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留兰香的钙通道阻滞活性解释了其在腹泻和肠道痉挛中的药用用途。

Calcium channel blocking activity of Mentha longifolia L. explains its medicinal use in diarrhoea and gut spasm.

机构信息

Natural Product and Drug Discovery Division, Department of Biological and Biomedical Sciences Aga Khan University Medical College, Karachi, Pakistan.

出版信息

Phytother Res. 2010 Sep;24(9):1392-7. doi: 10.1002/ptr.3263.

Abstract

Mentha longifolia has a reputation in traditional medicine in the indications of diarrhoea and gut spasm. This study was carried out to provide a possible pharmacological basis for its medicinal use in hyperactive gut disorders. In a castor oil induced diarrhoeal model, the crude extract of Mentha longifolia (Ml.Cr), at doses of 100-1000 mg/kg, provided 31-80% protection, similar to loperamide. In isolated rabbit jejunum preparations, Ml.Cr caused inhibition of spontaneous and high K(+)-induced contractions, with respective EC50 values of 1.80 (1.34-2.24; n = 6-8) and 0.60 mg/mL (0.37-0.85; n = 6-8), which suggests spasmolytic activity, mediated possibly through calcium channel blockade (CCB). The CCB activity was further confirmed when pretreatment of the tissue with Ml.Cr (0.3-1 mg/mL) caused a rightward shift in the Ca(++) concentration-response curves (CRCs), similar to verapamil. Loperamide also inhibited spontaneous and high K(+)-induced contractions and shifted the Ca(++) CRCs to the right. Activity-directed fractionation revealed that the petroleum spirit fraction was more potent than the parent crude extract and aqueous fraction. These data indicate that the antidiarrhoeal and spasmolytic effects of the crude extract of Mentha longifolia are mediated through the presence of CCB-like constituent(s), concentrated in the petroleum spirit fraction and this study provides indirect evidence for its medicinal use in diarrhoea and spasm.

摘要

留兰香在传统医学中有治疗腹泻和肠道痉挛的功效。本研究旨在为其在治疗肠道蠕动过度相关疾病方面的药用价值提供可能的药理学基础。在蓖麻油诱导的腹泻模型中,留兰香粗提物(Ml.Cr)在 100-1000mg/kg 剂量下可提供 31-80%的保护作用,与洛哌丁胺相当。在离体兔空肠标本中,Ml.Cr 可抑制自发性和高钾(K+)诱导的收缩,其 EC50 值分别为 1.80(1.34-2.24;n=6-8)和 0.60mg/mL(0.37-0.85;n=6-8),提示其具有解痉活性,可能通过钙通道阻断(CCB)介导。Ml.Cr(0.3-1mg/mL)预处理组织时,CCB 活性进一步得到证实,导致 Ca(++)浓度-反应曲线(CRC)右移,与维拉帕米相似。洛哌丁胺也抑制自发性和高钾(K+)诱导的收缩,并使 Ca(++)CRC 右移。活性导向的分步分离显示,石油醚部分比原始粗提物和水相部分更有效。这些数据表明,留兰香粗提取物的止泻和解痉作用是通过存在 CCB 样成分介导的,这些成分集中在石油醚部分,该研究为其在腹泻和痉挛方面的药用用途提供了间接证据。

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