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Synthesized 2-trifluoromethylquinazolines and quinazolinones protect BV2 and N2a cells against LPS- and H2O2-induced cytotoxicityNallathamby, Neeranjini ...Background: Microglia are associated with neuroinflammation, which plays a key role in the pathogenesis of neurodegenerative diseases. It has been reported that some quinazolines and quinazolinones ... possess anti-inflammatory properties. However, the pharmacological properties of certain quinazoline derivatives are still unknown. Objective: The antioxidant, cytotoxic, and protective effects of a series of synthesized 2-trifluoromethylquinazolines (2, 4, and 5) and quinazolinones (6-8) in lipopolysaccharide (LPS)-murine microglia (BV2) and hydrogen peroxide (H2O2)-mouse neuroblastoma-2a (N2a) cells were investigated. Method: The antioxidant activity of synthesized compounds was evaluated with ABTS and DPPH assays. The cytotoxic activities were determined by MTS assay in BV2 and N2a cells. The production of nitric oxide (NO) in LPS-induced BV2 microglia cells was quantified. Results: The highest ABTS and DPPH scavenging activities were observed for compound 8 with 87.7% of ABTS scavenge percentage and 54.2% DPPH inhibition. All compounds were non-cytotoxic in BV2 and N2a cells at 5 and 50 [micro]g/mL. The compounds which showed the highest protective effects in LPS-induced BV2 and H2O2-induced N2a cells were 5 and 7. All tested compounds, except 4, also reduced NO production at concentrations of 50 [micro]g/mL. The quinazolinone series 6-8 exhibited the highest percentage of NO reduction, ranging from 38 to 60%. Compounds 5 and 8 possess balanced antioxidant and protective properties against LPS- and H2O2-induced cell death, thus showing great potential to be developed into anti-inflammatory and neuroprotective agents. Conclusion: Compounds 5 and 7 were able to protect the BV2 and N2a cells against LPS and H2O2 toxicity, respectively, at a low concentration (5 [micro]g/mL). Compounds 6-8 showed potent reduction of NO production in BV2 cells.Vir: Medicinal chemistry. - ISSN 1573-4064 (Vol. 17, iss. 6, 2021, str. 623-629)Vrsta gradiva - članek, sestavni delLeto - 2021Jezik - angleškiCOBISS.SI-ID - 4882545
Avtor
Nallathamby, Neeranjini |
Phan, Chia-Wei |
Sova, Matej, 1979- |
Saso, Luciano |
Sabaratnam, Vikineswary
Teme
antioxidant |
anti-inflammatory |
neuroprotection |
quinazolines |
Quinazolinones |
BV2 |
N2a
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Nallathamby, Neeranjini | ![]() |
Phan, Chia-Wei | ![]() |
Sova, Matej, 1979- | 25490 |
Saso, Luciano | ![]() |
Sabaratnam, Vikineswary | ![]() |
Vir: Osebne bibliografije
in: SICRIS
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