Meier H L, Gross C L, Papirmeister B
Biochem Pharmacol. 1986 Dec 1;35(23):4125-30. doi: 10.1016/0006-2952(86)90686-6.
The serine esterase inhibitor diisopropyl fluorophosphate (DFP) had been reported previously to inhibit IgE-dependent histamine release. Recently, it has been demonstrated that lower concentrations of DFP enhance IgE-dependent histamine release and inhibit desensitization. This manuscript describes the abilities of several esterase inhibitors to cause release of histamine from human leukocytes (basophils), by a process that is IgE-independent. This esterase inhibitor-induced histamine release appears to be by a non-cytotoxic mechanism that requires calcium and is temperature dependent. These histamine release processes occurred over a longer period of time than IgE-dependent release. Direct release of histamine by these small molecular weight inhibitors and inhibition of desensitization both suggest that one or more serine esterases are involved in the regulation of histamine release from human basophils.
丝氨酸酯酶抑制剂二异丙基氟磷酸酯(DFP)此前已有报道可抑制IgE依赖性组胺释放。最近,有研究表明较低浓度的DFP可增强IgE依赖性组胺释放并抑制脱敏作用。本论文描述了几种酯酶抑制剂通过一种不依赖IgE的过程,使人白细胞(嗜碱性粒细胞)释放组胺的能力。这种酯酶抑制剂诱导的组胺释放似乎是通过一种非细胞毒性机制实现的,该机制需要钙且依赖温度。这些组胺释放过程比IgE依赖性释放持续的时间更长。这些小分子抑制剂直接释放组胺以及对脱敏作用的抑制均表明,一种或多种丝氨酸酯酶参与了人嗜碱性粒细胞组胺释放的调节。