丹皮酚的抗HIV-1活性初步实验研究  

Preliminary experimental study on anti HIV-1 activity of paeonol

作　　者：杨剑霜 班磊 王浦丁 张曼曼 刘洁 梁浩 叶力 刘欣 YANG Jianshuang;BAN Lei;WANG Puding;ZHANG Manman;LIU Jie;LIANG Hao;YE Li;LIU Xin(The First clinical Medical college,Guangxi Medical University,Nanning,Guangxi Zhuang Autonomous Region 530021,China;不详)

机构地区：[1]广西医科大学第一临床医学院,广西壮族自治区南宁530021 [2]广西医科大学生命科学研究院广西艾滋病防治研究重点实验室广西生物医药协同创新中心

出　　处：《医学动物防制》2023年第12期1209-1212,共4页Journal of Medical Pest Control

基　　金：2022年度广西高校中青年教师科研基础能力提升项目(2022KY0090);广西重点研发计划(桂科AB19245038);2020年创新创业训练计划自治区级项目(202010598120);广西医科大学未来学术之星(WLXSZX20002)。

摘　　要：目的基于国内艾滋病流行现状,以丹皮酚抗菌消炎、调节代谢、调理免疫、抗肿瘤、抗病毒等药理活性为基础,进一步明确丹皮酚的抗人类免疫缺陷病毒(Human immunodeficiency virus,HIV)-1活性,为新型抗HIV药物的研发提供依据。方法建立TZM-bl-HIV-1IIIB细胞系统,设计细胞毒性实验及抗病毒活性实验,通过检测荧光素酶报告基因在TZM-bl细胞中的表达水平,探讨丹皮酚的毒性及抗HIV-1活性。结果在细胞毒性实验及抗病毒活性实验中,细胞存活率及抗HIV-1IIIB活性均与药物浓度呈剂量依赖关系,且通过Graphpad Prism 5软件计算出丹皮酚对TZM-bl细胞的半数细胞毒性浓度(concentration of cytotoxicity 50%,CC50)为208.00μM,丹皮酚对HIV-1IIIB的半数抑制浓度(median effective concentration,IC50)>48.14μM,治疗指数(therapeutic index,TI)为4.32。结论多酚类化合物已在近年研究中被发现具备抗HIV的生物活性,丹皮酚属植物多酚类药物,既往研究表明其通过多靶点多通路机制表现出多种药理活性,本次实验中其表现出抗病毒活性强兼自身毒性弱的特点。可见丹皮酚具有一定的抗HIV-1活性,能为研发抗HIV-1药物提供新参考,促进抗HIV-1药物的研制。Objective Based on the current situation of the domestic AIDS epidemic,the anti-Human immunodeficiency virus(HIV)-1 activity of paeonol was determined based on the pharmacological basis of paeonol against bacteria,inflammation,metabolism,immunity,tumor and virus,to provide a basis for the development of new anti-HIV drugs.Methods The TZM-bl-HIV-1IIIB cell system was established,the cytotoxicity test and antiviral activity test were designed,and the toxicity and anti-HIV-1 activity were investigated by measuring the expression level of luciferase reporter gene in TZM-bl cells.Results In cytotoxicity test and antiviral activity test,cell survival rate and anti-HIV-1IIIB activity were dose-dependent on drug concentration,the concentration of cytotoxicity 50%(CC50)of paeonol on TZM-bl cells was 208.00μM by Graphpad Prism 5 software,and the median effective concentration(IC50)of paeonol on HIV-1IIIB cells was more than 48.14μM,the therapeutic index(TI)was 4.32.Conclusion Polyphenols compounds have been found to have anti-HIV biological activity in recent years.Paeonol is a plant polyphenol drug,previous studies have shown that it has a variety of pharmacological activities through the mechanism of multi-target and multi-pathway.In this experiment,it shows strong antiviral activity and weak toxicity,therefore,paeonol has certain anti-HIV-1 activity,which can provide a new reference for the development of anti-HIV-1 drugs and promote the development of anti-HIV-1 drugs.

关 键 词：丹皮酚 抗HIV-1活性 细胞毒性 多酚类化合物 治疗指数 

分 类 号：R285.5[医药卫生—中药学]