摘要
Omega-3(n-3)和omega-6(n-6)多不饱和脂肪酸(PUFA)在健康和病理状况中起着至关重要的作用,并且常常是相反的调节作用。 n-3和n-6 PUFA经历了生物转化,成为一系列平行的脂质介体,它们是许多细胞过程的有效调节剂。源自n-6 PUFA的脂质介体具有广泛的生物学作用,这些介体已成为许多临床批准药物(包括世界卫生组织列出的拉坦前列素(Xalatan:辉瑞))开发中的先导化合物。它被列为世卫组织基本药物模型清单。 n-3 PUFA衍生的介体受到的关注较少,部分原因是早期研究表明n-3 PUFA只是作为生物转化酶的竞争底物,并减少了n-6 PUFA衍生的脂质介体的形成。但是,最近的研究表明,n-3 PUFA衍生的介体本身具有生物学上的重要意义。现在正在出现,许多n-3 PUFA衍生的脂质介体具有与n-6对应物不同的有效且多样的活性。这些发现为药物发现提供了新的机会。在这里,我们审查了n-3 PUFA衍生的脂质介体的生物合成,并强调了其可用于药物开发的生物学作用。最后,我们提供了药物化学研究的实例,该实例利用了n-3 PUFA衍生的脂质介体作为药物设计中的新型先导化合物。
关键词: 多不饱和脂肪酸,脂质介体,脂蛋白,omega-3,生物转化,药物设计策略。
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