Recently, much attention has focused on the treatment of BPH with the
pollen extract, Cernilton. The present investigation was designed to i
dentify the active component in this agent which might be responsible
for the symptomatic relief of BPH as previously reported [1,2]. Sequen
tial purification of the active component present in the pollen extrac
t was carried out by a combination of dialysis, gel filtration, and re
verse phase chromatography. To monitor the biological activity of each
of the purified fractions, a biological assay employing the human pro
state cancer cell line DU145 was undertaken. While we have identified
a number of constituent components in the pollen extract, only one fra
ction designated V-7 (FV-7) maintained a strong inhibitory effect on t
he growth of DU145 cells. The inhibition was time- and dose-dependent,
and the concentrations of FV-7 required to reduce the cell numbers by
50% (IC50) after 2 days of exposure was 5 mu g/ml. FV-7 was also inhi
bitory towards the primary culture of prostate stroma and epithelial c
ells, with the stroma/fibroblast showing greater sensitivity towards t
he HPLC-purified component. However, it should be noted that this inhi
bitory activity measured in the primary culture cells was only achieve
d at higher concentrations of FV-7. Preliminary characterization of th
e active ingredient identified FV-7 as DIBOA which is a cyclic hydroxa
mic acid. FV-7 and DIBOA induce similar inhibitory effects on the grow
th of DU145 cells. (C) 1995 Wiley-Liss, Inc.