Comparison of Antimutagenic Activity of Two Benzimidazole Derivatives with (+S9) and without (-S9) Metabolic Activation

Mohamad Asri, Nurbaitie (2020) Comparison of Antimutagenic Activity of Two Benzimidazole Derivatives with (+S9) and without (-S9) Metabolic Activation. [Project Paper] (Submitted)

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Abstract

Antimutagenic activity refers to inhibition of mutation that leads to severe disease such as cancer. Benzimidazole is a heterocyclic aromatic compound which consists of benzene and imidazole that plays various important roles as therapeutic agents such as anti-ulcer, anthelmintic, anti-microbial, anti-viral, anti-inflammatory and analgesic drugs. However, the study of benzimidazole derivatives on cancer is still limited. Objectives: This study aims to evaluate the potential of antimutagenic activity of two benzimidazole derivatives (NN-1-5 and NN-1-7) using Ames test, followed by the comparison of structure-activity relationship (SAR). Methodology: Ames test was carried out by using standard mutagens (sodium azide, 2-nitro-fluorene and 2-aminoanthracene) as mutagenic inducer on two strains of Salmonella typhimurium (TA98 and TA100). The bacteria strains, TA98 and TA100 were used to assess the frameshift mutation and base-pair substitution mutation respectively. Five different concentrations (0.31, 0.63, 1.25, 2.5 and 5.0 mg/plate) of benzimidazole derivatives were tested on both strains in the absence (-S9) and presence (+S9) of metabolic activation. Group treated with PBS only was used as the negative control. Then, data of three independent experiments were analysed using two-way ANOVA and followed by post hoc Tukey’s test, p<0.05 indicate a significant value. It is considered absent/weak, moderate and strong antimutagenic compound if the percentage of mutagenic inhibition are <25%, (25-40%) and >40% respectively. The SAR was analysed based on the antimutagenic activity. Results: The data revealed that the compounds without metabolic activation had a significant (p<0.05) antimutagenic effect with strong antimutagenic activity in TA98 and less to moderate antimutagenic activity in TA100. In contrast, metabolic activation of tested compounds had produced no significant (p>0.05) antimutagenic effect. Conclusion: Both benzimidazoles derivatives had potential as antimutagenic agent specifically on frameshift mutations. However, the compound (NN-1-5) with one hydroxyl groups has a stronger antimutagenic effect as compared to (NN-1-7) with two hydroxyl groups.

Item Type:	Project Paper
Faculty:	Faculty of Medicine and Health Science
Depositing User:	Ms. Nor Safa'aton Saidin
Date Deposited:	23 Aug 2023 00:43
Last Modified:	23 Aug 2023 00:43
URI:	http://psaspb.upm.edu.my/id/eprint/1306

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