M. Paubertbraquet et al., EFFECT OF PYGEUM-AFRICANUM EXTRACT ON A23187-STIMULATED PRODUCTION OFLIPOXYGENASE METABOLITES FROM HUMAN POLYMORPHONUCLEAR CELLS, Journal of lipid mediators and cell signalling, 9(3), 1994, pp. 285-290
Pygeum africanum extract has been used for more than 20 years in Franc
e in patients suffering from benign prostatic hypertrophy (BPH). The e
xtract displays anti-inflammatory activity and inhibits bladder hyperr
eactivity during the above conditions. However, the mechanism of actio
n of P. africanum extract has never been clearly resolved. It has been
recently demonstrated that infiltration by inflammatory cells may be
involved in the development of BPH. Certain of these cell types, such
as macrophages, are known to produce chemotactic mediators including l
eukotrienes, and thus may contribute to the development of the disease
. In order to investigate the potential effect of P. africanum extract
on arachidonate metabolism, we examined its effect in vitro on leukot
riene (LT) synthesis in human polymorphonuclear cells stimulated with
the calcium ionophore A23187. Two formulations of the extract were tes
ted, one dissolved in DMSO and one aqueous solution obtained after alk
alinization (0.1 N; NaOH/acidification (0.1 N; HCl). Neither formulati
on had any effect on cell viability which was above 95% in both cases.
P. africanum extract dissolved in DMSO significantly inhibited the pr
oduction of 5-lipoxygenase metabolites (5-HETE, 20-COOH LTB4, LTB4 and
20-OH LTB(4)) at concentrations as low as 3 mu g/ml (p < 0.01), while
the same extract dissolved in NaOH/HCl only exhibited an inhibitory e
ffect at 10 mu g/ml (p < 0.01). This difference apparently reflects th
e greater solubility of the active components in the extract in DMSO.
The ability of P. africanum to antagonize 5-lipoxygenase metabolite pr
oduction may contribute, at least in part, to its therapeutic activity
in inflammatory component of BPH.