Brun Y, Wang X P, Willemot J, Sevenet T, Demenge P
Laboratoire de Physiologie et Pharmacologie-PCEBM, Faculté de Pharmacie, Université Joseph Fourier, La Tronche, France.
Fundam Clin Pharmacol. 1998;12(1):30-6. doi: 10.1111/j.1472-8206.1998.tb00920.x.
Experimental antidiarrheal activity of a traditionally used medication, Salicairine, was demonstrated in comparison to loperamide by significant inhibition of castor oil-induced diarrhea in mice (increases in hard faeces/total faeces ratio of 38 and 54 and 5 and 54% with respect to controls, at 0.5 and 1 mL/kg and 1 and 2 mg/kg, respectively) and bisacodyl-induced increase in large intestine transit in rats (125 and 280 and 210% with respect to controls, at 0.4 and 2 mL/kg Salicairine and 5 mg/kg loperamide, respectively). Salicairine was able to reduce contractions of isolated rat duodenum induced by barium chloride and acetylcholine, although not completely (that is about 60%) as seen with loperamide. Also, it did not change normal gastrointestinal transit in mice at doses of 0.5 to 1 mL/kg, conversely to loperamide which had a significant effect (decrease of 50%) at 2 mg/kg. Finally, Salicairine at 0.01 mL/mL, like loperamide at 0.2 mg/mL, significantly increased net fluid absorption in rat colon, either in basal conditions (30 and 64% respectively) or after a prostaglandin E1-induced increase in net fluid secretion (41 and 35%, respectively). The antidiarrheal activity of Salicairine is possibly related, at least in part, to an increase in colon net fluid absorption or a decrease in net fluid secretion.
通过与洛哌丁胺比较,证明了传统用药水杨苷的实验性抗腹泻活性。在小鼠中,它能显著抑制蓖麻油诱导的腹泻(在0.5和1 mL/kg剂量下,硬粪便/总粪便比率相对于对照组分别增加38%和54%;在1和2 mg/kg剂量下,分别增加5%和54%);在大鼠中,能抑制比沙可啶诱导的大肠转运增加(水杨苷在0.4和2 mL/kg剂量下,相对于对照组分别增加125%和280%;洛哌丁胺在5 mg/kg剂量下增加210%)。水杨苷能够降低氯化钡和乙酰胆碱诱导的离体大鼠十二指肠收缩,尽管不像洛哌丁胺那样完全(约60%)。此外,在0.5至1 mL/kg剂量下,它不会改变小鼠的正常胃肠转运,相反,洛哌丁胺在2 mg/kg剂量时有显著作用(降低50%)。最后,0.01 mL/mL的水杨苷与0.2 mg/mL的洛哌丁胺一样,在基础条件下(分别增加30%和64%)或在前列腺素E1诱导净液体分泌增加后(分别增加41%和35%),均能显著增加大鼠结肠的净液体吸收。水杨苷的抗腹泻活性可能至少部分与结肠净液体吸收增加或净液体分泌减少有关。