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毛果铁苋菜提取物及化合物的解痉活性

Antispasmodic activity of extracts and compounds of Acalypha phleoides Cav.

作者信息

Astudillo Adela, Hong Enrique, Bye Robert, Navarrete Andrés

机构信息

Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, Ciudad Universitaria, Coyoacán 04510, México D. F., México.

出版信息

Phytother Res. 2004 Feb;18(2):102-6. doi: 10.1002/ptr.1414.

Abstract

The aerial parts of Acalypha phleoides are usually prescribed in the Mexican traditional medicine for a variety of gastrointestinal complaints. The MeOH-CHCl(3) (1:1) extract of the aerial part of A. phleoides showed an inhibitory effect on the gastrointestinal propulsion of a charcoal meal in mice. In isolated guinea-pig ileum, this extract produced a concentration dependent inhibition of the contractions induced by 5-hydroxytryptamine, but it was unable to inhibit the contractions elicited by acetylcholine, histamine, KCl and BaCl(2). This extract produced also a concentration dependent inhibition of the spontaneous pendular movement of the isolated rabbit jejunum. This inhibitory activity was partially blocked by propranolol. The essential oil, obtained from the aerial part of this plant, was more potent than the MeOH-CHCl(3) (1:1) extract in inhibiting the spontaneous pendular movement of the rabbit jejunum. Thymol, camphor and gamma-terpinene were identified from the essential oil by GC-MS. These monoterpenes showed antispasmodic activity in the rabbit jejunum preparation, thymol was the most active compound, followed by camphor and gamma-terpinene. Thymol and camphor in high concentrations also showed tracheal relaxant properties, but gamma-terpinene did not. These in vivo and in vitro results tend to support the traditional use of A. phleoides as an antispasmodic agent.

摘要

墨西哥传统医学中,常使用粗毛铁苋菜的地上部分来治疗各种胃肠道疾病。粗毛铁苋菜地上部分的甲醇-三氯甲烷(1:1)提取物对小鼠炭末胃肠推进有抑制作用。在离体豚鼠回肠中,该提取物对5-羟色胺诱导的收缩产生浓度依赖性抑制,但不能抑制乙酰胆碱、组胺、氯化钾和氯化钡引起的收缩。该提取物对离体兔空肠的自发摆动运动也产生浓度依赖性抑制。普萘洛尔可部分阻断这种抑制活性。从该植物地上部分获得的精油在抑制兔空肠自发摆动运动方面比甲醇-三氯甲烷(1:1)提取物更有效。通过气相色谱-质谱联用仪从精油中鉴定出百里香酚、樟脑和γ-萜品烯。这些单萜在兔空肠标本中显示出解痉活性,百里香酚是最具活性的化合物,其次是樟脑和γ-萜品烯。高浓度的百里香酚和樟脑也显示出气管舒张特性,但γ-萜品烯没有。这些体内和体外实验结果倾向于支持粗毛铁苋菜作为解痉剂的传统用途。

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