4.4 Article

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

Journal

NATURAL PRODUCT RESEARCH
Volume 27, Issue 18, Pages 1611-1619

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2012.742079

Keywords

Lentinus polychrous Lev; sterol; estrogenic activity; anti-estrogenic activity; oestrogen receptor

Funding

  1. Office of the Higher Education Commission, Thailand
  2. Center of Research and Development of Herbal Health Products, Khon Kaen University, Thailand
  3. Laboratory of Pharmacognosy, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan

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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.

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