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.author | Egunlusi, Ayodeji O. | |
| dc.contributor.author | Malan, Sarel F. | |
| dc.contributor.author | Omoruyi, Sylvester Ifeanyi | |
| dc.date.accessioned | 2021-01-28T07:23:42Z | |
| dc.date.available | 2021-01-28T07:23:42Z | |
| dc.date.issued | 2020 | |
| dc.description.abstract | The 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.citation | Egunlusi, 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),4552 | en_US |
| dc.identifier.issn | 1420-3049 | |
| dc.identifier.uri | 10.3390/molecules25194552 | |
| dc.identifier.uri | http://hdl.handle.net/10566/5783 | |
| dc.language.iso | en | en_US |
| dc.publisher | MPDI | en_US |
| dc.subject | Cytotoxicity | en_US |
| dc.subject | Neurodegenerative disorders | en_US |
| dc.subject | Neuroprotection | en_US |
| dc.subject | Polycyclic cages | en_US |
| dc.subject | Voltage gated calcium channels | en_US |
| dc.title | 4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives as nmda receptor- And VGCC blockers with neuroprotective potential | en_US |
| dc.type | Article | en_US |