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

被引:43
作者
Fangkrathok, Niramai [1 ]
Sripanidkulchai, Bungorn [1 ]
Umehara, Kaoru [2 ]
Noguchi, Hiroshi [2 ]
机构
[1] Khon Kaen Univ, Ctr Res & Dev Herbal Hlth Prod, Fac Pharmaceut Sci, Khon Kaen 40002, Thailand
[2] Univ Shizuoka, Sch Pharmaceut Sci, Shizuoka 4228526, Japan
关键词
Lentinus polychrous Lev; sterol; estrogenic activity; anti-estrogenic activity; oestrogen receptor; ESTROGEN-RECEPTOR; BREAST-CANCER; CONSTITUENTS; MECHANISMS; PRODUCTS; GROWTH; STEROL;
D O I
10.1080/14786419.2012.742079
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
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-3,5,6-triol (2), 3,5-dihydroxy-(22E,24R)-ergosta-7,22-dien-6-one (3), ergosta-4,6,8(14),22-tetraen-3-one (4), (3,5,8,22E)-5,8-diepoxy-ergosta-6,22-dien-3-ol (5) and 5,8-epidioxy-(3,5,8,22E)-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 ER than ER. These results may suggest that most compounds suppressed this oestradiol-enhanced T47D proliferation via other mechanisms rather than ER binding.
引用
收藏
页码:1611 / 1619
页数:9
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