Evaluation of anti-motility and anti-secretory effects of Annona muricata leaves extract in castor oil-induced diarrhoeic rats

Ndidiamaka H. Okorie , Cyril C. Adonu , Charles O. Nnadi
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Abstract

Diarrhoea is a debilitating gastrointestinal disorder commonly affecting all age groups in the developing world due to lifestyle, hygiene and environmental factors. Most drugs used in the treatment of this disease have side effects and are out of reach in many rural areas. Hence a need to search for more tolerable, affordable and effective anti-diarrhoeal drugs from medicinal plants. The study evaluated the anti-motility and anti-secretory properties and phytochemical constituents of the leaves of Annona muricata. The dried coarse leaves were cold-macerated in methanol (95%v/v) and the resulting extract partitioned successively in n-hexane, ethyl acetate, n-butanol and water to afford their respective fractions using the solvent partition method. Phytochemical screening was conducted using standard methods while acute toxicity of the extract was carried out by the method of Lorke. The anti-motility and antisecretory studies were evaluated using the castor oil-induced diarrhea model in experimental rats. The extraction of the leaves and fractionation of methanol extract yielded 3.5%w/w of the extract and 0.46, 1.45, 0.62 and 0.62%w/w of the n-hexane, ethyl acetate n-butanol and aqueous partitions respectively. The acute toxicity study indicated that there were no unusual behavioural changes and mortality at an administered dose of 5000 mg of extract per kg of mice. The extract (200 and 400 mg/kg) exhibited non-dose-dependent anti-diarrheal activity. The extract and its ethyl acetate fraction (200 and 400 mg/kg) elicited a significant anti-motility activity (p < 0.05) compared to untreated. Pre-treatment of rats with ethyl acetate fraction (400 mg/kg) significantly inhibited the action of carbachol on gastric emptying (82.0 ± 5.0% vs. 28.1 ± 8.2%),) and gastrointestinal transit (83.5 ± 7.6%, vs 30.10 ± 5.2%) but with no significant effect on the actions of serotonin and metoclopramide. The extract and ethyl acetate fraction of A. muricata demonstrated a significant anti-motility activity which could be mediated by the anticholinergic effect of its phytoconstituents.
蓖麻油致腹泻大鼠抗运动和抗分泌作用的评价
由于生活方式、卫生和环境因素,腹泻是一种使人衰弱的胃肠道疾病,通常影响发展中国家所有年龄组。用于治疗这种疾病的大多数药物都有副作用,而且在许多农村地区遥不可及。因此,需要从药用植物中寻找更容易耐受、负担得起和有效的抗腹泻药物。本研究对村野番荔枝叶片的抗运动、抗分泌特性及植物化学成分进行了研究。将干燥后的粗叶用95%v/v的甲醇冷浸,提取液依次用正己烷、乙酸乙酯、正丁醇和水进行分馏,得到相应的溶剂分馏法。采用标准方法进行植物化学筛选,采用洛克法进行急性毒性试验。采用蓖麻油致腹泻大鼠模型,观察其抗运动和抗分泌作用。叶的提取和甲醇的分馏,提取液的w/w分别为3.5%,正己烷、乙酸乙酯、正丁醇和水馏分的w/w分别为0.46%、1.45%、0.62%和0.62%。急性毒性研究表明,给药剂量为每公斤5000毫克提取物的小鼠没有异常的行为变化和死亡。提取物(200和400 mg/kg)表现出非剂量依赖性的抗腹泻活性。提取物及其乙酸乙酯组分(200和400 mg/kg)均具有显著的抗运动活性(p <;0.05)。乙酸乙酯部分(400 mg/kg)预处理能显著抑制卡巴酚对大鼠胃排空(82.0±5.0% vs 28.1±8.2%)和胃肠道转运(83.5±7.6% vs 30.10±5.2%)的作用,但对血清素和甲氧氯普胺的作用无显著影响。木犀草提取物和乙酸乙酯部位具有明显的抗运动活性,其机制可能与木犀草的抗胆碱能作用有关。
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