Objective: To study the inhibitory effects of natural caffeoylquinic acid derivates against respiratory syncytial virus（ RSV） in vitro and their quantitative structure-activity relationship.
Methods: The anti-RSV activities of caffeoylquinic acid derivates were detected by cytopathic effect（ CPE） method,MTT assay was adopted to evaluate the cytotoxicities of caffeoylquinic acid derivates and a three-dimensional quantitative structure-activity relationship（ 3D-QSAR） model was built.
Results: The caffeoylquinic acid derivates showed different levels of anti-RSV activity. 4,5-d-CQAME（ CQA-4） was the most effective anti-RSV compound with IC50 of 2. 5μmol /L,and the SI was greater than 153. 8. Its effect was much better than the positive control drug ribavirin with the IC50 of 8. 3 μmol /L,and SI > 20,respectively. The result of 3D-QSAR study showed that caffeoyl group was important for the anti-RSV activity.
Conclusion: Natural caffeoylquinic acid derivates exhibit anti-RSV activity and dicaffeoylquinic derivates are the most effective anti-RSV compounds. Both configuration and substituent groups have a great influence on the anti-RSV activity.
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