Erman A, Azuri R, Raz A
Biochem Pharmacol. 1983 Jul 1;32(13):2083-7. doi: 10.1016/0006-2952(83)90430-6.
Mepacrine and p-bromophenacyl bromide, in addition to their inhibitory effect on lipolysis, are also potent inhibitors of fatty acid acylation into renal medullary lipids. Significant qualitative and quantitative differences in the inhibition by the two drugs were seen. p-Bromophenacyl bromide exerted a non-selective effect inhibiting the incorporation of saturated and unsaturated fatty acids into all phospholipid classes and triacylglycerols. In contrast, mepacrine selectively inhibited the incorporation of both saturated and unsaturated acids into phosphatidylcholine, phosphatidylethanolamine and triglycerides, and concurrently markedly enhanced their incorporation into phosphatidylinositol. Quantitative analysis of these mepacrine effects, together with the known inhibitory effects of this compound on phospholipase A2 and phosphatidylinositol-specific phospholipase C, suggests that mepacrine also inhibits phosphatidic acid phosphatase, thereby shunting the flux of phosphatidic acid away from diglyceride formation and into synthesis of phosphatidylinositol.
除了对脂肪分解有抑制作用外，米帕林和对溴苯甲酰溴还是脂肪酸酰化进入肾髓质脂质的有效抑制剂。观察到这两种药物在抑制作用上存在显著的定性和定量差异。对溴苯甲酰溴产生非选择性作用，抑制饱和脂肪酸和不饱和脂肪酸掺入所有磷脂类别和三酰甘油中。相比之下，米帕林选择性地抑制饱和脂肪酸和不饱和脂肪酸掺入磷脂酰胆碱、磷脂酰乙醇胺和甘油三酯中，同时显著增强它们掺入磷脂酰肌醇中的量。对这些米帕林作用的定量分析，连同该化合物对磷脂酶A2和磷脂酰肌醇特异性磷脂酶C的已知抑制作用，表明米帕林还抑制磷脂酸磷酸酶，从而使磷脂酸的通量从甘油二酯形成转向磷脂酰肌醇的合成。
