Barakat A, Skoglund G, Boissard C, Rosselin G, Marie J C
Institut National de la Santé et de la Recherche Médicale U.55, Hôpital Saint-Antoine, Paris, France.
Biosci Rep. 1994 Feb;14(1):1-13. doi: 10.1007/BF01901633.
The question as to whether the homologous peptides CGRP and IAPP can regulate insulin secretion in RINm5F cells was addressed. Chicken CGRP displayed a reproducible inhibitory effect on insulin secretion within 0.1 and 1 nM concentrations and a stimulatory effect at higher concentrations. The maximal stimulatory effects on insulin secretion were obtained with 1.0 microM of chicken CGRP (cCGRP), human alpha-CGRP (h alpha-CGRP) and human IAPP (hIAPP) which caused 246 +/- 22, 302 +/- 63 and 224 +/- 14 percent increases of control levels, respectively (p < 0.001). Similarly, maximal accumulations of cAMP were obtained with 1.0 microM of cCGRP, h alpha-CGRP and hIAPP with the respective percent increases of control levels of 587 +/- 24, 436 +/- 41 and 410 +/- 25 (p < 0.005). Thus the stimulatory effects on insulin secretion in RINm5F cells by cCGRP, h alpha-CGRP and hIAPP appear to be mediated by the cAMP pathway. Chicken CGRP, the most potent peptide tested, displayed a correlated dose response stimulation of intracellular cAMP and insulin release within the concentration range of 10-1000nM. The EC50 values of cCGRP for cAMP accumulation and insulin release were similar (20nM and 10nM respectively). The stimulatory effect of IAPP on cAMP was not additive with that of cCGRP suggesting that IAPP action was mediated by CGRP receptors. This hypothesis was further sustained by a preferential inhibition of 125I[His]h alpha-CGRP binding to RINm5F cells by cCGRP as compared to IAPP. We conclude that CGRP and IAPP, through a direct action on a chicken CGRP preferring receptor present in beta cells, stimulated insulin by a cAMP mediated pathway.
研究了同源肽降钙素基因相关肽(CGRP)和胰岛淀粉样多肽(IAPP)是否能调节RINm5F细胞中胰岛素分泌的问题。鸡CGRP在0.1至1 nM浓度范围内对胰岛素分泌表现出可重复的抑制作用,而在较高浓度时则表现出刺激作用。用1.0 microM的鸡CGRP(cCGRP)、人α-CGRP(hα-CGRP)和人IAPP(hIAPP)对胰岛素分泌产生最大刺激作用,分别使对照水平增加246±22%、302±63%和224±14%(p<0.001)。同样,用1.0 microM的cCGRP、hα-CGRP和hIAPP可使cAMP达到最大积累,对照水平分别增加587±24%、436±41%和410±25%(p<0.005)。因此,cCGRP、hα-CGRP和hIAPP对RINm5F细胞胰岛素分泌的刺激作用似乎是由cAMP途径介导的。所测试的最有效肽鸡CGRP在10 - 1000 nM浓度范围内对细胞内cAMP和胰岛素释放表现出相关的剂量反应刺激。cCGRP对cAMP积累和胰岛素释放的半数有效浓度(EC50)值相似(分别为20 nM和10 nM)。IAPP对cAMP的刺激作用与cCGRP的刺激作用无相加性,提示IAPP的作用是由CGRP受体介导的。与IAPP相比,cCGRP对125I[His]hα-CGRP与RINm5F细胞结合的优先抑制进一步支持了这一假说。我们得出结论,CGRP和IAPP通过直接作用于β细胞中存在的优先结合鸡CGRP的受体,通过cAMP介导的途径刺激胰岛素分泌。