Diterpenes from Cryptomeria japonica inhibit androgen receptor transcriptional activity in prostate cancer cells.
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.
Tu
Wei-Chun
WC
Agricultural Biotechnology Research Center, Academia Sinica, Taipei, Taiwan, ROC.
Wang
Sheng-Yang
SY
Chien
Shih-Chang
SC
Lin
Feng-Min
FM
Chen
Li-Ru
LR
Chiu
Chih-Yang
CY
Hsiao
Pei-Wen
PW
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*
D000972:Antineoplastic Agents, Phytogenic; D004224:Diterpenes; D010936:Plant Extracts; D011944:Receptors, Androgen