Beubler E, Kollar G, Saria A, Bukhave K, Rask-Madsen J
Department of Experimental and Clinical Pharmacology, University of Graz, Austria.
Gastroenterology. 1989 Feb;96(2 Pt 1):368-76. doi: 10.1016/0016-5085(89)91560-6.
The diarrhea of cholera is considered to rely solely on a cyclic adenosine monophosphate-mediated secretory mechanism. However, both 5-hydroxytryptamine and prostaglandin E2 have been proposed to be involved in the pathogenesis of cholera. In vivo experiments were performed, therefore, in the rat jejunum to investigate the influence of purified cholera toxin on fluid secretion, luminal release of 5-hydroxytryptamine and prostaglandin E2, and formation of mucosal cyclic adenosine monophosphate. Also the effects of ketanserin, indomethacin, verapamil, and nifedipine on the named parameters were studied. Cholera toxin dose-dependently (0.1-0.5 microgram/ml) and time-dependently (1-5 h) increased mean net fluid secretion with a maximum response at 4 h. It also caused a significant (p less than 0.01) rise in release of 5-hydroxytryptamine and prostaglandin E2, in addition to formation of cyclic adenosine monophosphate. The dose-response curve for cholera toxin-induced fluid secretion was shifted to the right by indomethacin (10 mg/kg s.c.) and ketanserin (200 micrograms/kg s.c.), none of which caused a change in cholera toxin-induced release of 5-hydroxytryptamine. However, both agents significantly decreased the release of prostaglandin E2. Verapamil (0.2-9.5 micrograms/min i.a.) and nifedipine (0.05-0.5 microgram/min i.a.) dose-dependently reduced cholera toxin-induced fluid secretion. The estimated local concentrations at half-maximal inhibition were 5 x 10(-7) M verapamil and 5 x 10(-8) M nifedipine, respectively. The cholera toxin-induced increase in release of 5-hydroxytryptamine and prostaglandin E2 and formation of cyclic adenosine monophosphate was unaffected by verapamil. These results support the concept that cholera toxin-induced fluid secretion in vivo is caused, in part, by release of 5-hydroxytryptamine, which in turn stimulates formation of prostaglandin E2.
霍乱腹泻被认为仅依赖于环磷酸腺苷介导的分泌机制。然而,5-羟色胺和前列腺素E2都被认为与霍乱的发病机制有关。因此,在大鼠空肠中进行了体内实验,以研究纯化的霍乱毒素对液体分泌、5-羟色胺和前列腺素E2的腔内释放以及黏膜环磷酸腺苷形成的影响。还研究了酮色林、吲哚美辛、维拉帕米和硝苯地平对上述参数的影响。霍乱毒素剂量依赖性地(0.1 - 0.5微克/毫升)和时间依赖性地(1 - 5小时)增加平均净液体分泌,在4小时时达到最大反应。它还导致5-羟色胺和前列腺素E2的释放以及环磷酸腺苷的形成显著增加(p < 0.01)。吲哚美辛(10毫克/千克皮下注射)和酮色林(200微克/千克皮下注射)使霍乱毒素诱导的液体分泌剂量反应曲线右移,两者均未引起霍乱毒素诱导的5-羟色胺释放的变化。然而,两种药物均显著降低了前列腺素E2的释放。维拉帕米(0.2 - 9.5微克/分钟腹腔注射)和硝苯地平(0.05 - 0.5微克/分钟腹腔注射)剂量依赖性地减少霍乱毒素诱导的液体分泌。半数最大抑制时的估计局部浓度分别为5×10⁻⁷ M维拉帕米和5×10⁻⁸ M硝苯地平。维拉帕米不影响霍乱毒素诱导的5-羟色胺和前列腺素E2释放以及环磷酸腺苷的形成增加。这些结果支持这样的概念,即霍乱毒素在体内诱导的液体分泌部分是由5-羟色胺的释放引起的,而5-羟色胺又反过来刺激前列腺素E2的形成。