title: Diterpenes from Cryptomeria japonica inhibit androgen receptor transcriptional activity in prostate cancer cells.
abstract: We identified eight diterpenes from Cryptomeria japonica (Taxodiaceae), which inhibit the activity of the androgen receptor (AR) in human prostate cancer (PCa) 22Rv1-derived 103E cells. The compounds 6,12-dihydroxyabieta-5,8,11,13-tetraen-7-one ( 2), sugiol ( 3), ferruginol ( 4), and 5-epixanthoperol ( 7) have near 100 % AR inhibition efficacy at concentrations of 10, 5, 25, and 25 microM, respectively. Because these compounds have very similar structures, analysis of their differential activity may aid in the design of inhibitors for PCa treatment.
authors.affiliation: Agricultural Biotechnology Research Center, Academia Sinica, Taipei, Taiwan, ROC.
authors.forename: Wei-Chun
authors.initials: WC
authors.lastname: Tu
authors.forename: Sheng-Yang
authors.initials: SY
authors.lastname: Wang
authors.forename: Shih-Chang
authors.initials: SC
authors.lastname: Chien
authors.forename: Feng-Min
authors.initials: FM
authors.lastname: Lin
authors.forename: Li-Ru
authors.initials: LR
authors.lastname: Chen
authors.forename: Chih-Yang
authors.initials: CY
authors.lastname: Chiu
authors.forename: Pei-Wen
authors.initials: PW
authors.lastname: Hsiao
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D045744:Cell Line, Tumor / Q000187:drug effects / Q000378:metabolism; D032485:Cryptomeria; D004224:Diterpenes / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D020128:Inhibitory Concentration 50; D008297:Male; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D011471:Prostatic Neoplasms / Q000517:prevention & control; D011944:Receptors, Androgen / Q000378:metabolism*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004224:Diterpenes; D010936:Plant Extracts; D011944:Receptors, Androgen