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• W1981595708 abstract "Anti-androgens are used to treat prostate cancer. Here, we report that hydroxyxanthones from a plant extract act as anti-androgens in androgen receptor (AR)-positive prostate cancer LNCaP cells. Anti-androgenic activity of the ethanol extract from Garcinia subelliptica was observed in a luciferase assay using LNCaP/MMTV cells with a stably integrated mouse mammary tumor virus (MMTV) promoter. HPLC-based activity profiling followed by a chemical library-based assay strategy enabled the rapid identification of several active principles bearing a xanthone core substituted with hydroxyl and isoprenyl groups. Among the active compounds, 2-(1,1-dimethyl-allyl)-1,4,5,6-tetrahydroxyxanthone (subelliptenone F) was identified as a potent inhibitor of AR transcriptional activity. The structure-activity relationship of some substituents on the xanthone core was also determined using the chemical library-based bioassay. A quantitative RT-PCR analysis revealed that treatment with the compound resulted in a significant reduction in AR-induced gene (KLK3) expression. Hydroxyxanthone may be a possible candidate for the development of a new anti-androgenic molecule." @default.
• W1981595708 created "2016-06-24" @default.
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• W1981595708 date "2014-01-01" @default.
• W1981595708 modified "2023-09-25" @default.
• W1981595708 title "Anti-androgenic activity of hydroxyxanthones in prostate cancer LNCaP cells" @default.
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• W1981595708 doi "https://doi.org/10.1016/j.fitote.2013.09.014" @default.
• W1981595708 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24084319" @default.
• W1981595708 hasPublicationYear "2014" @default.
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