Development and mechanistic study of novel anti-Alzheimer's disease drugs based on physiologically active fatty acid

我们已经报道了不含不稳定顺式双键的亚油酸类似物，称为DCP-LA，其在体外和体内系统中诱导LTP样持久促进海马神经传递。但是，DCP-LA是四种立体异构体的混合物，活性最强的异构体的测定方法一直存在争议。本研究采用脂肪酶介导的拆分方法，对DCP-LA的四种异构体进行了合成，并找到了活性最高的立体异构体。

We have already reported linoleic acid analogues without unstable cis-double bonds, called DCP-LA, which induced LTP-like long-lasting facilitation of hippocampal neurotransmission in both in vitro and in vivo systems. However, DCP-LA was four stereo-isomer mixtures, the determination of the most active isomer have been remained. In this reserch, we have developed synthetic route for the preparation of all of the four isomers of enantiomerically pure DCP-LA employing lipase-mediated resolution method, and found the most active stereoisomers.