Institute of Biological Sciences, Faculty of Science, University of Malaya.
Department of Chemistry, University of Malaya, Kuala Lumpur, Malaysia.
Int J Med Sci. 2017 Oct 15;14(13):1317-1326. doi: 10.7150/ijms.20984. eCollection 2017.
The newly synthesized, 3,4,5-Trihydroxy-N 0-[(2-methyl-1H-indol-3-yl)-methylidene] benzohydrazide (TIBH), is an indole and gallic acid derivative. The aim of this research investigation was to evaluate the acute toxicity and the ulcer prevention potential of TIBH in HCl/Ethanol-induced gastric ulcer rat model. Six groups of rats were orally received 5ml/kg of vehicle (1 % Carboxy methyl cellulose) for the normal and ulcer control groups each, Omeprazole (20mg/kg) for positive control, 50 mg/kg, 100 mg/kg and 200 mg/kg of TIBH for experimental groups, respectively. After one hour, instead of rats in the normal group which received 5ml/kg of 1% CMC, other groups received 5ml/kg of HCl/Ethanol. All rats were sacrificed after one additional hour. Gastric juice, gastric mucosa, morphologies of gastric ulcers and protein expressions of both control and treatment groups were evaluated. TIBH showed a ulcer prevention potential by increase of the mucus secretion, decrease of the gastric acidity, up-regulation of HSP70 protein, down-regulation of Bax protein, decrease of the lipid peroxidation and the increase of the Superoxide dismutase (SOD) activity in gastric tissue homogenate. Acute toxicity assay exposed valuable information on the safety of this compound. TIBH had a dose dependent ulcer prevention potential against HCl/Ethanol-triggered gastric ulcer.
新合成的 3,4,5-三羟基-N 0-[(2-甲基-1H-吲哚-3-基)-亚甲基]苯甲酰肼（TIBH）是一种吲哚和没食子酸衍生物。本研究旨在评估 TIBH 在 HCl/Ethanol 诱导的胃溃疡大鼠模型中的急性毒性和溃疡预防潜力。六组大鼠分别口服 5ml/kg 的载体（1%羧甲基纤维素）用于正常和溃疡对照组，奥美拉唑（20mg/kg）用于阳性对照组，50mg/kg、100mg/kg 和 200mg/kg 的 TIBH 用于实验组。一小时后，正常组大鼠除接受 5ml/kg 的 1%CMC 外，其余各组均接受 5ml/kg 的 HCl/Ethanol。一小时后，所有大鼠均被处死。评估胃液、胃黏膜、胃溃疡形态以及对照组和治疗组的蛋白质表达。TIBH 通过增加黏液分泌、降低胃酸、上调 HSP70 蛋白、下调 Bax 蛋白、减少脂质过氧化和增加胃组织匀浆中超氧化物歧化酶（SOD）活性，显示出预防溃疡的潜力。急性毒性试验提供了有关该化合物安全性的有价值信息。TIBH 对 HCl/Ethanol 诱导的胃溃疡具有剂量依赖性的预防作用。
