Abstract

Purpose: N-halamines were known for their antimicrobial action due to the presence of halogen in their structure. In our search for new anti-cancer agents, we have evaluated the anti-cancer and anti-oxidant properties of some synthetic N-Halamines with high and low molecular weight in comparison with their non-halogenated forms. Urea epichlorohydrin copolymer (1), 4(1H, 3H-2, 6-dioxo-1, 3, 5-trizenyl)-O-iminomethylpolyethylene (3) and cynuric acid (5) in addition to their halogenated forms 2, 4 and 6 were selected for this study. Methodology: the toxicity for the synthesized compounds was determined. The anti-cancer and anti-oxidant activities were studied by evaluation the viability of tumor cells, life span prolongation, and estimation of antioxidants, and effects of these compounds on liver histology. Findings: Doses up to 2000 mg/kg indicated good safety in all investigated compounds. In Vivo antitumor activity results against Ehrlich ascites carcinoma (EAC) cells for the investigated compounds revealed that, the volume of ascites was significantly decreased in compounds 1, 2, 3, 4, 5 and 6 treated groups. EAC cell count was significantly reduced for similar groups, respectively, compared to the positive control group. Malonadildehyde, and nitric oxide showed a significant reduction in their levels in the treated groups, while catalase showed a significant elevation in its activity in the same groups compared to positive control group. Conclusion: Halogenated compounds showed good anti-oxidant behavior while compound 6 showed the best anti-tumor effect.

Highlights

  • Cancer is a group of diseases that cause cells in the body to change and grow out of control (American Cancer Society, 2016)

  • Determination of median lethal dose (LD50) The acute toxicity LD50 was estimated by I.P. injection of compounds 1, 2, 3, 4, 5 and 6; doses up to 2000 mg /kg indicated safety in all polymers. 3.2

  • It was cleared that 10 mg/kg was found to be the most effective dose of compounds 1, 2, and 5; while; 5 mg/kg was found to be the most effective dose of compounds 3, 4, and 6; as this dose reduced the number of Ehrlich ascites carcinoma (EAC) cells compared to positive control group at twice I.P. injection, Figure 1

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Summary

Introduction

Cancer is a group of diseases that cause cells in the body to change and grow out of control (American Cancer Society, 2016). Cancer is considered one of the major causes of mortality in the world. Despite the recent advances in science, cancer has not been cured yet. It is estimated that by 2020 there will be 16 million new cancer cases every year (Devegowda et al, 2010). Some significant progress has been made to understand the pharmacological and chemical properties in this approach to provide more details which may improve and establish proper strategies to prevent cancer. The non-selectivity and acute toxicity of many antitumor agents have been the major deterrent in their usage for treating human cancer, prompting the search for new chemo-preventive and antitumor agents with improved tumor selectivity, efficiency and safety (Musa et al, 2011)

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