Damholt A B, Buchan A M, Kofod H
Diabetes Discovery, Novo Nordisk A/S, Bagsvaerd, Denmark.
Endocrinology. 1998 Apr;139(4):2085-91. doi: 10.1210/endo.139.4.5921.
Glucagon-like peptide-1(7-36)amide (GLP-1) is a potent insulinotropic peptide released from the small intestine. To investigate the regulation of GLP-1 secretion, we established a GLP-1 release assay based on primary canine intestinal L-cells. The ileal mucosa was digested with collagenase/EDTA to a single cell suspension and enriched for L-cells by counterstream centrifugal elutriation. We performed release assays on the cultured cells after 36 h, and GLP-1 in the supernatant was determined by enzyme-linked immunoabsorbent assay (ELISA). Glucose-dependent insulinotropic peptide (GIP) dose dependently stimulated the release of GLP-1 and resulted in a 2-fold increase at 100 nM GIP. This effect was fully inhibited by 10 nM somatostatin. However, neither basal or GIP stimulated GLP-1 secretion were affected by ambient glucose concentrations from 5-25 mM. The receptor-independent secretagogues beta phorbol myristate acetate and forskolin dose dependently increased the secretion of GLP-1; effects inhibited by staurosporine and H8 respectively. Costimulation with GIP and phorbol ester, but not forskolin, resulted in an additive response. Furthermore, the effect of GIP could be inhibited by H8 but not by staurosporine. These results indicate that glucose does not directly stimulate canine L-cells. It is more probable that glucose releases GIP from the upper intestine that in turn stimulates GLP-1 secretion. The ability of GIP to stimulate GLP-1 secretion is probably mediated through activation of protein kinase A.
胰高血糖素样肽-1(7-36)酰胺(GLP-1)是一种从小肠释放的强效促胰岛素肽。为了研究GLP-1分泌的调节机制,我们建立了一种基于原代犬肠道L细胞的GLP-1释放测定法。用胶原酶/乙二胺四乙酸(EDTA)消化回肠黏膜使其成为单细胞悬液,并通过逆流离心淘析法富集L细胞。36小时后对培养的细胞进行释放测定,通过酶联免疫吸附测定法(ELISA)测定上清液中的GLP-1。葡萄糖依赖性促胰岛素肽(GIP)以剂量依赖的方式刺激GLP-1的释放,在100 nM GIP时导致其释放量增加2倍。这种作用被10 nM生长抑素完全抑制。然而,基础状态下或GIP刺激的GLP-1分泌均不受5-25 mM环境葡萄糖浓度的影响。不依赖受体的促分泌剂佛波醇肉豆蔻酸酯和福斯高林以剂量依赖的方式增加GLP-1的分泌;其作用分别被星形孢菌素和H8抑制。GIP与佛波醇酯共同刺激,但与福斯高林共同刺激则不会,会产生相加反应。此外,GIP的作用可被H8抑制,但不能被星形孢菌素抑制。这些结果表明,葡萄糖不会直接刺激犬L细胞。更有可能的是,葡萄糖从上部肠道释放GIP,进而刺激GLP-1分泌。GIP刺激GLP-1分泌的能力可能是通过蛋白激酶A的激活介导的。