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.
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)
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)。
