Abstract
A series of new 2-(ethylthio)benzohydrazone derivatives (1–6) were prepared and characterised by IR, 1H NMR, and 13C NMR spectroscopy and mass spectrometry. The newly prepared compounds were screened for their in vitro antioxidant activities using free radical scavenging 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) assays. Among them, most powerful antioxidant, compound 1 has been selected in order to illustrate anti-ulcer effect on ethanol-induced gastric mucosal lesions in rats. Four groups of Sprague Dawley rats were respectively treated with 10% Tween 20 as ulcer control group, 20 mg/kg omeprazole as reference group, 50 mg/kg and 100 mg/kg compound 1 as experimental animals. Macroscopically, ulcer control group showed extensive hemorrhagic lesions of gastric mucosa compared with omeprazole or compound 1. Rats pre-treated with compound 1 showed increased in gastric pH and gastric mucus. Histologically, ulcer control group showed severe damage to gastric mucosa with edema and leucocytes infiltration of submucosal layer. In immunohistochemical analysis, rats which were pre-treated with compound 1 showed up-regulation of HSP70 and down-regulation of Bax proteins. In conclusion, the gastroprotective effect of compound 1 may be due to its antioxidant activity, and/or due to up-regulation of HSP70 and down-regulation of Bax protein in stained tissue section.
Highlights
Reactive oxygen species (ROS) and free radicals such as superoxide anion radical, hydroxyl radicals, and lipid peroxides are the injurious species known to cause many degenerativePLOS ONE | DOI:10.1371/journal.pone.0156022 June 7, 2016Antioxidant and Gastroprotective Effects diseases [1]
It was thought that stress is one of the etiological factors in the incidence of gastric ulcer by increasing catecholamine levels leading to vasoconstriction [5]
Our study shows that there are up regulation of HSP70 expression in the gastric tissues of rats pre-treated with compound 1 and omeprazole in ethanol-induced gastric ulcer, presumably due to antioxidant effect of compound 1 and omeprazole to attenuate the oxidative damage of ethanol
Summary
Reactive oxygen species (ROS) and free radicals such as superoxide anion radical, hydroxyl radicals, and lipid peroxides are the injurious species known to cause many degenerativePLOS ONE | DOI:10.1371/journal.pone.0156022 June 7, 2016Antioxidant and Gastroprotective Effects diseases [1]. Schiff base compounds have received much attention in the field of chemistry and biology due to their broad range of biological activities such as antibacterial [9], anti-inflammatory [10], antioxidant and antigastric ulcer properties [11]. The attachment of hydroxyl groups on the aromatic ring makes hydroxyl substituted Schiff bases the effective antioxidants, has been and potential drugs for the prevention of diseases due to free radical damage [12]. It is demonstrated that many drugs and formulations possess potent antioxidant action and are effective in healing the experimentally-induced gastric ulcers [13,14,15,16,17]. The most powerful antioxidant Schiff base, whether through hydrogen or electron transfer mechanisms, will be selected in order to illustrate its anti-ulcer effect on ethanol-induced gastric mucosal lesions in rats
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