Abood L G, Salem N, MacNeil M, Bloom L, Abood M E
Biochim Biophys Acta. 1977 Jul 4;468(1):51-62. doi: 10.1016/0005-2736(77)90150-x.
A study was undertaken on the possible involvement of phospholipids on stereospecific opiate binding to a rat brain membrane fraction comprised mainly of synaptic membranes. The addition of acidic phospholipids such as phosphatidylserine, phosphoinositides, and phosphatidic acid significantly enhanced opiate binding. With the exception of phosphatidylserine, when the acidic phospholipids contained a polyunsaturated acyl group, they were actually inhibitory, along with neutral phospholipids derived from brain. Both the C18:0, C18:1 form (derived from myelin) and the C18:0, C22:6 form of phosphatidylserine (derived from synaptic membranes) produced as much as a 45% enhancement in opiate binding. Unsaturated fatty acids were highly inhibitory, the degree of inhibition being related to the degree of unsaturation. Both phospholipase A and C were inhibitory; and the inhibitory effect of A could not be prevented by albumin or overcome with the addition of phosphatidylserine. With the use of the cross-linking agent, dinitrodifluorobenzene, it could be demonstrated that the phosphatidylserine of synaptic membranes appeared to be preferentially associated with membrane protein. The enhancement of opiate binding by phosphatidylserine diminished with increasing degree of cross-linking.
开展了一项关于磷脂可能参与立体特异性阿片类药物与主要由突触膜组成的大鼠脑膜组分结合的研究。添加酸性磷脂如磷脂酰丝氨酸、磷酸肌醇和磷脂酸可显著增强阿片类药物的结合。除磷脂酰丝氨酸外，当酸性磷脂含有多不饱和酰基时，它们实际上具有抑制作用，脑源性中性磷脂也是如此。磷脂酰丝氨酸的C18:0、C18:1形式（源自髓磷脂）和C18:0、C22:6形式（源自突触膜）在阿片类药物结合方面产生高达45%的增强作用。不饱和脂肪酸具有高度抑制作用，抑制程度与不饱和度相关。磷脂酶A和C均具有抑制作用；A的抑制作用不能被白蛋白阻止，也不能通过添加磷脂酰丝氨酸来克服。使用交联剂二硝基氟苯可以证明，突触膜的磷脂酰丝氨酸似乎优先与膜蛋白结合。随着交联程度的增加，磷脂酰丝氨酸对阿片类药物结合的增强作用减弱。
