二酰基甘油激酶和二酰基甘油脂肪酶抑制剂对大鼠腹膜肥大细胞组胺释放的作用。
The actions of inhibitors of diacylglycerol kinase and diacylglycerol lipase on histamine release from rat peritoneal mast cells.
作者信息
Cantwell M E, Foreman J C
机构信息
Department of Pharmacology, University College London.
出版信息
Br J Pharmacol. 1987 Nov;92(3):597-601. doi: 10.1111/j.1476-5381.1987.tb11361.x.
Abstract
- RHC 80267 and R59 022 are selective inhibitors of diacylglycerol (DAG) lipase and DAG kinase enzymes respectively. These inhibitors were examined with regard to their effects on oleoylacetylglycerol (OAG)-and anti-IgE- induced histamine secretion in rat peritoneal mast cells. 2. RHC 80267, 10 microM and R59 022, 50 microM both enhanced OAG-induced histamine release by 30% and 40% respectively. 3. In the concentration range 3-30 microM, R59 022 enhanced anti-IgE-induced histamine release by up to about 40%, whereas RHC 80267 was without effect. 4. The enhancement of anti-IgE-induced histamine release by R59 022 is consistent with a role for protein kinase C in transducing immunological signals to rat peritoneal mast cells. 5. The lack of effect of RHC 80267 in this situation may indicate that in the mast cell, DAG kinase is more active than DAG lipase in degrading physiological levels of DAG.
摘要
- RHC 80267和R59 022分别是二酰基甘油（DAG）脂肪酶和DAG激酶的选择性抑制剂。研究了这些抑制剂对大鼠腹膜肥大细胞中油酰乙酰甘油（OAG）和抗IgE诱导的组胺分泌的影响。2. 10微摩尔的RHC 80267和50微摩尔的R59 022分别使OAG诱导的组胺释放增加了30%和40%。3. 在3至30微摩尔的浓度范围内，R59 022使抗IgE诱导的组胺释放增加了约40%，而RHC 80267则没有作用。4. R59 022增强抗IgE诱导的组胺释放，这与蛋白激酶C在将免疫信号转导至大鼠腹膜肥大细胞中的作用一致。5. 在这种情况下RHC 80267没有作用，这可能表明在肥大细胞中，DAG激酶在降解生理水平的DAG方面比DAG脂肪酶更活跃。
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