyperforin also suppressed the activity of COX-1 with an IC(50) of about 90 nanomolar or 3 to 18 times more efficiently than aspirin. Hyperforin had no effect on COX-2, 12-LO or 15-LO.

Conclusion

Hyperforin acts as a dual inhibitor of 5-LO and COX-1, suggesting therapeutic potential of St John’s Wort in inflammatory and allergic diseases connected to eicosanoids.

References

Albert D, Zuendorf I, Dingermann T, Mueller WE, Steinhilber D, Werz O. Hyperforin is a dual inhibitor of cyclooxygenase-1 and 5-lipoxygenase. Biochemical Pharmacology 64 (12): 1767-1775, Dec 15, 2002.