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Gastroprotective activity of a novel Schiff base derived dibromo substituted compound against ethanol-induced acute gastric lesions in rats.
BMC Pharmacology and Toxicology ( IF 2.8 ) Pub Date : 2019-02-17 , DOI: 10.1186/s40360-019-0292-z
Kamelia Saremi 1 , Sima Kianpour Rad 2 , Faezeh Tayeby 1 , Mahmood A Abdulla 3 , Hamed Karimian 4 , Nazia Abdul Majid 1
Affiliation  

BACKGROUND Basic function of bromine in body is to activate pepsin production in gastritis with low acidity. The present study encompasses a broad in vivo study to evaluate gastroprotective activity of a novel dibromo substituted Schiff base complex against Sprague Dawley (SD) rats. METHODS 2, 2'-[1, 2-cyclohexanediylbis (nitriloethylidyne)]bis(4-bromophenol) (CNBP) is synthesized via a Schiff base reaction, using the related ketone and diamine as the starting materials. SD rats are divided as normal, ulcer control (5 ml/kg of 10% Tween 20), testing (10 and 20 mg/kg of CNBP) and reference groups (omeprazole 20 mg/kg). Except for the normal group, the rest of the groups are induced gastric ulcer by ethanol 1 h after the pre-treatment. Ulcer area, gastric wall mucus, and acidity of gastric content of the animal stomachs are measured after euthanization. Antioxidant activity of the compound is tested by Ferric reducing antioxidant power (FRAP) test and safety of the compound is identified through acute toxicity by [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Moreover, activities of superoxide dismutase (SOD), catalase (CAT), levels of prostaglandins E2 (PGE2) and also malondialdehyde (MDA) are determined. RESULTS Antioxidant activity of CNBP was approved via FRAP assay. Vast shallow hemorrhagic injury of gastric glandular mucosa was observed in the ulcer group compared to the CNBP-treated animals. Histological evaluations confirmed stomach epithelial defense effect of CNBP with drastic decrease of gastric ulceration, edema and leucocytes penetration of submucosal stratum. Immunostaining exhibited over-expression in HSP70 protein in CNBP-treated groups compared to that of the ulcer group. Also, gastric protein analysis showed low levels of MDA, PGE2 and high activity of SOD and CAT. CONCLUSIONS CNBP with noticeable antioxidant property showed gastroprotective activity in the testing rodents via alteration of HSP70 protein expression. Also, antioxidant enzyme activities which were changed after treatment with CNBP in the animals could be elucidated as its gastroprotective properties.

中文翻译:

新型席夫碱衍生的二溴取代化合物对大鼠乙醇诱导的急性胃损伤的胃保护作用。

背景技术溴在体内的基本功能是激活低酸度胃炎中胃蛋白酶的产生。本研究包括广泛的体内研究,以评估新型二溴取代的席夫碱复合物对Sprague Dawley(SD)大鼠的胃保护活性。方法2,使用相关的酮和二胺作为起始原料,通过席夫碱反应合成了2,2'-[1,2-环己烷二基双(亚硝基乙二炔)]双(4-溴苯酚)(CNBP)。将SD大鼠分为正常组,溃疡对照组(5ml / kg的10%Tween 20),测试组(10和20mg / kg的CNBP)和参考组(奥美拉唑20mg / kg)。除正常组外,其余各组均在预处理1 h后被乙醇诱发胃溃疡。溃疡部位,胃壁粘液,安乐死后测量动物胃中胃内容物的酸度和酸度。通过三价铁还原抗氧化剂能力(FRAP)测试来测试该化合物的抗氧化活性,并通过[3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四唑溴化物(MTT)的急性毒性来确定该化合物的安全性)分析。此外,确定了超氧化物歧化酶(SOD),过氧化氢酶(CAT),前列腺素E2(PGE2)和丙二醛(MDA)的活性。结果CNBP的抗氧化活性已通过FRAP测定得到认可。与CNBP治疗的动物相比,在溃疡组中观察到胃腺粘膜的巨大浅层出血性损伤。组织学评估证实了CNBP的胃上皮防御作用,并显着降低了胃溃疡,水肿和粘膜下层白细胞渗透。与溃疡组相比,在CNBP治疗组中免疫染色显示HSP70蛋白过表达。此外,胃蛋白分析显示MDA,PGE2含量低,SOD和CAT活性高。结论具有明显抗氧化作用的CNBP通过改变HSP70蛋白的表达在测试啮齿类动物中具有胃保护作用。同样,可以阐明在用CNBP处理后在动物中改变的抗氧化酶活性作为其胃保护性质。结论具有明显抗氧化作用的CNBP通过改变HSP70蛋白的表达在测试啮齿类动物中具有胃保护作用。同样,可以阐明在用CNBP处理后在动物中改变的抗氧化酶活性作为其胃保护性质。结论CNBP具有显着的抗氧化性能,通过改变HSP70蛋白表达,在测试啮齿动物中具有胃保护作用。同样,可以阐明在用CNBP处理后在动物中改变的抗氧化酶活性作为其胃保护性质。
更新日期:2019-11-01
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