Anti-androgenic activity of fatty acids

Jie Liu, Kuniyoshi Shimizu, Ryuichiro Kondo

Research output: Contribution to journalArticlepeer-review

39 Citations (Scopus)


In this study, we show that 5α-reductase derived from rat fresh liver was inhibited by certain aliphatic free fatty acids. The influences of chain length, unsaturation, oxidation, and esterification on the potency to inhibit 5a-reductase activity were studied. Among the fatty acids we tested, inhibitory saturated fatty acids had C12-C16 chains, and the presence of a C=C bond enhanced the inhibitory activity. Esterification and hydroxy compounds were totally inactive. Finally, we tested the prostate cancer cell proliferation effect of free fatty acids. In keeping with the results of the 5α-reductase assay, saturated fatty acids with a C12 chain (lauric acid) and unsaturated fatty acids (oleic acid and α-linolenic acid) showed a proliferation inhibitory effect on lymph-node carcinoma of the prostate (LNCaP) cells. At the same time, the testosterone-induced prostate-specific antigen (PSA) mRNA expression was down-regulated. These results suggested that fatty acids with 5α-reductase inhibitory activity block the conversion of testosterone to 5α-dihydrotestosterone (DHT) and then inhibit the proliferation of prostate cancer cells.

Original languageEnglish
Pages (from-to)503-512
Number of pages10
JournalChemistry and Biodiversity
Issue number4
Publication statusPublished - 2009

All Science Journal Classification (ASJC) codes

  • Bioengineering
  • Biochemistry
  • General Chemistry
  • Molecular Medicine
  • Molecular Biology


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