Antioxidant and neuroprotective activities of selected 2-pyridones: In vitro and in silico study
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2022
Authors
Lunić, TanjaLađarević, Jelena
Mandić, Marija
Veruševski, Vanja
Božić-Nedeljković, Biljana
Mijin, Dušan
Božić, Bojan
Article (Published version)
Metadata
Show full item recordAbstract
Series of twenty-four 2-pyridone derivatives were screened and selected using the antioxidant ABTS assay
in order to find the most prominent compounds for further in vitro and in silico analyses. Seven derivatives with the highest antioxidant activities were selected and evaluated by β-carotene bleaching assay,
where all of the compounds exhibited better activities than standard antioxidant substance, vitamin C.
Furthermore, seven selected 2-pyridones exhibited significant anti-neuroinflammatory activity by reducing the production of pro-inflammatory mediators (ROS, NO, IL-6, and TNF-α) by LPS-stimulated BV2
microglial cells. Moreover, neuroprotective activity in microglia supernatant transfer model system on
SH-SY5Y neuronal cells has been observed. Anti-neuroinflammatory mechanisms of selected 2-pyridones
have been investigated by molecular docking studies of the TLR4 signaling pathway proteins as well as
inducible nitric oxide synthase. The present study suggests that selecte...d 2-pyridone derivatives can alleviate neuroinflammation in microglial cells and protect the surrounding neuronal cells from damage,
which qualifies them for further investigations towards neurodegenerative diseases associated with inflammation.
Keywords:
Pyridone derivatives / Antioxidants / Neuroprotection / Neuroinflammation / Docking studySource:
Journal of Molecular Structure, 2022, 1256, 132546-Publisher:
- Elsevier B.V.
Funding / projects:
- Ministry of Science, Technological Development and Innovation of the Republic of Serbia, institutional funding - 200178 (University of Belgrade, Faculty of Biology) (RS-MESTD-inst-2020-200178)
- Ministry of Science, Technological Development and Innovation of the Republic of Serbia, institutional funding - 200135 (University of Belgrade, Faculty of Technology and Metallurgy) (RS-MESTD-inst-2020-200135)
DOI: 10.1016/j.molstruc.2022.132546
ISSN: 0022-2860
WoS: 00079001080001
Scopus: 2-s2.0-85124298138
Institution/Community
Tehnološko-metalurški fakultetTY - JOUR AU - Lunić, Tanja AU - Lađarević, Jelena AU - Mandić, Marija AU - Veruševski, Vanja AU - Božić-Nedeljković, Biljana AU - Mijin, Dušan AU - Božić, Bojan PY - 2022 UR - http://TechnoRep.tmf.bg.ac.rs/handle/123456789/4728 AB - Series of twenty-four 2-pyridone derivatives were screened and selected using the antioxidant ABTS assay in order to find the most prominent compounds for further in vitro and in silico analyses. Seven derivatives with the highest antioxidant activities were selected and evaluated by β-carotene bleaching assay, where all of the compounds exhibited better activities than standard antioxidant substance, vitamin C. Furthermore, seven selected 2-pyridones exhibited significant anti-neuroinflammatory activity by reducing the production of pro-inflammatory mediators (ROS, NO, IL-6, and TNF-α) by LPS-stimulated BV2 microglial cells. Moreover, neuroprotective activity in microglia supernatant transfer model system on SH-SY5Y neuronal cells has been observed. Anti-neuroinflammatory mechanisms of selected 2-pyridones have been investigated by molecular docking studies of the TLR4 signaling pathway proteins as well as inducible nitric oxide synthase. The present study suggests that selected 2-pyridone derivatives can alleviate neuroinflammation in microglial cells and protect the surrounding neuronal cells from damage, which qualifies them for further investigations towards neurodegenerative diseases associated with inflammation. PB - Elsevier B.V. T2 - Journal of Molecular Structure T1 - Antioxidant and neuroprotective activities of selected 2-pyridones: In vitro and in silico study SP - 132546 VL - 1256 DO - 10.1016/j.molstruc.2022.132546 ER -
@article{ author = "Lunić, Tanja and Lađarević, Jelena and Mandić, Marija and Veruševski, Vanja and Božić-Nedeljković, Biljana and Mijin, Dušan and Božić, Bojan", year = "2022", abstract = "Series of twenty-four 2-pyridone derivatives were screened and selected using the antioxidant ABTS assay in order to find the most prominent compounds for further in vitro and in silico analyses. Seven derivatives with the highest antioxidant activities were selected and evaluated by β-carotene bleaching assay, where all of the compounds exhibited better activities than standard antioxidant substance, vitamin C. Furthermore, seven selected 2-pyridones exhibited significant anti-neuroinflammatory activity by reducing the production of pro-inflammatory mediators (ROS, NO, IL-6, and TNF-α) by LPS-stimulated BV2 microglial cells. Moreover, neuroprotective activity in microglia supernatant transfer model system on SH-SY5Y neuronal cells has been observed. Anti-neuroinflammatory mechanisms of selected 2-pyridones have been investigated by molecular docking studies of the TLR4 signaling pathway proteins as well as inducible nitric oxide synthase. The present study suggests that selected 2-pyridone derivatives can alleviate neuroinflammation in microglial cells and protect the surrounding neuronal cells from damage, which qualifies them for further investigations towards neurodegenerative diseases associated with inflammation.", publisher = "Elsevier B.V.", journal = "Journal of Molecular Structure", title = "Antioxidant and neuroprotective activities of selected 2-pyridones: In vitro and in silico study", pages = "132546", volume = "1256", doi = "10.1016/j.molstruc.2022.132546" }
Lunić, T., Lađarević, J., Mandić, M., Veruševski, V., Božić-Nedeljković, B., Mijin, D.,& Božić, B.. (2022). Antioxidant and neuroprotective activities of selected 2-pyridones: In vitro and in silico study. in Journal of Molecular Structure Elsevier B.V.., 1256, 132546. https://doi.org/10.1016/j.molstruc.2022.132546
Lunić T, Lađarević J, Mandić M, Veruševski V, Božić-Nedeljković B, Mijin D, Božić B. Antioxidant and neuroprotective activities of selected 2-pyridones: In vitro and in silico study. in Journal of Molecular Structure. 2022;1256:132546. doi:10.1016/j.molstruc.2022.132546 .
Lunić, Tanja, Lađarević, Jelena, Mandić, Marija, Veruševski, Vanja, Božić-Nedeljković, Biljana, Mijin, Dušan, Božić, Bojan, "Antioxidant and neuroprotective activities of selected 2-pyridones: In vitro and in silico study" in Journal of Molecular Structure, 1256 (2022):132546, https://doi.org/10.1016/j.molstruc.2022.132546 . .