SPECIFIC-INHIBITION OF CALCINEURIN BY TYPE-II SYNTHETIC PYRETHROID INSECTICIDES
SPECIFIC-INHIBITION OF CALCINEURIN BY TYPE-II SYNTHETIC PYRETHROID INSECTICIDES
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DOI：
10.1016/0006-2952(92)90710-z
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发表时间：
1992-04-15
影响因子：
5.8
通讯作者：
MATSUMURA, F
中科院分区：
文献类型：
--
作者：
ENAN, E;MATSUMURA, F
用一种放射性示踪剂和两种比色法研究了拟除虫菊酯和几种氯代烃类杀虫剂对神经钙调素依赖性蛋白磷酸酶钙调神经磷酸酶的抑制作用。研究发现，所有的II型拟除虫菊酯(氯氰菊酯、溴氰菊酯和氰戊菊酯)都是从牛脑中分离的钙调神经磷酸酶的有效抑制剂。它们的IC50值约为10(-9)~10(-11)M，而这些拟除虫菊酯、神经活性I型拟除虫菊酯和神经活性氯代烃杀虫剂的非杀虫手性异构体对该酶都没有显示出类似的活性。为了在原位证实II型拟除虫菊酯的作用，分离的完整大鼠脑突触体与[P-32]磷酸孵育，然后在存在和不存在0.1-mU-M溴氰菊酯的情况下去极化。正如预期的那样，由于钙调神经磷酸酶的作用，蛋白质的磷酸化水平急剧上升。溴氰菊酯导致脱磷过程明显延迟。结果表明，二型拟除虫菊酯对钙调神经磷酸酶有特异性抑制作用。
The inhibitory action of synthetic pyrethroids and some chlorinated hydrocarbon insecticides on the neural calcium-calmodulin-dependent protein phosphatase, calcineurin, was studied using one radiotracer and two colorimetric methods. It was found that all insecticidal Type II pyrethroids (cypermethrin, deltamethrin and fenvalerate) are potent inhibitors of isolated calcineurin from bovine brain. Their IC50 values were approximately 10(-9) to 10(-11) M. By contrast, neither noninsecticidal chiral isomers of these pyrethroids, neuroactive Type I pyrethroids nor neuroactive chlorinated hydrocarbon insecticides showed comparable potencies against this enzyme. To confirm the action of Type II pyrethroid in situ, isolated intact rat brain synaptosomes were incubated with [P-32]phosphoric acid and subsequently depolarized in the presence and absence of 0.1-mu-M deltamethrin. As expected, there was a sharp rise in protein phosphorylation due to the action of calcineurin. Deltamethrin caused a distinct delay in the dephosphorylation process. The results clearly indicate that calcineurin is specifically inhibited by Type II pyrethroids.