Cristoni A, Nizzola R, Malandrino S, Pifferi G
Laboratorio Ricerca, Inverni della Beffa, Milano, Italy.
Farmaco. 1994 Apr;49(4):281-4.
Disodium salts of the dihemiphthalates of urs-12-ene-3 beta, 28-diol 3b and of ursa-9(11), 12-diene-3 beta,28-diol 4b were synthesized from uvaol and examined for their gastroprotective activity in rats. The effects showed by 3b and 4b, given p.o. in two antiulcer tests (ethanol induced gastric lesions and diclofenac induced gastric ulcers), were 5-25 times better than those of carbenoxolone. When given p.o. in the rat once a day for 5 days at a gastroprotective dose, 3b and 4b did not induce any change in urine excretion, whereas carbenoxolone significantly reduced urine volume, Na+ excretion and Na+/K+ ratio. In conclusion, 3b and 4b are effective antiulcer agents, devoid of mineral-corticoid activity and therefore provided with a good therapeutic index.
从羽扇豆醇合成了乌苏 -12-烯 -3β,28 -二醇3b和乌苏 -9(11),12 -二烯 -3β,28 -二醇4b的二半酞酸二钠盐，并对其在大鼠中的胃保护活性进行了研究。在两种抗溃疡试验（乙醇诱导的胃损伤和双氯芬酸诱导的胃溃疡）中口服给予3b和4b所显示的效果比甘珀酸钠好5至25倍。以胃保护剂量每天一次给大鼠口服3b和4b，持续5天，未引起尿量排泄的任何变化，而甘珀酸钠显著减少了尿量、Na⁺排泄和Na⁺/K⁺比值。总之，3b和4b是有效的抗溃疡药物，没有盐皮质激素活性，因此具有良好的治疗指数。
