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[酪氨酸激酶和酪氨酸磷酸酶抑制剂对ATP和毒胡萝卜素诱导的大鼠腹膜巨噬细胞Ca2+内流的影响]

[Effect of tyrosine kinase and tyrosine phosphatase inhibitors on ATP- and thapsigargin-induced CA2+ entry in rat peritoneal macrophages].

作者信息

Krutetskaia Z I, Levedev O E, Tiushev V E, Krutetskaia N I, Roshchina N G

出版信息

Tsitologiia. 1997;39(2-3):164-76.

PMID:9312907
Abstract

The effect of two structurally distinct tyrosine kinase inhibitors, genistein (100 microM) and methyl-2, 5-dihydroxycinnamate (25 microM) on ATP- and thapsigargin-induced Ca2+ signals in Fura-2-loaded rat peritoneal macrophages was investigated. Both compounds were shown to inhibit ATP-evoked Ca2+ entry but not to release from internal stores. Both compounds also inhibit the store-dependent or "capacitative" Ca2+ influx stimulated by emptying the intracellular Ca2+ stores with endoplasmic Ca(2+)-ATPase inhibitor thapsigargin (100 nM). Genistein and methyl-2, 5-dihydroxycinnamate have no effect on Ca2+ release from intracellular stores. Tyrosine phosphatase inhibitor orthovanadate Na (50 microM) increases ATP-induced Ca2+ entry but does not prevent the inhibitory effect of genistein. These data are compatible with the role played by tyrosine phosphorylation in the control of Ca2+ entry in rat peritoneal macrophages.

摘要

研究了两种结构不同的酪氨酸激酶抑制剂染料木黄酮(100微摩尔)和2,5 - 二羟基肉桂酸甲酯(25微摩尔)对用Fura - 2负载的大鼠腹腔巨噬细胞中ATP和毒胡萝卜素诱导的Ca2+信号的影响。结果表明,这两种化合物均能抑制ATP诱发的Ca2+内流,但不会导致细胞内钙库释放Ca2+。这两种化合物还能抑制通过用内质网Ca(2+)-ATP酶抑制剂毒胡萝卜素(100纳摩尔)排空细胞内Ca2+储存而刺激的储存依赖性或“容量性”Ca2+内流。染料木黄酮和2,5 - 二羟基肉桂酸甲酯对细胞内钙库释放Ca2+没有影响。酪氨酸磷酸酶抑制剂原钒酸钠(50微摩尔)可增加ATP诱导的Ca2+内流,但不能阻止染料木黄酮的抑制作用。这些数据与酪氨酸磷酸化在大鼠腹腔巨噬细胞Ca2+内流控制中所起的作用相符。

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