Aburada M, Takeda S, Sakurai M, Harada M
J Pharmacobiodyn. 1980 Aug;3(8):423-33. doi: 10.1248/bpb1978.3.423.
In the experiment on continuous perfusion of rat stomach in vivo, genipin inhibited only the gastric acid secretion induced by carbachol, but not by tetragastrin, or histamine. In the experiment on isolated organs, genipin showed a weak competitive anti-acetylcholine action on the intestinal contraction. Based on these facts and results reported previously, it is conceivable that anti-cholinergic action at least partly contributes to the genipin-induced inhibitory effect on gastric functions. Erythritol clearance was increased with the increase in bile flow by administration of genipin. Genipin showed a significant choleretic action, and just then the concentration of biliary bile acid was decreased inversely. In the relationship between bile flow and biliary bile acid excretion rate, the slope of regression line obtained from genipin-treated group was not significantly different from that of control, and these lines were approximately parallel to each other. Genipin did not affect the concentration of sodium, potassium, chloride, or bicarbonate in the bile collected during the initial stage, in which bile flow was increased, after administration. It is concluded from these results that genipin-induced choleretic action proceeds by a mechanism wherein water is driven along osmotic gradient which originates in the transport of bile acid-independent fraction from hepatocytes into canaliculi, mainly through active Na+ transport.
在大鼠胃体内连续灌注实验中，京尼平仅抑制由卡巴胆碱诱导的胃酸分泌，而不抑制由四肽胃泌素或组胺诱导的胃酸分泌。在离体器官实验中，京尼平对肠收缩表现出微弱的竞争性抗乙酰胆碱作用。基于这些事实以及先前报道的结果，可以推测抗胆碱作用至少部分促成了京尼平对胃功能的抑制作用。给予京尼平后，随着胆汁流量增加，赤藓醇清除率升高。京尼平表现出显著的利胆作用，与此同时，胆汁中胆汁酸的浓度呈相反降低。在胆汁流量与胆汁中胆汁酸排泄率的关系中，京尼平处理组得到的回归线斜率与对照组无显著差异，且这些线大致相互平行。京尼平不影响给药后胆汁流量增加的初始阶段所收集胆汁中钠、钾、氯或碳酸氢盐的浓度。从这些结果可以得出结论，京尼平诱导的利胆作用是通过一种机制进行的，即水沿着渗透梯度被驱动，这种渗透梯度源于胆汁酸非依赖部分从肝细胞向胆小管的转运，主要通过主动钠转运。
