Study of antidiabetic activity of two novel Schiff base derived dibromo and dichloro substituted compounds in streptozotocin-nicotinamide-induced diabetic rats: pilot study

Schiff bases are aldehyde-or ketone-like chemical compounds in which an imine or azomethine group replaces the carbonyl group. Such compounds show various beneficial biological activities, such as anti-inflammation and antioxidants. The present study addresses comprehensiveevaluation of antidiabetic effect of two novel dibromides and dichlorides substituted Schiff bases substituted Schiff bases (2,2'-[1,2-cyclohexanediylbis (nitriloethylidyne)]bis[4-chlorophenol] (CNCP) and 2, 2'-[1,2-cyclohexanediylbis(nitriloethylidyne)]bis[4-bromophenol] (CNBP) with two different doses, high (LD) and low (LD) in streptozotocin and nicotinamide induced diabetic rats. The rats were separated into normal, untreated, treated and reference groups. Except for the normal group, diabetes traits were induced in the rest animals. Insulin level was measured, and the effect of the compounds on biochemical parameters of liver function and lipid profile were evaluated. High glucose and decreased insulin level are observed in the groups. The histological evaluation confirms that the hepatic architecture in the treated animals with a low dose of CNCP is quite similar to that of the normal hepatic structure and characterized by normal central vein, hepatocytes without any fatty alterations and mild red blood cell infiltration. CNCP (LD) and CNBP (HD) are more successful in enhancing cell survival in the diabetic rat’s liver and can be responsible for causing much healthier structure and notable morphology improvement

In vivo evaluation of wound healing improvement of a new Schiff base derived bromine compound (CNBP) in rats

Background: The effect of delivered bromine vapor and also bromine substitutions are shown to play an important role in anti-inflammatory activity. The present study encompasses a broad in vivo study to size up healing activity of a novel dibromide substituted Schiff based compound against cutaneous wound model in Sprague Dawley (SD) rats. Methodology/principal findings: 2, 2′-[1, 2-Cyclohexanediylbis(nitriloethylidyne)] bis[4-bromophenol], CNBP, is synthesized through a Schiff base reaction applying the related ketone and diamine as the initiators. Four groups of six in each male SD rats are divided as negative group which are treated with gum acacia, positive control animals which are treated with topical dosage of Intrasite gel, and testing groups treated with low (10 mg/kg) and high (20 mg/kg) doses of CNBP. The excisional wounds are created on the posterior neck area of each group and the wound closure percentage was measured in the two separated days of the experiment. Moreover, the histopathological evaluation and determination of activities of superoxide dismutase (SOD), catalase (CAT), peroxidase (GPx), and malondialdehyde (MDA) of the skin sections are performed. Furthermore, the immunohistochemistry consists of the evaluation of Hsp70 and BAX proteins. Conclusions/significance: The wound closure percentage showed a significant increase in high dose CNBP-treated group compared to the negative control. Histopathological evaluation of the skin sections showed that granulation tissue contained more proliferating fibroblast, collagen deposition, angiogenesis, and also less inflammatory cells in the high dose CNBP-treated group compared to the normal rats. In the treated groups with CNBP, SOD, CAT, and GPx activities were found significantly higher, however, the MDA level was shown to be lower (*P < 0.05; **P < 0.01; ***P < 0.001) than the negative control. At the molecular level, CNBP (20 mg/ml, HD) improved wound-healing process via down and up regulation of Bax and Hsp70 protein, respectively at the wound site. © 201

Gastroprotective activity of a novel Schiff base derived dibromo substituted compound against ethanol-induced acute gastric lesions in rats

Abstract 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