Shareef Huma, Rizwani Ghazala H, Mandukhail Safur R, Watanabe Naoharu, Gilani Anwar H
Department of Pharmacognosy, Faculty of Pharmacy, University of Karachi, University road, Karachi 75270, Pakistan.
BMC Complement Altern Med. 2014 Dec 12;14:479. doi: 10.1186/1472-6882-14-479.
Traditionally, Operculina turpethum has been used in a wide range of ailments such as, gastrointestinal disturbances and asthma. It is found in China, South Asia, Pacific Islands, and Australia. This study was aimed to provide a possible pharmacological basis for the medicinal use of O. turpethum in gut and airways disorders.
Castor oil-induced diarrhoeal mice model and isolated tissue preparations such as, rabbit jejunum and guinea-pig tracheal preparations were used to test the antidiarrhoeal, antispasmodic and bronchodilator effects and the possible mode of action(s) of the 70% aqueous-ethanolic extract of O. turpethum black variety (OTB).
In the castor oil-induced diarrhoea in mice, the crude extract of OTB caused a dose-dependent (300-1000 mg/kg) protection from diarrhoea, similar to that of loperamide. In isolated rabbit jejunum preparations, OTB produced a dose-dependent inhibition of spontaneous and high K+(80 mM)-induced contractions with resultant median effective concentrations (EC50 with 95% confidence interval) of 1.04 mg/ml (0.59-1.54) and 0.12 mg/ml (0.10-0.15; n = 4) respectively, thus showing more potency against K+. Pretreatment of the tissue with OTB (0.01 and 0.03 mg/ml) caused a rightward shift in the concentration response curves of Ca++, similar to that of verapamil. In isolated guinea-pig tracheal preparations, OTB caused inhibition of carbachol and high K+-induced constriction at similar concentrations with respective EC50 value of 0.66 mg/ml (0.53-0.82) and 0.59 mg/ml (0.45-0.62). Activity-directed fractionation revealed that the ethyl acetate fraction was more potent than the parent crude extract and hexane fraction.
These results suggest that the crude extract of O. turpethum possesses antidiarrhoeal, antispasmodic and bronchodilator activities, mediated possibly through the presence of Ca++ antagonist like constituent(s), though additional mechanism(s) cannot be ruled out. Thus, this study provides the evidence for the medicinal use of plant in diarrhoea and asthma.
传统上，圆叶牵牛已被用于治疗多种疾病，如胃肠道紊乱和哮喘。它在中国、南亚、太平洋岛屿和澳大利亚均有发现。本研究旨在为圆叶牵牛在肠道和气道疾病中的药用提供可能的药理学依据。
采用蓖麻油诱导的腹泻小鼠模型以及离体组织标本，如兔空肠和豚鼠气管标本，来测试圆叶牵牛黑色变种（OTB）70%水乙醇提取物的止泻、解痉和支气管扩张作用及其可能的作用方式。
在蓖麻油诱导的小鼠腹泻中，OTB粗提物对腹泻产生剂量依赖性（300 - 1000 mg/kg）的保护作用，与洛哌丁胺相似。在离体兔空肠标本中，OTB对自发收缩和高钾（80 mM）诱导的收缩产生剂量依赖性抑制，其半数有效浓度（EC50及95%置信区间）分别为1.04 mg/ml（0.59 - 1.54）和0.12 mg/ml（0.10 - 0.15；n = 4），因此对钾离子表现出更强的效力。用OTB（0.01和0.03 mg/ml）预处理组织导致钙离子浓度 - 反应曲线右移，与维拉帕米相似。在离体豚鼠气管标本中，OTB在相似浓度下对卡巴胆碱和高钾诱导的收缩产生抑制作用，其EC50值分别为0.66 mg/ml（0.53 - 0.82）和0.59 mg/ml（0.45 - 0.62）。活性导向分级分离显示乙酸乙酯级分比母体粗提物和己烷级分更有效。
这些结果表明，圆叶牵牛粗提物具有止泻、解痉和支气管扩张活性，可能是通过存在类似钙离子拮抗剂的成分介导的，尽管不能排除其他机制。因此，本研究为该植物在腹泻和哮喘治疗中的药用提供了证据。
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