Abstract

PROTECTIVE ACTION OF THE GENISTEIN DERIVATIVE IN GASTRIC ULCER PREVENTION INDUCED BY ETHANOL IN RATS

Quan-Cheng Zhou, Gui-Hua Sheng, Xiang-Fei Chen, Na Liu, Chuan-Xing Feng,Guang-Yao Zhang, Xiao-Yu Yang, Hai-Liang Zhu

ABSTRACT

Aim: In the present study, a genistein derivative (GD) was firstly synthesized and evaluated for antigastric ulcer activity in vivo and investigated the possible mechanisms underlying the anti-ulcerogenic effects of GD. Materials and methods: GD was synthesized through genistein with phenylpiperazine, and was analyzed through 1H-NMR and element analysis. GD was subjected to assess acute oral toxicity study of animal model, and evaluate the protective effect of ethanolinduced gastric damage in rat model. Ulcer index value, NOx, GSH/GSSG ratio, CAT, SOD, MPO activity, IL-6, IL-10 and PEG2 were also determined in the stomach tissues or blood serum. Results: GD has no acute oral toxicity. GD (equivalent to 0.45, 4.5 and 45 mg/kg) dose-dependently reduced the gastric ulcer index, significantly decreased the NOx, GSH/GSSG ratio, CAT activity and IL-6, and increase SOD, MPO activity, IL-10, PEG2 and. Conclusion: GD possesses an enhanced mucosal barrier defense activity. Their possible mechanism of action was discussed and due to their many positive properties including antioxidant, antiinflammatory and gastroprotective activities might represent a cost effective alternative sought for in the treatment of gastric ulcers. Based on the results, we suggest that GD has potential to provide a therapeutic approach to ethanol mediated ulcer as an effective antiulcer agent.

Keywords: genistein, phenylpiperazine, synthesis, gastric ulcer, derivative, prevention.