[Protective effects of (-)-S.R-daurisoline on neuronal injury in rat primary cortical cultures].
The neuroprotective effects of (-)-S.R-daurisoline on glutamate-induced neurotoxicity were studied in rat primary cortical cultures. The inhibitory effects of (-)-S.R-daurisoline on glutamate-elicited free intracellular Ca2+ increase were also studied in freshly dissociated single brain cells isolated from new born rat using AR-CM-MIC Cation Measurement System. Our experimental results demonstrated that (-)-S.R-daurisoline could obviously inhibit the neurotoxicity induced by glutamate and significantly increased cell viability in dose-dependent manner. In inhibiting glutamate-induced neurotoxicity, the IC50 value of (-)-S.R-daurisoline was found to be 3.4 mumol.L-1. (-)-S.R-daurisoline was also shown to markedly inhibit glutamate-elicited increase of cytosolic free Ca2+ concentration in dose-dependent manner with IC50 value of 2.0 mumol.L-1. Our results showed that (-)-S.R-daurisoline has an obvious protective effect on glutamate-induced neurotoxicity in primary cortical cultures. The protective mechanism of (-)-S.R-daurisoline may be relevant to inhibit Ca2+ influx into cells via glutamate-mediated ligand-gated ion channels.
Liu
J
J
Department of Pharmacology, China Pharmaceutical University, Nanjing 210009.
Li
R
R
Liu
G
G
Wang
J
J
D000470:Alkaloids / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D000831:Animals, Newborn; D044182:Benzylisoquinolines; D001693:Biological Transport, Active / Q000187:drug effects; D002118:Calcium / Q000378:metabolism*; D002121:Calcium Channel Blockers / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D002540:Cerebral Cortex / Q000378:metabolism* / Q000473:pathology; D018698:Glutamic Acid; D009474:Neurons / Q000378:metabolism; D018696:Neuroprotective Agents / Q000494:pharmacology*; D051381:Rats; D013237:Stereoisomerism
D000470:Alkaloids; D044182:Benzylisoquinolines; D002121:Calcium Channel Blockers; D018696:Neuroprotective Agents; D018698:Glutamic Acid; C023968:daurisoline; D002118:Calcium