Greenwood-Van Meerveld B, Tyler K R, Venkova K, Kuge T
Oklahoma Foundation for Digestive Research, VA Medical Center, University of Oklahoma Health Science Center, USA.
Biol Pharm Bull. 2000 Aug;23(8):952-6. doi: 10.1248/bpb.23.952.
Wood creosote, a mixture of guaiacol, creosol and related compounds, has long been used as an antidiarrheal agent. The goal of our study was to investigate the antisecretory effect of wood creosote and to compare it to the effect of loperamide, a synthetic opioid widely used in the treatment of diarrhea. Experiments were performed in rat jejunal and colonic mucosal sheets, mounted in modified Ussing chambers. Active electrogenic transport was monitored electrically as short circuit current (Isc) and hypersecretory responses were induced by acetylcholine (ACh). Neither loperamide nor wood creosote had any significant effect on basal lsc, when added to the serosal bathing solution at concentrations of 0.1-50microg/ml. In contrast, under hypersecretory conditions, both agents showed concentration-dependent (0.1--100microg/ml) antisecretory effects inhibiting ACh-induced responses in the jejunum and colon. However, the effects suggest regional differences, with loperamide being most potent in the jejunum, while wood creosote showed equal potency in both jejunum and colon. Based upon these in vitro findings, we conclude that like loperamide, the antidiarrheal action of wood creosote is due, at least in part, to its antisecretory activity.
木馏油,一种由愈创木酚、甲酚和相关化合物组成的混合物,长期以来一直被用作止泻剂。我们研究的目的是调查木馏油的抗分泌作用,并将其与洛哌丁胺(一种广泛用于治疗腹泻的合成阿片类药物)的作用进行比较。实验在安装于改良的尤斯灌流小室中的大鼠空肠和结肠黏膜片上进行。主动电转运通过短路电流(Isc)进行电监测,乙酰胆碱(ACh)诱导分泌亢进反应。当以0.1 - 50微克/毫升的浓度添加到浆膜浴液中时,洛哌丁胺和木馏油对基础Isc均无显著影响。相比之下,在分泌亢进条件下,两种药物均表现出浓度依赖性(0.1 - 100微克/毫升)的抗分泌作用,抑制空肠和结肠中ACh诱导的反应。然而,这些作用显示出区域差异,洛哌丁胺在空肠中作用最强,而木馏油在空肠和结肠中作用相当。基于这些体外研究结果,我们得出结论,与洛哌丁胺一样,木馏油的止泻作用至少部分归因于其抗分泌活性。