Palla Amber Hanif, Khan Naveed Ahmed, Bashir Samra, Ur-Rehman Najeeb, Iqbal Junaid, Gilani Anwarul-Hassan
Department of Biological and Biomedical Sciences, The Aga Khan University Medical College, Karachi 74800, Pakistan.
Department of Biological and Biomedical Sciences, The Aga Khan University Medical College, Karachi 74800, Pakistan; Department of Pharmacy, College of Health Sciences, Mekelle University, PO Box 1871, Mekelle, Ethiopia.
J Ethnopharmacol. 2015 Feb 3;160:61-8. doi: 10.1016/j.jep.2014.11.030. Epub 2014 Nov 26.
ETHNOPHARMACOLOGICAL RELEVANCE: Linum usitatissimum, commonly known as Flaxseed has traditionally been used for the management of diarrhea and gastrointestinal infections. This study was planned to assess pharmacological basis for the medicinal use of Flaxseed in infectious and non-infectious diarrhea. MATERIALS AND METHODS: The crude aqueous-methanolic extract of Flaxseed was studied using the in vivo castor oil-induced diarrhea, gut motility and enteropooling assays. Mechanistic basis was further elucidated by testing the inhibitory effect on spontaneously contracting isolated rabbit jejunum preparations, suspended in a 10ml tissue bath containing Tyrode׳ solution, maintained at 37°C and aerated with carbogen. Antibacterial efficacy of the Flaxseed extract was tested against different enteric and non-enteric pathogenic bacteria using in vitro antibacterial assays. RESULTS: Flaxseed extract reduced the diarrheal score in mice, by 39%, 63.90% and 68.34% at the respective doses of 100, 300 and 500mg/kg. Intestinal secretions were reduced by 24.12%, 28.09% and 38.80%, whereas the intestinal motility was reduced by 31.66%, 46.98% and 56.20% at respective doses of 100, 300 and 500mg/kg. When tested on isolated rabbit jejunum preparations, Flaxseed extract produced a dose-dependent inhibition of both spontaneous and high K(+) (80mM)-induced contractions, and shifted the concentration-response curves of Ca(++) to the right with suppression of the maximum response, similar to that caused by verapamil. Flaxseed extract was found to possess bactericidal activity at the tested concentrations of 12.5mg/ml, against vancomycin-resistant Enterococcus faecalis (100%), Escherichia coli K1 (88.88%), methicillin-resistant Staphylococcus aureus (98.76%), Bacillus cereus (92.64%), Pseudomonas aeruginosa (76.83%) and Salmonella typhi (26.91±3.35%). The concentration of 10mg/ml showed bactericidal effects against all the aforementioned pathogens except Escherichia coli K1, whereas for Pseudomonas aeruginosa and Salmonella typhi, it was bacteriostatic at this concentration. CONCLUSIONS: Our results indicate that Linum usitatissimum (Flaxseed) extract exhibits antidiarrheal and antispasmodic activities by virtue of its antimotility and antisecretory effects which are mediated possibly through inhibition of Ca(++) channels, though additional mechanism(s) cannot be ruled out. Flaxseed extract proved effective against both enteric and non-enteric pathogens causing diarrhea, thus ensuring wide coverage and rationalizing its medicinal use in both the infectious and non-infectious diarrhea.
民族药理学相关性:亚麻籽,通常被称为亚麻籽,传统上一直用于治疗腹泻和胃肠道感染。本研究旨在评估亚麻籽在感染性和非感染性腹泻药用方面的药理学依据。 材料与方法:使用蓖麻油诱导的体内腹泻、肠道运动和肠内积液试验研究亚麻籽的粗水-甲醇提取物。通过测试对悬浮于含台氏液的10ml组织浴中、维持在37°C并用混合气充气的离体兔空肠自发收缩制剂的抑制作用,进一步阐明其作用机制。使用体外抗菌试验测试亚麻籽提取物对不同肠道和非肠道病原菌的抗菌效果。 结果:亚麻籽提取物在100、300和500mg/kg的相应剂量下,使小鼠腹泻评分分别降低了39%、63.90%和68.34%。在100、300和500mg/kg的相应剂量下,肠道分泌分别减少了24.12%、28.09%和38.80%,而肠道运动分别减少了31.66%、46.98%和56.20%。在离体兔空肠制剂上进行测试时,亚麻籽提取物对自发收缩和高钾(80mM)诱导的收缩均产生剂量依赖性抑制,并使钙离子浓度-反应曲线向右移动,同时最大反应受到抑制,类似于维拉帕米所引起的作用。发现在12.5mg/ml的测试浓度下,亚麻籽提取物对耐万古霉素粪肠球菌(100%)、大肠杆菌K1(88.88%)、耐甲氧西林金黄色葡萄球菌(98.7%)、蜡样芽孢杆菌(92.64%)、铜绿假单胞菌(76.83%)和伤寒沙门氏菌(26.91±3.35%)具有杀菌活性。10mg/ml的浓度对除大肠杆菌K1外的所有上述病原体均显示出杀菌作用,而对于铜绿假单胞菌和伤寒沙门氏菌,在此浓度下具有抑菌作用。 结论:我们的结果表明,亚麻籽提取物通过其抗运动和抗分泌作用表现出止泻和解痉活性,这可能是通过抑制钙离子通道介导的,尽管不能排除其他机制。亚麻籽提取物对引起腹泻的肠道和非肠道病原体均有效,从而确保了广泛的覆盖范围,并使其在感染性和非感染性腹泻中的药用合理化。
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