Jackson J K, Lauener R, Duronio V, Burt H M
Faculty of Pharmaceutical Sciences, University of British Columbia, Vancouver, Canada.
J Rheumatol. 1997 Feb;24(2):341-8.
We investigated whether phosphatidylinositol (PI) 3-kinase is involved in the signal transduction pathway leading to neutrophil activation by inflammatory microcrystals.
Neutrophil chemiluminescence and degranulation responses to opsonized crystals were measured in the presence of selective inhibitors known to inhibit PI 3-kinase activity in neutrophils.
Wortmannin and LY 294002, 2 selective inhibitors of PI 3-kinase, were shown to inhibit neutrophil activation induced by plasma opsonized crystals of calcium pyrophosphate dihydrate (CPPD) [both monoclinic (M) and triclinic (T) forms] and monosodium urate monohydrate (MSUM). IC50 for wortmannin or LY 294002 inhibition of crystal induced respiratory burst (measured by chemiluminescence) was about 3 nM and 0.3 microM, respectively, proving the pivotal role of PI 3-kinase in neutrophil respiratory burst activation by all 3 crystals. Degranulation responses of neutrophils to CPPD(M) and CPPD(T) crystals were also inhibited by about 50% by wortmannin in the 10 to 20 nM concentration range, supporting the direct involvement of PI 3-kinase in signal transduction pathways leading to crystal induced neutrophil degranulation. All 3 crystals induced the activation of PI 3-kinase in neutrophils as measured by the increased PI 3-kinase activity associated with immunoprecipitated tyrosine phosphorylated proteins from 1 min crystal-neutrophil incubations. Neutrophils pretreated with wortmannin at 10 nM showed sub-basal levels of PI 3-kinase activity at all time points measured.
PI 3-kinase plays a central role in the signal transduction pathways leading to respiratory burst and degranulation responses in neutrophils activated by inflammatory microcrystals.
我们研究了磷脂酰肌醇(PI)3激酶是否参与炎症微晶导致中性粒细胞激活的信号转导途径。
在已知能抑制中性粒细胞中PI 3激酶活性的选择性抑制剂存在的情况下,测量中性粒细胞对调理晶体的化学发光和脱颗粒反应。
PI 3激酶的两种选择性抑制剂渥曼青霉素和LY 294002被证明可抑制由焦磷酸钙(CPPD)[单斜(M)和三斜(T)形式]和一水合尿酸钠(MSUM)的血浆调理晶体诱导的中性粒细胞激活。渥曼青霉素或LY 294002抑制晶体诱导的呼吸爆发(通过化学发光测量)的IC50分别约为3 nM和0.3 μM,证明PI 3激酶在所有3种晶体激活中性粒细胞呼吸爆发中起关键作用。渥曼青霉素在10至20 nM浓度范围内也使中性粒细胞对CPPD(M)和CPPD(T)晶体的脱颗粒反应抑制约50%,支持PI 3激酶直接参与导致晶体诱导中性粒细胞脱颗粒的信号转导途径。通过与1分钟晶体 - 中性粒细胞孵育后免疫沉淀的酪氨酸磷酸化蛋白相关的PI 3激酶活性增加来测量,所有3种晶体均诱导中性粒细胞中PI 3激酶的激活。用10 nM渥曼青霉素预处理的中性粒细胞在所有测量时间点均显示PI 3激酶活性低于基础水平。
PI 3激酶在炎症微晶激活的中性粒细胞导致呼吸爆发和脱颗粒反应的信号转导途径中起核心作用。