Galloylalbiflorin

Galloylalbiflorin (6′-O-Galloylalbiflorin) is an androgen receptor (AR) antagonist isolated from the roots of Paeonia lactiflora and exhibits an IC50 value of 53.3 μM. Galloylalbiflorin (6′-O-Galloylalbiflorin) has been reported to possess anti-androgen activity. The androgen receptor antagonistic activity of Galloylalbiflorin (6′-O-Galloylalbiflorin) supports the application of Galloylalbiflorin (6′-O-Galloylalbiflorin) in research investigating androgen receptor signaling, hormone-responsive cellular pathways, and androgen-dependent disease mechanisms.

Method: Rat androgen receptor membrane preparations were incubated with 1.5 nM [³H]-mibolerone and 6′-O-galloylalbiflorin at concentrations of 3.8–60 μg/mL for 4 h at 4°C. Receptor-bound radioligand was isolated using hydroxyapatite and quantified to evaluate androgen receptor binding activity.
Rresult: 6′-O-Galloylalbiflorin inhibited [³H]-mibolerone binding to the androgen receptor in a concentration-dependent manner, with an IC50 of 33.7 μg/mL (53.3 μM).[1]
Method: Androgen-responsive LNCaP-FGC human prostate cancer cells were preincubated for 24 h and subsequently treated with 6′-O-galloylalbiflorin at concentrations of 20–100 μg/mL for 72 h. Cell growth was assessed using the alamarBlue assay after an additional 6 h of incubation.
Rresult: 6′-O-Galloylalbiflorin inhibited LNCaP-FGC cell growth in a concentration-dependent manner, with an IC50 of 58.0 μg/mL (91.8 μM). Together with its androgen receptor-binding activity, the result indicated that it acted as an androgen receptor antagonist.[1]