新合成的亚油酸衍生物DCP-LA作为潜在抗痴呆药物的评价

Tomoyuki Nishizaki , Takeshi Kanno , Akinobu Gotoh
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引用次数: 0

摘要

目的用环丙烷环代替顺双键合成亚油酸衍生物8-[2-(2-戊基-环丙基甲基)-环丙基]辛酸(DCP-LA)。本文介绍一种新型抗痴呆药物DCP-LA。研究片段和结果dcp - la选择性直接激活蛋白激酶C-ε (PKCε),通过促进α7乙酰胆碱(ACh)受体向细胞表面转运和增加突触前谷氨酸释放来增强突触前α7乙酰胆碱(ACh)受体的活性。DCP-LA的这种作用引起了海马突触传递的持久促进,从而改善了动物模型中的学习和记忆障碍。结论dcp - la是一种很有前途的抗痴呆药物,为治疗包括阿尔茨海默病在内的痴呆症提供了新的希望。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Evaluation of the newly synthesized linoleic acid derivative DCP-LA as a potential anti-dementia drug

Purpose

We synthesized the linoleic acid derivative 8-[2-(2-pentyl-cyclopropylmethyl)-cyclopropyl]-octanoic acid (DCP-LA) with cyclopropane rings instead of cis-double bonds. Here, we introduce DCP-LA as a novel anti-dementia drug.

Study section and results

DCP-LA selectively and directly activated protein kinase C-ε (PKCε) to enhance the activity of presynaptic α7 acetylcholine (ACh) receptors by promoting receptor translocation to the cell surface and increasing presynaptic glutamate release. This action of DCP-LA caused a long-lasting facilitation of hippocampal synaptic transmission, which improved learning and memory impairments in animal models.

Conclusion

DCP-LA could be developed as a promising anti-dementia drug, offering new hope for treating dementias including Alzheimer disease.

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