4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives as nmda receptor- And VGCC blockers with neuroprotective potential

dc.contributor.authorEgunlusi, Ayodeji O.
dc.contributor.authorMalan, Sarel F.
dc.contributor.authorOmoruyi, Sylvester Ifeanyi
dc.date.accessioned2021-01-28T07:23:42Z
dc.date.available2021-01-28T07:23:42Z
dc.date.issued2020
dc.description.abstractThe impact of excitotoxicity mediated by N-methyl-D-aspartate (NMDA) receptor overactivation and voltage gated calcium channel (VGCC) depolarization is prominent among the postulated processes involved in the development of neurodegenerative disorders. NGP1-01, a polycyclic amine, has been shown to be neuroprotective through modulation of the NMDA receptor and VGCC, and attenuation of MPP+-induced neurotoxicity. Recently, we reported on the calcium modulating effects of tricycloundecene derivatives, structurally similar to NGP1-01, on the NMDA receptor and VGCC of synaptoneurosomes. In the present study, we investigated novel 4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives for their cytotoxicity, neuroprotective effects via attenuation of MPP+-induced neurotoxicity and calcium influx inhibition abilities through the NMDA receptor and VGCC using neuroblastoma SH-SY5Y cells. All compounds, in general, showed low or no toxicity against neuroblastoma cells at 10-50 μM concentrations. At 10 μM, all compounds significantly attenuated MPP+-induced neurotoxicity as evident by the enhancement in cell viability between 23.05 ± 3.45% to 53.56 ± 9.29%.en_US
dc.identifier.citationEgunlusi, Ayodeji O. et al. (2020). 4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives as nmda receptor- And VGCC blockers with neuroprotective potential. Molecules ,25(19),4552en_US
dc.identifier.issn1420-3049
dc.identifier.uri10.3390/molecules25194552
dc.identifier.urihttp://hdl.handle.net/10566/5783
dc.language.isoenen_US
dc.publisherMPDIen_US
dc.subjectCytotoxicityen_US
dc.subjectNeurodegenerative disordersen_US
dc.subjectNeuroprotectionen_US
dc.subjectPolycyclic cagesen_US
dc.subjectVoltage gated calcium channelsen_US
dc.title4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives as nmda receptor- And VGCC blockers with neuroprotective potentialen_US
dc.typeArticleen_US

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