摘要
目的 探讨鹰嘴豆芽素A对靶酶丝裂原激活蛋白激酶P38α亚型(P38αMAPK)的抑制作用。方法 应用软件Autodock Vina将鹰嘴豆芽素A与P38αMAPK晶体三维结构1KV2的活性位点进行分子对接,而后利用脂多糖(LPS)诱导的小鼠RAW 264.7细胞炎症模型验证鹰嘴豆芽素A对P38αMAPK的抑制活性。结果 鹰嘴豆芽素A可结合于靶酶晶体结构1KV2的活性位点以干扰正常底物的进入,从而对P38αMAPK的生物学功能起到抑制作用;细胞炎症模型实验证明,与LPS模型组比较,阳性对照药地塞米松和鹰嘴豆芽素A单体浓度各剂量(25、50、100μmol/L)干预后可明显下调细胞上清液中一氧化氮和肿瘤坏死因子-α水平(P<0.05)。结论 鹰嘴豆芽素A可作用于P38αMAPK活性位点而发挥抗炎的药理活性。
Objective To investigate the inhibitory effect of biochanin A on P38 mitogen-activated protein kinase(P38αMAPK).Methods The software Autodock Vina was used to perform molecular docking between biochanin A and the active site of P38αMAPK crystal structure 1KV2,and then the lipopolysaccharide(LPS)-induced inflammation model of mouse RAW 264.7 cells was used to verify the inhibitory effect of biochanin A on activity of P38αMAPK.Results Biochanin A could bind to the active site of 1KV2 to interfere with the entry of normal substrate of the target enzyme,which led to an inhibitory effect on the biological functions of P38αMAPK.The experiments in cell inflammation models showed that compared with the LPS model group,after intervention with the positive control Dexamethasone,biochanin A,at monomer concentrations of 25,50 and 100μmol/L,the levels of NO and TNF-αin cell supernatants were significantly down-regulated(P<0.05).Conclusion Biochanin A can act on the active site of P38αMAPK and exert the anti-inflammatory pharmacological activity.
作者
薛倩
侯春立
张丽波
高聪慧
吴红海
陈虹
何强
苏彦雷
XUE Qian;HOU Chunli;ZHANG Libo;GAO Conghui;WU Honghai;CHEN Hong;HE Qiang;SU Yanlei(Department of Clinical Pharmacy,the 980th Hospital of the Joint Logistics Support Force,Shijiazhuang 050082,China;Department of Oncology,the 980th Hospital of the Joint Logistics Support Force,Shijiazhuang 050082,China;Second Outpatient Department,the 980th Hospital of the Joint Logistics Support Force,Shijiazhuang 050082,China;Department of Respiratory,the 980th Hospital of the Joint Logistics Support Force,Shijiazhuang 050082,China;Department of Dermatology,the 980th Hospital of the Joint Logistics Support Force,Shijiazhuang 050082,China)
出处
《转化医学杂志》
2024年第2期158-161,共4页
Translational Medicine Journal
基金
河北省卫生健康委重点医学科研攻关计划(20231303)
河北省卫生健康委医学科研计划课题(20220276)。
