Agbaje E O
Department of Pharmacology, College of Medicine, University o Lagos P. M. B. 12003, Idi-araba, Lagos, Nigeria.
Nig Q J Hosp Med. 2008 Jul-Sep;18(3):137-41. doi: 10.4314/nqjhm.v18i3.45015.
Gastrointestinal disorders constitute one of the most common diseases world-wide and the treatment of some of them has since constituted a great challenge to health workers, which therefore calls for an urgent search into newer agents. In recent years, several efforts have been made through series of investigations on natural resources.
The plant Syzigium aromaticum (SYZ), commonly known as clove has since been employed locally to treat constipation. Attempt to complement the effort of other researchers called for its selection for laboratory investigation, in order to determine its possible effect on intestinal propulsion in rodents as well as its suspected gastrointestinal protective properties.
SYZ hot aqueous extract was investigated using selected doses in the various study models. Effect of the decoction on intestinal propulsion was studied by administering 300 and 700 mg kg(-1) hot extract to groups of overnight fasted mice, while using charcoal meal as a marker. The effect of the herbal drug was compared with other standard drugs and antagonists. In the same vein, the same doses of the extract were administered orally to groups of overnight fasted rats prior to challenge with different necrotizing agents-absolute ethanol (1 ml/rat), indomethacin (30 mg kg(-1)) and 70% ethanol in 150 mM HCl (1 ml/rat). Both negative and positive controls were similarly treated simultaneously with distilled water (10 ml kg(-1)) and standard antiulcer drugs (omeprazole 20.0 mg kg(-1), cimetidine 100.0 mg kg(-1) and misoprostol 0.2 mg kg(-1)), respectively. Lastly, the effect of SYZ was investigated on a segment of isolated rabbit ileum and subsequently compared with acetylcholine 5.5 x 10(-5) M. The effects of atropine (3.4 x 10(-6) M and 3.4 x 10(-5) M) on SYZ were also studied.
The extract was found to increase the gut muscle propulsion similar to the standard drugs-carbachol and metoclopramide. When used together with atropine, SYZ produced a reduction in intestinal propulsion which suggested the involvement of cholinergic mechanisms in the action of the extract. In the ulcer models, the decoction reduced the ulcer number and ulcer area in the ethanol and HCl-ethanol models, with significant respective ulcer indices of 2.80 +/- 3.51 and 11.4 +/- 3.79 compared with controls (p < 0.05). In the indomethacin model, the extract, 700 mg kg(-1), compared favourably with misoprostol with an index of 0.20 +/- 0.11 which was also found to be significant compared with the control. In the in-vitro investigation on the rabbit ileum SYZ (200-6400 microg ml(-1)) contracted the tissue in a dose-dependent fashion but it was found to be less effective than acetylcholine (5.5 x 10(-5) M). Atropine sulphate 3.4 x 10(-6) M and 3.4 x 10(-5) M reduced gut contractility induced by SYZ, similar to the in-vivo observation. The latter could substantiate the earlier speculation of the herbal drug exerting its effect via cholinergic mechanism apart from the diverse possible activities of the various bioactive components that were identified through phytochemical testing of SYZ.
The present findings explain the folkloric uses of SYZ as an antiulcer and a purgative agent as well as its possible mechanism of action.
胃肠道疾病是全球最常见的疾病之一,其中一些疾病的治疗对医护人员构成了巨大挑战,因此迫切需要寻找新的药物。近年来,通过对自然资源的一系列研究已经做出了一些努力。
植物丁香(Syzygium aromaticum,SYZ),俗称丁香,在当地一直被用于治疗便秘。为了补充其他研究人员的工作,需要对其进行实验室研究,以确定其对啮齿动物肠道推进的可能影响以及其疑似的胃肠道保护特性。
在各种研究模型中使用选定剂量对SYZ热的水提取物进行研究。通过给禁食过夜的小鼠组灌胃300和700 mg kg⁻¹热提取物,同时使用炭末作为标记物,研究水煎剂对肠道推进的影响。将草药的作用与其他标准药物和拮抗剂进行比较。同样,在给禁食过夜的大鼠组口服相同剂量的提取物后,用不同的坏死剂进行攻击——无水乙醇(1 ml/只大鼠)、吲哚美辛(30 mg kg⁻¹)和150 mM HCl中的70%乙醇(1 ml/只大鼠)。阴性和阳性对照分别用蒸馏水(10 ml kg⁻¹)和标准抗溃疡药物(奥美拉唑20.0 mg kg⁻¹、西咪替丁100.0 mg kg⁻¹和米索前列醇0.2 mg kg⁻¹)同时进行类似处理。最后,研究了SYZ对一段离体兔回肠的作用,并随后与5.5×10⁻⁵ M的乙酰胆碱进行比较。还研究了阿托品(3.4×10⁻⁶ M和3.4×10⁻⁵ M)对SYZ的影响。
发现该提取物能增加肠道肌肉推进,类似于标准药物卡巴胆碱和甲氧氯普胺。当与阿托品一起使用时,SYZ导致肠道推进减少,这表明胆碱能机制参与了提取物的作用。在溃疡模型中,水煎剂在乙醇和盐酸 - 乙醇模型中减少了溃疡数量和溃疡面积,与对照组相比,各自显著的溃疡指数分别为2.80±3.51和11.4±3.79(p < 0.05)。在吲哚美辛模型中,700 mg kg⁻¹的提取物与米索前列醇相比效果良好,指数为0.20±0.11,与对照组相比也具有显著性。在对兔回肠的体外研究中,SYZ(200 - 6400 μg ml⁻¹)以剂量依赖性方式使组织收缩,但发现其效果不如乙酰胆碱(5.5×10⁻⁵ M)。3.4×10⁻⁶ M和3.4×10⁻⁵ M的硫酸阿托品降低了SYZ诱导的肠道收缩性,类似于体内观察结果。后者可以证实之前关于该草药通过胆碱能机制发挥作用的推测,此外,通过对SYZ的植物化学测试鉴定出的各种生物活性成分可能具有多种不同的活性。
目前的研究结果解释了丁香作为抗溃疡和泻药的民间用途及其可能的作用机制。