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大黄素蒽酮对豚鼠离体回肠蠕动反射的影响:前列腺素的参与

Influence of rhein anthrone on peristaltic reflex of guinea-pig isolated ileum: involvement of prostaglandins.

作者信息

Nijs G, de Witte P, Geboes K, Meulemans A, Schuurkes J, Lemli J

机构信息

Laboratory of Pharmaceutical Biology and Phytopharmacology, Institute of Pharmaceutical Sciences, K.U. Leuven, Belgium.

出版信息

Br J Pharmacol. 1993 Jan;108(1):269-73. doi: 10.1111/j.1476-5381.1993.tb13473.x.

Abstract

1 The influence of rhein anthrone on the peristaltic reflex was studied with a modified Trendelenburg technique in a range from 10(-8) M to 4 x 10(-5) M, on a normal and reversed guinea-pig ileum segment. Rhein anthrone had no significant effects on longitudinal muscle tension, intraluminal pressure or volume displacement when tested on the normal segment in doses up to 10(-5) M. When applied to the mucosal side (reversed segment), rhein anthrone produced a dose-dependent increase of longitudinal muscle tension (significant from 10(-7) M), of intraluminal pressure (significant from 3 x 10(-6) M) and of volume displacement (significant from 10(-7) M). The data show that rhein anthrone possesses in vitro activity which is dependent on contact with the mucosa. 2 The action of rhein anthrone on the reversed segment was inhibited by BW755C (a dual inhibitor of cyclo-oxygenase and lipoxygenase), by indomethacin and by SC19220 (an antagonist of prostaglandin E2 (PGE2) and PGF2 alpha). The effects remaining on longitudinal muscle tension, intraluminal pressure and volume displacement, calculated as percentage (mean +/- s.e.mean) of the initial value, were respectively: 13 +/- 8; 23 +/- 13; 112 +/- 5 for BW755C; 66 +/- 19; 51 +/- 8; 53 +/- 8 for indomethacin and 27 +/- 12; 13 +/- 7; 50 +/- 5 for SC19220. It is concluded that arachidonic acid metabolites, especially PGE2 and PGF2 alpha are involved in the effects of rhein anthrone on the reversed segment.

摘要
  1. 采用改良的特伦德伦伯卧位技术,在10(-8)M至4×10(-5)M的浓度范围内,研究了大黄素蒽酮对正常及倒置豚鼠回肠段蠕动反射的影响。在正常肠段上,以高达10(-5)M的剂量测试时,大黄素蒽酮对纵肌张力、腔内压力或容积位移均无显著影响。当应用于黏膜侧(倒置肠段)时,大黄素蒽酮可使纵肌张力(从10(-7)M起显著升高)、腔内压力(从3×10(-6)M起显著升高)和容积位移(从10(-7)M起显著升高)呈剂量依赖性增加。数据表明,大黄素蒽酮具有体外活性,且这种活性依赖于与黏膜的接触。2. BW755C(环氧化酶和脂氧化酶的双重抑制剂)、吲哚美辛和SC19220(前列腺素E2(PGE2)和前列腺素F2α的拮抗剂)可抑制大黄素蒽酮对倒置肠段的作用。以初始值的百分比(平均值±标准误)计算,对纵肌张力、腔内压力和容积位移仍保留的影响分别为:BW755C为13±8、23±13、112±5;吲哚美辛为66±19、51±8、53±8;SC19220为27±12、13±7、50±5。由此得出结论,花生四烯酸代谢产物,尤其是PGE2和PGF2α参与了大黄素蒽酮对倒置肠段的作用。

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