天然咖啡酰基奎宁酸类化合物抗RSV活性及其构效关系研究

发布时间：2018-01-14 06:32

本文关键词：天然咖啡酰基奎宁酸类化合物抗RSV活性及其构效关系研究　出处：《中药材》2016年02期 　论文类型：期刊论文

【摘要】：目的:研究天然来源的咖啡酰基奎宁酸类化合物体外抗呼吸道合胞病毒(Respiratory Syncytial Virus,RSV)的活性及其构效关系。方法:采用细胞病变(cytopathic effect,CPE)法对咖啡酰基奎宁酸类化合物抗RSV体外活性进行筛选,MTT法检测化合物对HEp-2细胞的细胞毒性,通过3D-QSAR(three-dimensional quantitative structureactivity relationship)模型分析其构效关系。结果:CPE结果显示咖啡酰基奎宁酸类化合物均表现出较好的抗RSV作用,其中活性最好的4,5-双咖啡酰基奎宁酸甲酯(CQA-4)的IC_(50)=2.5μmol/L,选择性指数SI153.8,远远优于阳性对照药物利巴韦林(IC_(50)=8.3μmol/L,SI20);3D-QSAR分析结果显示,咖啡酰基为咖啡酰基奎宁酸衍生物抗RSV的活性基团。结论:天然来源的咖啡酰基奎宁酸类衍生物均具有抗RSV活性,其中双咖啡酰基奎宁酸类化合物活性最好。构效关系研究表明,该类化合物抗RSV活性受其构型和取代基的影响很大。
[Abstract]:Objective: to study the anti-respiratory syncytial Syncytial Virus of caffeyl quininic acid compounds from natural sources in vitro. Methods: cytopathic effect was used. The activity of caffeyl quininic acid against RSV in vitro was screened by RSV method. The cytotoxicity of the compounds to HEp-2 cells was detected by MTT assay. Through 3D-QSAR (. Three-dimensional quantitative structureactivity relationship. Results the results showed that the caffeoyl quinic acid compounds showed good anti- RSV effect. The IC_(50)=2.5 渭 mol / L, selectivity index (SI153.8) of CQA-4 was the most active. It was much better than the positive control drug ribavirin in IC50 / L 8.3 渭 mol / L SI20; The results of 3D-QSAR analysis showed that the caffeyl group was the active group of caffeyl quininic acid derivatives against RSV. Conclusion: all the naturally derived caffeyl quininic acid derivatives have anti-#en1# activity. The results of structure-activity relationship showed that the anti- RSV activity of these compounds was greatly affected by their configurations and substituents.
【作者单位】：暨南大学中药及天然药物研究所;广东药学院中心实验室;
【基金】：国家自然科学基金(81202429;81473114) 广东省自然科学基金重点项目(S2013020012864)
【分类号】：R373.1
【正文快照】： 呼吸道合胞病毒(respiratory syncytial virus,RSV)是一种RNA病毒,属副粘液病毒科,是一种常见的呼吸道感染病原体,多见于新生儿及6月以内的婴儿,可导致婴幼儿期肺炎、支气管炎和儿童支气管哮喘〔1〕,亦可导致老年人和免疫力低下人群呼吸道疾病。目前临床上对RSV感染尚无特异有

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