Zawalich W S, Diaz V A
Am J Physiol. 1987 Mar;252(3 Pt 1):E370-4. doi: 10.1152/ajpendo.1987.252.3.E370.
Asperlicin, a product derived from the fungus Aspergillus alliaceus, antagonized the multiple stimulatory effects of cholecystokinin (CCK-8S) on isolated islets. At a level of 10 microM, asperlicin completely inhibited insulin release in response to 25 nM CCK-8S. Increasing the level of CCK-8S to 100 nM partially restored a secretory response, while an even greater insulin stimulatory effect was noted with 500 nM CCK-8S. The inhibitory effect of asperlicin on CCK-8S-induced release was reversible. Asperlicin exposure had no effect on glucose or glyceraldehyde-induced secretion. Asperlicin reduced, in parallel with secretion, the increase in 3H efflux from [3H]inositol prelabeled islets usually noted with CCK-8S addition. Asperlicin did not influence the small glucose-stimulated increase in 3H efflux. The results support the notion that asperlicin is a specific and potent antagonist of the multiple stimulatory effects of CCK-8S on islet tissue.
asperlicin是从真菌蒜曲霉中提取的一种产物，它能拮抗胆囊收缩素（CCK - 8S）对分离胰岛的多种刺激作用。在10微摩尔的浓度下，asperlicin能完全抑制胰岛对25纳摩尔CCK - 8S的胰岛素释放反应。将CCK - 8S的浓度增加到100纳摩尔可部分恢复分泌反应，而500纳摩尔的CCK - 8S则能产生更强的胰岛素刺激作用。asperlicin对CCK - 8S诱导的释放的抑制作用是可逆的。暴露于asperlicin对葡萄糖或甘油醛诱导的分泌没有影响。asperlicin与分泌同时减少了通常在添加CCK - 8S时所观察到的[3H]肌醇预标记胰岛中3H外流的增加。asperlicin不影响葡萄糖刺激引起的3H外流的小幅增加。这些结果支持了asperlicin是CCK - 8S对胰岛组织多种刺激作用的特异性强效拮抗剂这一观点。
