Hall D W, van den Hoven W E
Scand J Gastroenterol Suppl. 1986;122:11-3. doi: 10.3109/00365528609102579.
Colloidal bismuth subcitrate (CBS), PGE2, sucralfate, and cimetidine have been investigated for their mucosal protective effects in the ethanol-induced gastric erosion model in rats; moreover, to gain an insight into the mechanisms of action of CBS, its ability to stimulate the synthesis of gastric mucosal PGE2 was determined. Although less potent than PGE2 at inhibiting ethanol-induced gastric lesions, CBS was about 4 times more potent than sucralfate. Cimetidine displayed only very weak protective activities. CBS showed a time-dependent inhibition of ethanol-induced lesions. Complete protection was observed 15 min after treatment with CBS and partial protection was observed at 8 h, although no protection was found at 16 h. CBS increased the potential of rat gastric mucosa to synthesize PGE2 in a dose-dependent way. Up to 3-fold increases above the basal levels were found. Peak synthesis of PGE2 occurred 15 min after CBS and elevated levels were still found after 4 h. It is concluded from these studies that CBS produces potent gastric protection towards ethanol-induced injury in the rat. CBS also considerably increases the ability of rat gastric mucosa to synthesize PGE2 which may be an underlying biochemical mechanism for its protective properties on the gastric mucosa.
已对枸橼酸铋钾(CBS)、前列腺素E2(PGE2)、硫糖铝和西咪替丁在乙醇诱导的大鼠胃糜烂模型中的黏膜保护作用进行了研究;此外,为深入了解CBS的作用机制,还测定了其刺激胃黏膜PGE2合成的能力。虽然在抑制乙醇诱导的胃损伤方面不如PGE2有效,但CBS的效力约为硫糖铝的4倍。西咪替丁仅表现出非常微弱的保护活性。CBS对乙醇诱导的损伤呈现出时间依赖性抑制作用。用CBS治疗15分钟后观察到完全保护作用,8小时时观察到部分保护作用,而在16小时时未发现保护作用。CBS以剂量依赖性方式增加大鼠胃黏膜合成PGE2的能力。发现其水平比基础水平最高增加了3倍。CBS给药后15分钟时PGE2合成达到峰值,4小时后仍维持在较高水平。从这些研究得出结论,CBS对大鼠乙醇诱导的损伤具有强大的胃保护作用。CBS还显著提高了大鼠胃黏膜合成PGE2的能力,这可能是其对胃黏膜具有保护特性的潜在生化机制。