摘要
目的：探讨致痫剂马桑内酯（ｃｏｒｉａｒｉａｌａｃｔｏｎｅ）对大鼠大脑皮层突触膜Ｃａ２＋，Ｍｇ２＋ＡＴＰ酶的作用。方法：酶底物动力学分析（Ｈａｎｅｓ作图法）。结果：马桑内酯对Ｃａ２＋，Ｍｇ２＋ＡＴＰ酶具有抑制作用，在１．２×１０－９～６．０×１０－７ｍｏｌ·Ｌ－１范围内，随浓度增加其抑制作用增强。此作用有明显的时效关系，抑制作用随作用时间延长而增强。酶底物动力学分析表明，马桑内酯对该酶的抑制属非竞争性抑制。结论：马桑内酯是Ｃａ２＋，Ｍｇ２＋ＡＴＰ酶的强力抑制剂。本文对Ｃａ２＋，Ｍｇ２＋ＡＴＰ酶与胞内游离钙之间的关系及该酶抑制在癫痫发病机制中的意义进行了讨论。
OBJECTIVE:To study the effects of coriaria lactone(CL) on the Ca 2+ ,Mg 2+ ATPase activities of rat brain synaptic membranes.METHOD:Enzyme substrate kinetic analysis using Hanes plot.RESULTS:The inhibitory effect of CL was obviously dose dependent within the extent of 6×10 -9 ～6×10 -7 mol·L -1 .This inhibitory action was increased with the prolonged incubation time between CL(1.2×10 -7 mol·L -1 ) and the synaptic membranes.The enzyme substrate kinetic analysis indicated that it was the noncompetitive inhibition.CONCLUSION:CL was a potent inhibitor of Ca 2+ ,Mg 2+ ATPase.Furthermore,the significance of the inhibitory effect in the epileptic mechanism and the relationship between intracellular free calcium and the Ca 2+ ,Mg 2+ ATPase activity were discussed.
出处
《中国药学杂志》
CAS
CSCD
北大核心
1997年第1期14-16,共3页
Chinese Pharmaceutical Journal
