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Effects of Inhibitors of Protein Kinase C on the Release and Synthesis of Histamine in Rat Basophilic Leukemia Cells (2H3)

机译:蛋白激酶C抑制剂对大鼠嗜碱性粒细胞(2H3)组织胺释放和合成的影响

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References(27) Cited-By(1) In rat basophilic leukemia cells (2H3), a tumor analog of mast cells, the aggregation of IgE receptors results in histamine secretion and the increase in histidine decarboxylase activity which synthesizes histamine. Using inhibitors of protein kinase C, we studied the relationships between these events and protein kinase C which is activated by antigens. Histamine release is suppressed by inhibitors of protein kinase C, staurosporine, K252-a and H-7, in this decreasing order of effectiveness; and the IC50 values are 1.5 nM, 29.9 nM and 3.8 μM, respectively. The changes in the intracellular Ca concentration monitored by fura-2 fluorescence is not modified by staurosporine, although the histamine response is suppressed. Meanwhile, the increase of histidine decarboxylase was abolished by inhibitors of protein kinase C; staurospor ine was the strongest, K-252a of moderate activity and H-7, the weakest, having IC50 values of 0.8 nM, 100 nM and 11.5 μM, respectively. The inhibitors of protein kinase C suppress both histamine secretion and synthesis. Therefore, the histamine synthesis may be stimulated via activation of protein kinase C to supplement the released histamine.
机译:参考文献(27)被引用的By(1)在肥大细胞的肿瘤类似物大鼠嗜碱性粒细胞(2H3)中,IgE受体的聚集导致组胺的分泌和组氨酸脱羧酶活性的增加,从而合成了组胺。我们使用蛋白激酶C的抑制剂研究了这些事件与被抗原激活的蛋白激酶C之间的关系。组胺的释放被蛋白激酶C,星形孢菌素,K252-a和H-7的抑制剂抑制,其有效性递减。 IC50值分别为1.5 nM,29.9 nM和3.8μM。尽管组胺反应受到抑制,但呋喃2荧光未改变呋喃2荧光监测的细胞内Ca浓度的变化。同时,蛋白激酶C抑制剂消除了组氨酸脱羧酶的增加;星形孢菌素最强,中等活性的K-252a,最弱的H-7,IC50值分别为0.8 nM,100 nM和11.5μM。蛋白激酶C的抑制剂抑制组胺的分泌和合成。因此,可以通过激活蛋白激酶C来补充所释放的组胺来刺激组胺的合成。

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