26-01-2016, 08:58 PM
Have you seen this study?
Androgen Modulators from the Roots of Paeonia lactiflora (Paeoniae
Radix) Grown and Processed in Nara Prefecture, Japan
Kazuto W ASHIDA ,* , a Yoshiyuki I TOH , b Takashi I WASHITA , b and Kyosuke N OMOTO a
https://www.jstage.jst.go.jp/article/cpb...9_971/_pdf
Androgen Modulators from the Roots of Paeonia lactiflora (Paeoniae
Radix) Grown and Processed in Nara Prefecture, Japan
Kazuto W ASHIDA ,* , a Yoshiyuki I TOH , b Takashi I WASHITA , b and Kyosuke N OMOTO a
https://www.jstage.jst.go.jp/article/cpb...9_971/_pdf
Quote:We have thus isolated the first hormone modulators from
the roots of P. lactiflora. This is the first report of paeoni-
florin and albiflorin derivatives such as 1, 2, 4 and 5 showing
AR binding activity. Interestingly, compounds 6 and 7
showed no AR binding activity. The AR binding activity of
6-O-galloylalbiflorin (2) was much stronger than that of the
galloylpaeoniflorin derivatives (1, 5). These results suggested
that both the structure of albiflorin and the galloyl moiety
were important for 2 to show strong AR binding activity. Ad-
ditionally, 6-O-galloylpaeoniflorin (5) displayed the weakest
AR binding activity of the paeoniflorin derivatives (1, 4, 5).
The only structural differences between 2 and 5 are at C-4
and C-9, so the galloyl moiety of 2 might interact with the
carbonyl group of C-9 and/or the hydroxyl group of C-4.
It has been reported that 3 can inhibit growth of prostate
cancer LNCaP cells by two aspects including inhibition of 5-
a -reductase activity and expression of AR protein levels;
however, the AR binding activity of 3 has not been re-
ported. 12) We propose that 3 inhibits prostate cancer cell
growth partly by acting as an AR antagonist.
The AR binding activity of compound 3 was equivalent to
flutamide (IC 50 5.0 m M ), 13) which is in clinical use, and the
activity of compound 2 was also relatively strong. Additon-
ally, because Paeoniae radix was taken in long time as a
crude drug, compounds 2 and 3 might be candidates as safe,
natural AR antagonists.