Goppelt-Strübe M, Pfannkuche H J, Gemsa D, Resch K
Department of Pharmacology and Toxicology, Medical School Hannover, Federal Republic of Germany.
Biochem J. 1987 Nov 1;247(3):773-7. doi: 10.1042/bj2470773.
Prostanoids are synthesized by resident macrophages upon stimulation with diacylglycerols. Oleoylacetylglycerol and dioctanoylglycerol induced prostaglandin E and thromboxane synthesis in a time- and concentration-dependent manner. Both diacylglycerols inhibited the lysophosphatide acyltransferase, which is the key enzyme in the reacylation of arachidonic acid. By this mechanism the pool of free arachidonic acid available for prostanoid synthesis is increased. Both diacylglycerols were able to inhibit the membrane-bound lysophosphatide acyltransferase by a direct interaction independent of protein kinase C. Thus lysophosphatide acyltransferase could be shown to be a new target of these diacylglycerols, known as activators of protein kinase C.
前列腺素类物质是由驻留巨噬细胞在二酰基甘油刺激下合成的。油酰乙酰甘油和二辛酰甘油以时间和浓度依赖的方式诱导前列腺素E和血栓素的合成。这两种二酰基甘油均抑制溶血磷脂酰转移酶,该酶是花生四烯酸再酰化的关键酶。通过这种机制,可用于前列腺素合成的游离花生四烯酸池增加。这两种二酰基甘油都能够通过独立于蛋白激酶C的直接相互作用抑制膜结合的溶血磷脂酰转移酶。因此,溶血磷脂酰转移酶可被证明是这些二酰基甘油(已知为蛋白激酶C激活剂)的一个新靶点。