Cattaneo M G, Amoroso D, Gussoni G, Sanguini A M, Vicentini L M
Department of Pharmacology, University of Milan, Italy.
FEBS Lett. 1996 Nov 18;397(2-3):164-8. doi: 10.1016/s0014-5793(96)01159-3.
Somatostatin possesses antisecretory and antiproliferative activity on some human tumors. We herein report that, in a human neuroblastoma cell line, the somatostatin analogue BIM 23014 inhibited mitogen-activated protein (MAP) kinase activity stimulated by either insulin-like growth factor-1, whose receptor bears a tyrosine kinase, or carbachol, which acts at a G-protein coupled receptor. In a human small cell lung carcinoma line BIM inhibited serum-stimulated MAP kinase activation. These inhibitory actions occur in a dose range quite similar to that observed for suppression of proliferation induced by the analogue in the same cell lines. The decrease in cAMP elicited by the analogue in the two cell lines is not responsible for its inhibitory action on MAP kinase and cell growth. Moreover, the analogue did not modify intracellular [Ca2+] and pH. An involvement of a phosphatase activity is suggested.
生长抑素对某些人类肿瘤具有抗分泌和抗增殖活性。我们在此报告,在一种人类神经母细胞瘤细胞系中,生长抑素类似物BIM 23014可抑制由胰岛素样生长因子-1(其受体带有酪氨酸激酶)或卡巴胆碱(作用于G蛋白偶联受体)刺激的丝裂原活化蛋白(MAP)激酶活性。在一种人类小细胞肺癌细胞系中,BIM可抑制血清刺激的MAP激酶活化。这些抑制作用发生的剂量范围与在相同细胞系中观察到的该类似物抑制增殖的剂量范围非常相似。该类似物在两种细胞系中引起的cAMP减少并非其对MAP激酶和细胞生长的抑制作用的原因。此外,该类似物未改变细胞内[Ca2+]和pH。提示有磷酸酶活性参与其中。