【摘要】 研究反肉桂酰 亮 异亮 甘 精 亮 鸟 [酰胺 ](tc LIGRLO) ,一种PAR 2激动剂 ,对肥大细胞类胰蛋白酶释放的影响。结果显示 ,经过 15min的培养 ,tc LIGRLO可引起比基础分泌量增加 1倍以上的类胰蛋白酶释放 ,作用强度超过抗IgE抗体和钙离子导入剂 (calciumionophoreA2 3 187,CI)。而反PAR 2激动剂 反肉桂酰 鸟 亮 精 甘 异亮 亮 [酰胺 ](tc OLRGIL)无此作用。培养时间延长到 3 0min时对tc LIGRLO的作用无明显影响。其时间关系曲线表明 ,tc LIGRLO的作用从 1min开始 ,3min后达高峰。结果表明 ,PAR 2激动剂tc LIGR LO是一种高效类胰蛋白酶释放刺激剂 ,在肥大细胞上可能有PAR 2存在更多还原

【Abstract】 Proteinase-activated receptor-2 (PAR-2) expression has been observed on numerous cell types. However, little is known about the functional expression of PAR-2 in human mast cells. In the current study, the actions of a PAR-2 agonist trans-cinnamoyl-Leu-Ile-Gly-Arg-Leu-Orn-amide (tc-LIGRLO) on tryptase release from dispersed human colonic mast cells were examined. The results showed that tc-LIGRLO was able to induce a fold increase in tryptase release over the basal level following a 15 min incubation of colonic mast cells, whereas tc-OLRGIL did not have any effect on tryptase release. The potency of tc-LIGRLO appeared greater than that of anti-IgE and calcium ionophore A23187 (CI) in induction of tryptase release. Extending the incubation time to 30 min had no significant effect on the actions of tc-LIGRLO or anti-IgE. In the time course study, it was observed that the tryptase release from mast cells induced by tc-LIGRLO started at 1 min and peaked at 3 min following incubation. The above-mentioned results indicate that tc-LIGRLO is a potent stimulus of tryptase release from human mast cells, which strongly suggests that PAR-2s are expressed in human mast cells.更多还原