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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
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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1000μmol/L Bz-ATP激发的电流反应较强;10μmol/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。 Objective:To explore whether oridonin has an effect on P2X7 receptor agonist-induced current in hippocampal CA1 astrocytes.Methods:Autodock software was used 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 1000μmol/L Bz-ATP is much stronger.1 hour of incubation with 10μmol/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 affinity,and inhibit P2X7 receptor agonist Bz-ATP induced current response in hippocampal CA1 astrocytes.
作者 赵亚飞 吴嘉思 童宇 睢婉婉 时政 Zhao Yafei;Wu Jiasi;Tong Yu;Zhui Wanwan;Shi Zheng(College of acupuncture and moxibustion,Chengdu University of Traditional Chinese Medicine,Chengdu,611137,China;School of Clinical Medicine,Chengdu University,Chengdu,610106,China)
出处 《成都中医药大学学报》 2024年第3期8-11,共4页 Journal of Chengdu University of Traditional Chinese Medicine
基金 中国博士后基金(BX20220049,2022MD713682) 成都大学附属医院院级课题项目(Y2021006,Y202232,Y202234) 成都大学临床医学院/附属医院创新团队项目(CDFYCX202208)。
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 Oridonin P2X7 receptor Molecular docking Patch clamp Hippocampal astrocytes
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