Faculty of Pharmaceutical Sciences, University of Kinshasa, PO Box 212, Kinshasa XI, Democratic Repubic of Congo.
J Ethnopharmacol. 2010 Feb 3;127(2):215-20. doi: 10.1016/j.jep.2009.11.018. Epub 2009 Nov 29.
The study was aimed to evaluate the in vitro antispasmodic activity of Morinda morindoides leaves aqueous extract, its soluble fractions and isolated compounds to provide the pharmacological basis for its use for the treatment of constipation and diarrhoea in traditional medicine.
The antispasmodic activity of each sample was evaluated on acetylcholine (ACh) and the depolarized KCl solution induced contractions on guinea-pig isolated ileum suspended in Tyrode's solution.
At a test concentration of 40mug/ml in organ bath, the aqueous extract and its petroleum ether soluble fraction showed a spasmogenic effect on both agonists. The diethylether, ethyl acetate, n-butanol and residual aqueous phase soluble fractions from the partition of the aqueous extract exhibited spasmolytic activity producing 47-100% inhibition of contractions induced by both agonists with IC(50) values ranged from 6 to 15 microg/ml according to the case. In addition, the n-butanol and residual aqueous phase soluble fractions showed an inhibitory effect of 75 and 66% respectively on low high [K(+)] (25 mM) and 65 and 60% respectively on high [K+] (80 mM). Crude flavonoids showed spasmolytic on both agonists while crude saponins only showed spasmolytic activity on ACh and displayed spasmogenic effect on KCl. Quercetin, quercitrin and rutin exhibited significant antispasmodic effect with IC(50) values <0.1 microg/ml. Epoxygaertneroside and gaertneroside showed good antispasmodic activity on both agonists (4<IC(50)<7 microg/ml).
Morinda morindoides leaves possess spasmogenic and spasmolytic properties that can at least explain and support its traditional use against constipation and diarrhoea respectively.
本研究旨在评估菝葜叶水提物及其可溶部分和分离化合物的体外抗痉挛活性,为其在传统医学中治疗便秘和腹泻的应用提供药理学基础。
采用乙酰胆碱(ACh)和去极化 KCl 溶液诱导豚鼠离体回肠收缩的方法,评价各样本的抗痉挛活性。
在器官浴中 40μg/ml 的测试浓度下,水提物及其石油醚可溶部分对两种激动剂均表现出痉挛作用。水提物分配得到的二乙醚、乙酸乙酯、正丁醇和剩余水相可溶部分表现出痉挛抑制活性,对两种激动剂诱导的收缩分别产生 47-100%的抑制作用,根据情况,IC(50)值范围为 6-15μg/ml。此外,正丁醇和剩余水相可溶部分对低高[K+](25mM)分别表现出 75%和 66%的抑制作用,对高[K+](80mM)分别表现出 65%和 60%的抑制作用。粗黄酮对两种激动剂均表现出痉挛抑制作用,而粗皂苷仅对 ACh 表现出痉挛抑制作用,对 KCl 表现出痉挛作用。槲皮素、槲皮苷和芦丁表现出显著的抗痉挛作用,IC(50)值<0.1μg/ml。环氧加特纳苷和加特纳苷对两种激动剂均表现出良好的抗痉挛活性(4<IC(50)<7μg/ml)。
菝葜叶具有痉挛作用和痉挛抑制作用,至少可以分别解释和支持其传统上用于治疗便秘和腹泻的用途。