engleski

CYTOTOXICITY OF FLUORESCENT BENZIMIDAZOLE CORE COMPOUNDS

Background: Benzimidazoles are heterocyclic aromatic organic compounds, which consist of the fusion of benzene and imidazole. Various biological actions have been identified for this class of compounds, such as antineoplastic, antimicrobial and anti-inflammatory. The in vitro cellular toxicity of biologically active compounds is a preclinical approach that definesthe therapeutic window ofdrugs. Therefore, we evaluated the in vitro cytotoxicity of six fluorescent benzimidazole core compounds (NB2, NB5, NB6, NB7, NB8, NB9), using a mitochondrial assay based on the reduction of MTT. Methods: VERO cells were cultured in DMEM supplemented with 10% fetal bovine serum (conventional medium) at 37°C in a humid atmosphere with 5% CO2. Cell cultures at 80% confluence were exposed for 72h to 0.001, 0.01, 0.1, 1.0, 10 and 100 μM of each of the six compounds. Untreated cells maintained in conventional medium were used as negative control (100% viable cells). After the incubation time, the MTT assay was performed and the cytotoxic concentrationfor 50% of the cells (CC50) was calculated from the polynomial equation of the dose-response pattern. Results: All concentration versus cell viability curves obtained exhibit a concentration dependent profile. Taking into consideration the maximum concentration evaluated (100 μM) and the CC50 of each compound, NB5 (97%), NB7 (100%) and NB8 (100%) showed the highest cytotoxicity’s. NB2 and NB9 showed 54% and 72% of cytotoxicity, respectively, while NB6 was the least toxic compound with around 75% of viable cells remaining. The CC50 concentrations of the NB compounds were between 20 μM (NB8) and 2.35μM (NB6). Interestingly, increased mitochondrial activities of up to 25% were determined below 1.0 μM. Conclusions: This study demonstrates that the benzimidazole compound NB6 is the least toxic one and may be tested in a broader therapeutic window to evaluate its biological action like antiviral, antibacterial or antifungal.

in vitro toxicity ; cell viability ; MTT, benzimidazole analogs

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