首页|冬凌草甲素对海马CA1星形胶质细胞P2X7受体电流的影响

冬凌草甲素对海马CA1星形胶质细胞P2X7受体电流的影响

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目的:探索冬凌草甲素是否对海马CA1星形胶质细胞P2X7受体电流有影响.方法:采用Autodock软件对冬凌草甲素与P2X7蛋白进行分子对接;采用全细胞膜片钳记录冬凌草甲素对海马CA1星形胶质细胞P2X7受体激动剂Bz-ATP激发电流的影响.结果:冬凌草甲素与P2X7蛋白的结合能为-5.86 kcal/mol,可与P2X7蛋白的Lys592残基形成氢键,与Tyr550残基形成疏水作用;Bz-ATP能激发海马CA1区星形胶质细胞的电流反应,且1 000 µmol/L Bz-ATP激发的电流反应较强;10 μmol/L冬凌草甲素溶液孵育1 h后,海马CA1区星形胶质细胞对谷氨酸能受体激动剂NMDA和AMPA溶液的电流反应无明显变化;对Bz-ATP的电流反应降低,差异具有统计学意义(P<0.05).结论:冬凌草甲素可与P2X7蛋白对接形成稳定的复合物,具有较好的亲和力;冬凌草甲素可抑制海马CA1星形胶质细胞P2X7受体电流.
Effect of Oridonin on P2X7 Receptor Agonist-induced Current Response in Hippocampal CA1 Astrocytes
Objective:To explore whether oridonin has an effect on P2X7 receptor agonist-induced current in hippocampal CA1 astro-cytes.Methods:Autodock software wasused to perform molecular docking between oridonin and P2X7 protein;whole cell patch clamp to record the effect of oridonin on P2X7 receptor agonist Bz-ATP induced current responseof hippocampal CA1 astrocytes.Results:The binding energy between oridonin and P2X7 protein is-5.86 kcal/mol,which can form hydrogen bonds with the Lys592 residue of P2X7 protein and hydrophobic interactions with Tyr550 residue.Bz-ATP could stimulate a current response of astrocytes in the CA1 region of hippocampus,and the current response stimulated by 1000 pmol/L Bz-ATP is much stronger.1 hour of incubation with 10 p,mol/L oridonin solution decreased Bz-ATP induced current response of astrocyte significantly(P<0.05),while glutamate receptor agonists NMDA and AMPA have no influence on that.Conclusion:oridonin can dock with P2X7 protein to form a stable complex with good af-finity,and inhibit P2X7 receptor agonist Bz-ATP induced current response in hippocampal CA1 astrocytes.

OridoninP2X7 receptorMolecular dockingPatch clampHippocampal astrocytes

赵亚飞、吴嘉思、童宇、睢婉婉、时政

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成都中医药大学针灸推拿学院,四川成都 611137

成都大学临床医学院/成都大学附属医院,四川成都 610106

冬凌草甲素 P2X7受体 分子对接 膜片钳 海马星形胶质细胞

中国博士后科学基金中国博士后科学基金成都大学附属医院院级项目成都大学附属医院院级项目成都大学附属医院院级项目成都大学临床医学院/附属医院创新团队项目

BX202200492022MD713682Y2021006Y202232Y202234CDFYCX202208

2024

成都中医药大学学报
成都中医药大学

成都中医药大学学报

影响因子:0.572
ISSN:1004-0668
年,卷(期):2024.47(3)
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