Bioactive ergostanoids and a new polyhydroxyoctane from Lentinus polychrous mycelia and their inhibitory effects on E2-enhanced cell proliferation of T47D cells.

From mycelia of Lentinus polychrous, a Thai local edible mushroom cultured under solid-state fermentation, a new compound, 6-methylheptane-1,2,3,4,5-pentaol (1), and five ergostanoids, namely (22E,24R)-ergosta-7,22-dien-3β,5α,6β-triol (2), 3β,5α-dihydroxy-(22E,24R)-ergosta-7,22-dien-6-one (3), ergosta-4,6,8(14),22-tetraen-3-one (4), (3β,5α,8α,22E)-5,8-diepoxy-ergosta-6,22-dien-3-ol (5) and 5,8-epidioxy-(3β,5α,8α,22E)-ergosta-6,9(11),22-trien-3-ol (6), was isolated and characterised. The compounds were determined for their oestrogenic and anti-oestrogenic activities by using human breast cancer T47D cells. All compounds had no oestrogenic activity but exhibited suppressive effect on oestradiol-enhanced cell proliferation. Among these compounds, only 4 significantly competed with oestradiol in the binding to oestrogen receptors (ERs) with higher selectivity to ERα than ERβ. These results may suggest that most compounds suppressed this oestradiol-enhanced T47D proliferation via other mechanisms rather than ER binding.