冬凌草甲素对海马CA1星形胶质细胞P2X7受体电流的影响
Effect of Oridonin on P2X7 Receptor Agonist-induced Current Response in Hippocampal CA1 Astrocytes
赵亚飞 1吴嘉思 1童宇 2睢婉婉 2时政2
作者信息
- 1. 成都中医药大学针灸推拿学院,四川成都 611137
- 2. 成都大学临床医学院/成都大学附属医院,四川成都 610106
- 折叠
摘要
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.
Abstract
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.
关键词
冬凌草甲素/P2X7受体/分子对接/膜片钳/海马星形胶质细胞Key words
Oridonin/P2X7 receptor/Molecular docking/Patch clamp/Hippocampal astrocytes引用本文复制引用
基金项目
中国博士后科学基金(BX20220049)
中国博士后科学基金(2022MD713682)
成都大学附属医院院级项目(Y2021006)
成都大学附属医院院级项目(Y202232)
成都大学附属医院院级项目(Y202234)
成都大学临床医学院/附属医院创新团队项目(CDFYCX202208)
出版年
2024
国家科技期刊平台
NSTL
万方数据