Okumura K, Nomura H, Iwakawa S, Hori R
Department of Hospital Pharmacy, School of Medicine, Kobe University, Japan.
J Pharmacobiodyn. 1991 Jun;14(6):301-7. doi: 10.1248/bpb1978.14.301.
The effect of fasting and sialoadenectomy on the binding of human epidermal growth factor (hEGF), beta-urogastrone, to plasma membranes isolated from rat gastric mucosa was studied to investigate the physiological changes in gastric EGF receptors for developing hEGF as an anti-ulcer drug. The binding of [125I]hEGF to the gastric membranes was significantly decreased after 40 h of fasting. Maximal binding was decreased to 74% of the control value without alteration of the binding affinity (Kd = 0.42 and 0.44 nM for the control and fasting group, respectively). There was little change in the binding of [125I]insulin to the gastric plasma membranes in response to fasting. Removal of the submandibular glands did not decrease EGF binding to the gastric membranes. These results indicate that changes in EGF binding to its receptors occur on plasma membranes of the rat gastric mucosa depending on the nutrient state.
为了研究禁食和唾液腺切除对人表皮生长因子(hEGF,即β-尿抑胃素)与从大鼠胃黏膜分离的质膜结合的影响,以探究胃表皮生长因子受体的生理变化,从而开发hEGF作为抗溃疡药物。禁食40小时后,[125I]hEGF与胃膜的结合显著降低。最大结合量降至对照值的74%,而结合亲和力未改变(对照组和禁食组的Kd分别为0.42和0.44 nM)。禁食对[125I]胰岛素与胃质膜的结合几乎没有影响。切除下颌下腺并未降低EGF与胃膜的结合。这些结果表明,大鼠胃黏膜质膜上EGF与其受体的结合变化取决于营养状态。