Abstract
The compound dichlorido-copper(II)-4-(2-5-bromobenzylideneamino)ethyl) piperazin-1-ium phenolate (CuLBS) was synthesized, characterized and screened for acute toxicity and protective activity against ethanol-induced gastric mucosal injury in rats. Gross microscopic lesions, biochemical and immunological parameters and histochemcial staining of glycogen storage were taken into consideration. Oral administration of CuLBS (30 and 60 mg/Kg) for two weeks dose-dependently flattened gastric mucosa, significantly increased gastric mucus and total acidity, compared with control group (P < 0.01). Serum levels of liver enzymes aspartate (AST) and alanine transaminases (ALT), pro-inflammatory (IL-6 and TNF-α) and anti-inflammatory (IL-10) cytokines in the rats exposed to ethanol induced ulceration have been altered. Administration of CuLBS showed considerable (P < 0.05) protection against ulceration by modulating the acute alterations of cytokines AST, ALT and stomach glycogen. Interestingly, CuLBS did not interfere with the natural release of nitric oxide. CuLBS alone (60 mg/Kg) did not exhibit any ulcerogenic effect as assessed using Adami’s scoring scale. An acute toxicity study showed that rats treated with CuLBS (1,000 and 2,000 mg/Kg) manifested no abnormal signs. These findings therefore, suggested that the gastroprotective activity of CuLBS might contribute in modulating the inflammatory cytokine-mediated oxidative damage to gastric mucosa.
Highlights
The inflammation caused by ethanol-induced gastric injuries has become a standard measure for testing the therapeutic potencies of many synthetic compounds
The pathogenesis caused by this ulcer model involved inhibition of the enzyme cyclooxygenase, which in turn suppressed the output of endogenous prostaglandins leading to changes in gastric motility [2]
Piperazine derivatives afford biologically active compounds against enzyme and receptor targets, for example a potent HIV protease inhibitor indinavir that has been approved for use in man or clozapine, an antipsychotic agent that blocks dopamine and potent MC4-receptor, to mention a few examples where a piperazine core has been used as a scaffold to produce biologically active compounds
Summary
The inflammation caused by ethanol-induced gastric injuries has become a standard measure for testing the therapeutic potencies of many synthetic compounds. Piperazine derivatives afford biologically active compounds against enzyme and receptor targets, for example a potent HIV protease inhibitor indinavir that has been approved for use in man or clozapine, an antipsychotic agent that blocks dopamine and potent MC4-receptor, to mention a few examples where a piperazine core has been used as a scaffold to produce biologically active compounds. This makes the piperazine core a privileged motif for drug design [7]. This study aimed to synthesize, characterize and evaluate the copper complex derived from the Schiff base bromosalicylaldimino-ethylpiperazine for acute toxicity and protective activity against ethanol-induced gastric injuries
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