Department of Pharmacology, Faculty of Pharmaceutical Sciences, Government College University, Faisalabad, Pakistan.
College of Pharmacy, Department of Pharmacology, University of Punjab Old Campus, Lahore, Pakistan.
BMC Complement Med Ther. 2020 Jan 16;20(1):14. doi: 10.1186/s12906-019-2793-0.
Euphorbia hirta (Linn) family Euphorbiaceae has been used in indigenous system of medicine for the treatment of gastrointestinal disorders. This study was designed to determine the pharmacological basis for the medicinal use of E. hirta in diarrhea and constipation.
The aqueous-methanol extract of whole herb of E. hirta (EH.Cr) and its petroleum ether (Pet.EH), chloroform (CHCl.EH), ethyl acetate (Et.Ac.EH) and aqueous (Aq.EH) fractions were tested in the in-vivo experiments using Balb/c mice, while the in-vitro studies were performed on isolated jejunum and ileum preparations of locally bred rabbit and Sprague Dawley rats, respectively, using PowerLab data system.
Qualitative phytochemical analysis showed the presence of alkaloids, saponins, flavonoids, tannins, phenols, cardiac glycosides, while HPLC of EH.Cr showed quercetin in high proportion. In mice, EH.Cr at the dose of 500 and 1000 mg/kg showed 41 and 70% protection from castor oil-induced diarrhea, respectively, similar to the effect of quercetin and loperamide, while at lower doses (50 and 100 mg/kg), it caused an increase in the fecal output. In loperamide-induced constipated mice, EH.Cr also displayed laxative effect with respective values of 28.6 and 35.3% at 50 and 100 mg/kg. In rabbit jejunum, EH.Cr showed atropine-sensitive inhibitory effect in a concentration-dependent manner, while quercetin and nifedipine exhibited atropine-insensitive effects. Fractions of E. hirta also produced atropine-sensitive inhibitory effects except Pet.EH and CHCl.EH. On high (80 mM) and low (20 mM) K - induced contractions, the crude extract and fractions exhibited a concentration-dependent non-specific inhibition of both spasmogens and displaced concentration-response curves of Ca to the right with suppression of the maximum effect similar to the effect quercetin and nifedipine. Fractions showed wide distribution of spasmolytic and Ca antagonist like effects. In rat ileum, EH.Cr and its fractions exhibited atropine-sensitive gut stimulant effects except Pet.EH.
The crude extract of E. hirta possesses antidiarrheal effect possibly mediated through Ca antagonist like gut inhibitory constituents, while its laxative effect was mediated primarily through muscarinic receptor agonist like gut stimulant constituents. Thus, these findings provide an evidence to the folkloric use of E. hirta in diarrhea and constipation.
大戟科大戟属植物大飞扬（Euphorbia hirta （Linn））在传统医学中被用于治疗胃肠道疾病。本研究旨在确定大飞扬在腹泻和便秘中的药用价值的药理学基础。
采用Balb/c 小鼠进行体内实验，分别用大飞扬全草的水-甲醇提取物（EH.Cr）及其石油醚（Pet.EH）、氯仿（CHCl.EH）、乙酸乙酯（Et.Ac.EH）和水（Aq.EH）部分进行测试；同时，采用 PowerLab 数据系统，分别使用本地饲养的兔空肠和回肠以及 Sprague Dawley 大鼠的离体空肠和回肠制备物进行体外研究。
定性植物化学分析表明，该植物含有生物碱、皂苷、黄酮、单宁、酚类、强心苷，而 HPLC 分析显示高比例的槲皮素。在小鼠中，EH.Cr 以 500 和 1000mg/kg 的剂量分别显示出 41%和 70%对蓖麻油诱导的腹泻的保护作用，与槲皮素和洛哌丁胺的作用相似，而在较低剂量（50 和 100mg/kg）时，它会增加粪便排出量。在洛哌丁胺诱导的便秘小鼠中，EH.Cr 也显示出泻剂作用，分别在 50 和 100mg/kg 时达到 28.6%和 35.3%。在兔空肠中，EH.Cr 以浓度依赖性方式表现出阿托品敏感的抑制作用，而槲皮素和硝苯地平则表现出对阿托品不敏感的作用。除 Pet.EH 和 CHCl.EH 外，大飞扬的馏分也产生了阿托品敏感的抑制作用。在高（80mM）和低（20mM）K 引起的收缩中，粗提取物和馏分对两种痉挛原均表现出浓度依赖性的非特异性抑制作用，并使 Ca 对右位移的浓度反应曲线右移，最大效应受到抑制，与槲皮素和硝苯地平的作用相似。馏分显示出广泛的解痉和钙拮抗剂样作用。在大鼠回肠中，EH.Cr 及其馏分表现出阿托品敏感的肠道刺激作用，除 Pet.EH 外。
大飞扬的粗提取物具有抗腹泻作用，可能是通过类似钙拮抗剂的肠道抑制成分介导的，而其通便作用主要是通过类似毒蕈碱受体激动剂的肠道刺激成分介导的。因此，这些发现为大飞扬在腹泻和便秘中的民间应用提供了证据。
