摘要
In this study, we show that 5-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 5-reductase activity were studied. Among the fatty acids we tested, inhibitory saturated fatty acids had C12–C16 chains, and the presence of a CC 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 5-reductase assay, saturated fatty acids with a C12 chain (lauric acid) and unsaturated fatty acids (oleic acid and -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 5-reductase inhibitory activity block the conversion of testosterone to 5-dihydrotestosterone (DHT) and then inhibit the proliferation of prostate cancer cells.
摘要译文
在这项研究中，我们表明，5-还原酶从大鼠新鲜肝脏衍生抑制由某些脂肪的游离脂肪酸。链长的影响，不饱和度，氧化，和酯化对效力抑制5-还原酶活性进行了研究。间的脂肪酸我们测试，抑制饱和脂肪酸有C 12 -C 16链，和一个CC键的存在而增强的抑制活性。酯化和羟基化合物是完全无效的。最后，我们测试了游离脂肪酸的前列腺癌细胞增殖的作用。符合5-还原酶测定的结果，脂肪酸与C 12链（月桂酸）和不饱和脂肪酸（油酸和亚麻酸）显示对前列腺（LNCaP细胞）细胞的淋巴结癌的增殖抑制效果。同时，睾酮诱导的前列腺特异性抗原（PSA）的mRNA表达下调。结果表明，脂肪酸与5α-还原酶抑制活性嵌段睾酮转化为5-二氢睾酮（DHT），然后抑制前列腺癌细胞的增殖。
Jie Liu, Kuniyoshi Shimizu and Ryuichiro Kondo. Anti-Androgenic Activity of Fatty Acids[J]. Chemistry & Biodiversity, 2009,6(4): 503-512