Open AccessEffects of the flavonoid baicalin and its metabolite baicalein on androgen receptor expression, cell cycle progression and apoptosis of prostate cancer cell lines
Author(s) -
Chen S.,
Ruan Q.,
Bedner E.,
Deptala A.,
Wang X.,
Hsieh T.C.,
Traganos F.,
Darzynkiewicz Z.
Publication year - 2001
Publication title -
cell proliferation
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.647
H-Index - 74
eISSN - 1365-2184
pISSN - 0960-7722
DOI - 10.1046/j.0960-7722.2001.00213.x
Subject(s) - baicalein , baicalin , lncap , androgen receptor , cell growth , chemistry , apoptosis , in vivo , pharmacology , prostate cancer , biology , biochemistry , medicine , cancer , high performance liquid chromatography , microbiology and biotechnology , chromatography
. Recent studies on the Chinese herbal medicine PC SPES showed biological activities against prostate cancer in vitro , in vivo and in patients with advanced stages of the disease. In investigating its mode of action, we have isolated a few of the active compounds. Among them, baicalin was the most abundant (about 6%) in the ethanol extract of PC SPES, as determined by HPLC. Baicalin is known to be converted in vivo to baicalein by the cleavage of the glycoside moiety. Therefore, it is useful to compare their activities in vitro . The effects of baicalin and baicalein were studied in androgen‐positive and ‐negative human prostate cancer lines LNCaP and JCA‐1, respectively. Inhibition of cell growth by 50% (ED 50 ) in LNCaP cells was seen at concentrations of 60.8 ± 3.2 and 29.8 ± 2.2 µ m baicalin and baicalein, respectively. More potent growth inhibitory effects were observed in androgen‐negative JCA‐1 cells, for which the ED 50 values for baicalin and baicalein were 46.8 ± 0.7 and 17.7 ± 3.4, respectively. Thus, it appears that cell growth inhibition by these flavonoids is independent of androgen receptor status. Both agents (1) caused an apparent accumulation of cells in G 1 at the ED 50 concentration, (2) induced apoptosis at higher concentrations, and (3) decreased expression of the androgen receptor in LNCaP cells.