1-linoleoylglycerol (1-monolinolein)

1-Linoleoyl glycerol（1-LG）是一种从三白草（Saururus chinensis）根中分离的天然脂肪酸甘油单酯，它是脂蛋白相关磷脂酶A2（LpPLA2，又称PAF乙酰水解酶，PAF-AH）的特异性抑制剂，以45μM的IC50值竞争性结合酶活性位点[1]。血小板活化因子（PAF）是一种具有生物活性的磷脂，由多种受刺激细胞合成，可作为血小板聚集、炎症及过敏反应的介质[2,3]。PAF可被PAF乙酰水解酶（PAF-AH）转化为无生物活性的溶血PAF，研究发现，血浆PAF-AH与动脉粥样硬化相关，可能是人类冠心病的一个正向危险因素[4]。同时，1-LG的甘油骨架与亚油酸链的结构特性使其成为磷脂、糖脂等复杂脂质的生物合成前体，为脂质组学研究提供关键中间体[5]。此外，1-LG能显著减轻载脂蛋白CIII诱导的炎症反应，通过下调促炎症因子IL-6的表达发挥免疫调节功能[6]。这些特性使1-LG在动脉粥样硬化模型构建、脂质代谢通路解析及天然产物抗炎机制研究中具有广泛的研究价值。

参考文献

[1] Lee WS, Kim MJ, Beck YI, Park YD, Jeong TS. Lp-PLA2 inhibitory activities of fatty acid glycerols isolated from Saururus chinensis roots. Bioorg Med Chem Lett. 2005 Aug 1;15(15):3573-5.

[2] Prescott SM, Zimmerman GA, McIntyre TM. Platelet-activating factor. J Biol Chem. 1990 Oct 15;265(29):17381-4.

[3] Snyder F. Platelet-activating factor and related acetylated lipids as potent biologically active cellular mediators. Am J Physiol. 1990 Nov;259(5 Pt 1):C697-708.

[4] Caslake MJ, Packard CJ. Lipoprotein-associated phospholipase A2 (platelet-activating factor acetylhydrolase) and cardiovascular disease. Curr Opin Lipidol. 2003 Aug;14(4):347-52.

[5] Archambault AS, Tinto F, Dumais É, Rakotoarivelo V, Kostrzewa M, Plante PL, Martin C, Simard M, Silvestri C, Pouliot R, Laviolette M, Boulet LP, Vitale RM, Ligresti A, Di Marzo V, Flamand N. Biosynthesis of the Novel Endogenous 15-Lipoxygenase Metabolites N-13-Hydroxy-octodecadienoyl-ethanolamine and 13-Hydroxy-octodecadienoyl-glycerol by Human Neutrophils and Eosinophils. Cells. 2021 Sep 5;10(9):2322.

[6] Han X, Wang T, Zhang J, Liu X, Li Z, Wang G, Song Q, Pang D, Ouyang H, Tang X. Apolipoprotein CIII regulates lipoprotein-associated phospholipase A2 expression via the MAPK and NFκB pathways. Biol Open. 2015 Apr 2;4(5):661-5.