Department of Biology, Faculty of Applied Science, University Teknologi MARA, Shah Alam 40450, Malaysia.
Molecules. 2012 Aug 3;17(8):9306-20. doi: 10.3390/molecules17089306.
Indolic compounds have attracted a lot of attention due to their interesting biological properties. The present study was performed to evaluate the subacute toxicity and anti-ulcer activity of BClHC against ethanol-induced gastric ulcers. Experimental animal groups were orally pre-treated with different doses of BClHC (50, 100, 200 and 400 mg/kg) in 10% Tween 20 solution (vehicle). Blank and ulcer control groups were pre-treated with vehicle. The positive group was orally pretreated with 20 mg/kg omeprazole. After one hour, all groups received absolute ethanol (5 mL/kg) to generate gastric mucosal injury except the blank control group which was administered the vehicle solution. After an additional hour, all rats were sacrificed, and the ulcer areas of the gastric walls determined. Grossly, the ulcer control group exhibited severe mucosal injury, whereas pre-treatment with either derivative or omeprazole resulted in significant protection of gastric mucosal injury. Flattening of gastric mucosal folds was also observed in rats pretreated with BClHC. Histological studies of the gastric wall of ulcer control group revealed severe damage of gastric mucosa, along with edema and leucocytes infiltration of the submucosal layer compared to rats pre-treated with either BClHC or omeprazole where there were marked gastric protection along with reduction or absence of edema and leucocytes infiltration of the submucosal layer. Subacute toxicity study with a higher dose of derivative (5 g/kg) did not manifest any toxicological signs in rats. In conclusions, the present finding suggests that benzyl N'-(5-chloroindol-3-ylmethylidene)hydrazinecarbodithioate promotes ulcer protection as ascertained by the comparative decreases in ulcer areas, reduction of edema and leucocytes infiltration of the submucosal layer.
吲哚类化合物因其有趣的生物特性而引起了广泛关注。本研究旨在评估 BClHC 对乙醇诱导的胃溃疡的亚急性毒性和抗溃疡活性。实验动物组分别用不同剂量的 BClHC(50、100、200 和 400mg/kg)在 10%吐温 20 溶液(载体)中进行口服预处理。空白和溃疡对照组用载体预处理。阳性对照组用 20mg/kg 奥美拉唑进行口服预处理。一小时后,除空白对照组给予载体溶液外,所有组均给予 5mL/kg 绝对乙醇以产生胃黏膜损伤。额外一小时后,所有大鼠均被处死,并确定胃壁的溃疡面积。大体上,溃疡对照组表现出严重的黏膜损伤,而用衍生物或奥美拉唑预处理则显著保护胃黏膜免受损伤。用 BClHC 预处理的大鼠胃黏膜褶皱也变平。与用 BClHC 或奥美拉唑预处理的大鼠相比,溃疡对照组的胃壁组织学研究显示胃黏膜严重损伤,伴有黏膜下层水肿和白细胞浸润。亚急性毒性研究中,用更高剂量的衍生物(5g/kg)处理的大鼠没有表现出任何毒理学迹象。总之,本研究结果表明,苄基 N'-(5-氯吲哚-3-基甲基亚肼基)二硫代甲酰胺通过比较减少溃疡面积、减少水肿和白细胞浸润黏膜下层来促进溃疡保护。