Deparment of Botany, Islamia College University, Peshawar 25120, Pakistan.
Department of Pharmacy, Abdul Wali Khan University Mardan, Mardan 23200, Pakistan.
Molecules. 2022 Mar 26;27(7):2143. doi: 10.3390/molecules27072143.
(Euphorbiaceae) has been used as an emetic, anthelminthic, and cathartic agent in traditional medicine. We used gas chromatography-mass spectrometry (GC-MS) to characterize the composition of ethyl acetate (EAC) and dichloromethane (DCMC) fractions from the whole plant. EAC and DCMC fractions were evaluated for acetylcholinesterase (AChE) inhibitory activity and acute toxicity. Their effects on intestinal propulsive movement and spasmogenic activity of the gastrointestinal tract (GIT) muscle were also assessed. The compounds detected in both fractions were mostly fatty acids, with about seven compounds in EAC and 10 in DCMC. These included pharmacologically active compounds such as imipramine, used to treat depression, or hexadecanoic acid methyl ester, an antioxidant. Both EAC and DCMC fractions inhibited acetylcholinesterase (AChE) activity with IC values of 10 µg and 130 µg, respectively. Both the fractions were found to be toxic in a dose-dependent manner, inducing emesis at 0.5 g or higher and lethargy and mortality from 3-5 g upwards. Similarly, both of the fractions showed laxative activity in metronidazole- and loperamide-induced constipation models. EAC relaxed the intestinal muscle at a lower dose (1 mg/mL) than DCMC. Similarly, the EAC extract showed a significant relaxation effect (EC = 0.67 ± 0.15 mg/mL) on KCL-induced contraction in rabbit jejunum as compared to DCMC (EC = 5.04 ± 0.05 mg/kg). The present study strongly supports the folklore that this valuable plant is a cathartic agent. Further work is required to isolate and validate the bioactive compounds that act as diarrheal agents in
大戟科（Euphorbiaceae）植物在传统医学中被用作催吐剂、驱虫剂和泻药。我们使用气相色谱-质谱联用技术（GC-MS）对整株植物的乙酸乙酯（EAC）和二氯甲烷（DCMC）部分的成分进行了表征。评估了 EAC 和 DCMC 部分对乙酰胆碱酯酶（AChE）抑制活性和急性毒性的影响。还评估了它们对肠道推进运动和胃肠道（GIT）肌肉痉挛活性的影响。在这两个部分中检测到的化合物主要是脂肪酸，EAC 中有大约七种，DCMC 中有十种。其中包括用于治疗抑郁症的丙咪嗪等具有药理活性的化合物，或作为抗氧化剂的十六烷酸甲酯。EAC 和 DCMC 部分均能抑制乙酰胆碱酯酶（AChE）活性，IC 值分别为 10 µg 和 130 µg。这两个部分都表现出剂量依赖性毒性，在 0.5 g 或更高剂量下引起呕吐，在 3-5 g 或更高剂量下引起昏睡和死亡。同样，这两个部分在甲硝唑和洛哌丁胺诱导的便秘模型中均表现出通便活性。EAC 在较低剂量（1 mg/mL）下使肠平滑肌松弛，而 DCMC 则在较高剂量（1 mg/mL）下使肠平滑肌松弛。同样，与 DCMC 相比，EAC 提取物在兔空肠的 KCL 诱导收缩中显示出显著的松弛作用（EC = 0.67 ± 0.15 mg/mL）（EC = 5.04 ± 0.05 mg/kg）。本研究强烈支持民间传说，即这种有价值的植物是一种泻药。需要进一步的工作来分离和验证作为腹泻剂的生物活性化合物
