Bierwolf B, Hartrodt B, Neubert R, Jakubke H D, Blech W
Biomed Biochim Acta. 1986;45(5):611-8.
By isolated perfused pancreas of Wistar rats the glucose (11 mmol/l) and arginine (10 mmol/l) stimulated insulin (IRI) and glucagon (IRG) secretion was measured in order to investigate the inhibitory activities of somatostatin-14 (SS 14) and the somatostatin analogue [3,14-L-seleno-cysteine, 8-D-tryptophan]-somatostatin (SeSS). SS-14 or SeSS (152.8 nmol/l) inhibit the glucose stimulated IRI secretion by 75 and 65%, respectively. Only the second phase of the biphasic arginine stimulated insulin secretion pattern by 40%. SeSS has under these conditions no effect, whereas 58 nmol/l SS-14 or SeSS show a suppressing effect on the first (20 and 55%, respectively) and second phase (65 and 85%, respectively) of the insulin secretion. Using 5.8 nmol/l SS-14 or SeSS the arginine stimulated IRG secretion was inhibited only in the second phase of the biphasic glucagon secretion pattern by about 40%. 58 nmol/l SS-14 or SeSS show an inhibiting effect on the first and on the second phase of secretion, in both cases about 50%. It is concluded that in the SS-14 molecule the sulfur of cysteine in position 3 and 14 can be exchanged by selenium without modifying the biological activities measured in the glucose or arginine stimulated IRI and IRG secretion in vitro. The D-Trp8 in the SeSS analogue does not show the typical better inhibitory action of D-Trp8-SS-14 on insulin and glucagon secretion compared with SS-14. Possibly the selenium in the SeSS analogue abolishes this effect.
通过对Wistar大鼠的离体灌注胰腺进行实验,测量葡萄糖(11 mmol/l)和精氨酸(10 mmol/l)刺激后的胰岛素(IRI)和胰高血糖素(IRG)分泌,以研究生长抑素-14(SS 14)和生长抑素类似物[3,14-L-硒代半胱氨酸,8-D-色氨酸]-生长抑素(SeSS)的抑制活性。SS-14或SeSS(152.8 nmol/l)分别使葡萄糖刺激的IRI分泌抑制75%和65%。仅对精氨酸刺激的胰岛素分泌双相模式的第二阶段有40%的抑制作用。在这些条件下SeSS无作用,而58 nmol/l的SS-14或SeSS对胰岛素分泌的第一阶段(分别为20%和55%)和第二阶段(分别为65%和85%)有抑制作用。使用5.8 nmol/l的SS-14或SeSS时,精氨酸刺激的IRG分泌仅在胰高血糖素分泌双相模式的第二阶段受到约40%的抑制。58 nmol/l的SS-14或SeSS对分泌的第一阶段和第二阶段均有抑制作用,两种情况下均约为50%。得出结论:在SS-14分子中,3位和14位半胱氨酸的硫可被硒取代,而不改变体外葡萄糖或精氨酸刺激的IRI和IRG分泌所测得的生物学活性。与SS-14相比,SeSS类似物中的D-Trp8对胰岛素和胰高血糖素分泌没有显示出D-Trp8-SS-14典型的更好抑制作用。可能是SeSS类似物中的硒消除了这种作用。