Mimura T, Tsujibo H, Nishikawa M, Yamabe Y, Aonuma S
J Pharmacobiodyn. 1980 Sep;3(9):435-43. doi: 10.1248/bpb1978.3.435.
Fatty acids of C10:0, C12:0, C13:0, C14:0 and C16:0 significantly inhibited the amount of gastric juice, total acid output, and total peptic activity, but fatty acids of C17:0-C20:0 entirely failed to show significant inhibitory activity. Only the methyl ester of C14:0 showed significant inhibition of these parameters at the dose of 100 mg/kg, while at the dose of 200 mg/kg, methyl esters of fatty acids of fatty acids of C10:0, C12:0, C14:0, and C16:0 significantly inhibited these three parameters. alpha-Monoglyceride of C14:0 significantly inhibited the amount of gastric juice at the dose of 100 mg/kg, while alpha-monoglycerides of C10:0, C12:0', C13:0, C14:0, and C16:0 significantly inhibited the amount of gastric juice, total acid output, and total peptic activity at the dose of 200 mg/kg. In the case of intraduodenal administration, myristic acid also showed significant inhibition of these parameters at 100 and 200 mg/kg doses. The dose-activity correlation in gastric secretion inhibitory activity was examined with myristic acid and this activity was found to increase with increasing dose of the acid administered. Myristic acid significantly decreased the ulcer index in aspirin-induced ulcer, it was entirely ineffective in preventing histamine-induced ulcer. Finally, inhibitory effect of myristic acid on pepsin and histidine decarboxylase was examined in vitro and it was found that myristic acid inhibited peptic activity, but it had almost no effect of inhibiting the histidine decarboxylase activity.
C10:0、C12:0、C13:0、C14:0和C16:0脂肪酸显著抑制胃液分泌量、总酸排出量和总胃蛋白酶活性,但C17:0 - C20:0脂肪酸完全未表现出显著的抑制活性。仅C14:0甲酯在100 mg/kg剂量时对这些参数有显著抑制作用,而在200 mg/kg剂量时,C10:0、C12:0、C14:0和C16:0脂肪酸的甲酯显著抑制这三个参数。C14:0α - 单甘油酯在100 mg/kg剂量时显著抑制胃液分泌量,而C10:0、C12:0、C13:0、C14:0和C16:0的α - 单甘油酯在200 mg/kg剂量时显著抑制胃液分泌量、总酸排出量和总胃蛋白酶活性。在十二指肠内给药的情况下,肉豆蔻酸在100和200 mg/kg剂量时也对这些参数有显著抑制作用。用肉豆蔻酸研究了胃分泌抑制活性中的剂量 - 活性关系,发现该活性随给药酸剂量的增加而增强。肉豆蔻酸显著降低阿司匹林诱导溃疡的溃疡指数,但对组胺诱导的溃疡完全无效。最后,在体外研究了肉豆蔻酸对胃蛋白酶和组氨酸脱羧酶的抑制作用,发现肉豆蔻酸抑制胃蛋白酶活性,但对组氨酸脱羧酶活性几乎没有抑制作用。