紫草素(shikonin)抗奥密克戎毒株的实验研究及机制分析  

Preliminary study on Activity of Shikonin against Omicron Subvariant and Mechanism Analysis

作　　者：王秀民[1] 谢小华 孙永[3] 袁媛[3] 崔志梅[1] 张涛[1] 苏彦雷 孙殿兴 吴红海 张晶[5] WANG Xiuming;XIE Xiaohua;SUN Yong;YUAN Yuan;CUI Zhimei;ZHANG Tao;SU Yanei;SUN Dianxing;WU Honghai;ZHANG Jing(The Traditional Chinese Medicine Hospital of Shijiazhuang,Shijiazhuang 050011,Hebei,China;Hebei General Hospital,Shijiazhuang 050051,Hebei,China;Anhui Provincial Center for Disease Control and Prevention,Hefei 230601,Anhui,China;The 980th Hospital of the Joint Logistics Support Force of the Chinese People's Liberation Army,Shijiazhuang 050082,Hebei,China;Institute of Medicinal Biotechnology,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China)

机构地区：[1]石家庄市中医院,河北石家庄050011 [2]河北省人民医院,河北石家庄050051 [3]安徽省疾病预防控制中心,安徽合肥230601 [4]联勤保障部队第九八〇医院,河北石家庄050082 [5]中国医学科学院、北京协和医学院医药生物技术研究所,北京100050

出　　处：《中华中医药学刊》2024年第9期23-25,I0001,共4页Chinese Archives of Traditional Chinese Medicine

基　　金：国家自然科学基金项目(81672041);河北省卫生健康委员会重点科研攻关计划项目(20231303);河北省中医药管理局科研计划基金项目(2022455)。

摘　　要：目的探讨右旋体紫草素(shikonin)抗奥密克戎毒株的药理作用和对新型冠状病毒主蛋白酶的抑制活性。方法使用奥密克戎毒株BA.2.2转染的Vero细胞模型检测shikonin的抗病毒活性;利用体外主蛋白酶荧光偏振模型测试shikonin对于新型冠状病毒主蛋白酶的抑制活性,实验以奈玛特韦为阳性对照化合物。结果Vero细胞模型药理活性测试发现shikonin具有抑制奥密克戎毒株核酸复制的作用;而在体外荧光偏振模型活性测试实验中,shikonin在20、50μM药物浓度并未表现出对主蛋白酶的显著抑制活性。结论紫草素(shikonin)在细胞水平的实验中表现出抗奥密克戎毒株的药理活性,但其可能是主蛋白酶的非特异性抑制剂,抗病毒的作用机理极可能为抑制新型冠状病毒RNA聚合酶。Objective To investigate the pharmacological activity of shikonin against Omicron strain and the inhibitory effect on the main protease of the novel coronavirus.Methods The antiviral activity of shikonin was tested using the Vero cell model trans-fected with the omicron BA.2.2 strain,and then nirmatrelvir was used as a positive control compound,and the inhibitory activity of shikonin against the novel coronavirus main protease was tested by using main protease fluorescence polarisation screening model in vitro.Results The extracorporal pharmacological activity test used Vero cell model showed that shikonin had the effect of inhibiting nucleic acid replication of the omicron strain,but shikonin did not show significant inhibitory activity against the main protease at the 20μM、50μM concentrations in a fluorescence polarisation screening model activity test.Conclusion Shikonin has pharmacological activity against the omicron strain at the cellular level,but it may be a non-specific inhibitor of the main prote-ase,and the mechanism of antiviral action is most likely to inhibit the novel coronavirus RNA polymerase.

关 键 词：紫草素 奥密克戎毒株 RNA聚合酶 主蛋白酶 荧光偏振筛选模型 分子对接 

分 类 号：R282.11[医药卫生—中药学]