Identification of di-caffeoylquinic acids （di-CQAs） from Artemisia selengensis Turcz leaves and structure-activity relationship of di-CQAs on inhibiting xanthine oxidase （XOD） and inhibiting monosodium urate （MSU） induced IL-1β in vitro were studied. Di-CQAs from Artemisia selengensis Turcz leaves were identified by HPLC-Q/TOF-MS， and the effects of different di-CQAs on inhibiting XOD and inhibiting monosodium urate induced IL-1β were systematically studied. Results showed that five di-CQAs （1，4-diCQA， 3，4-diCQA， 1，5-diCQA， 3，5-diCQA and 4，5-diCQA） were identified in Artemisia selengensis Turcz leaves， and 1，4-diCQA was identified in Artemisia selengensis Turcz leaves in this study for the first time. The XOD inhibitory activity of caffeic acid substitution sites on di-CQAs was ranked as follows： C1 substitution > C4 substitution > C5 substitution > C3 substitution； The MSU-inducedIL-1β inhibitory activity of caffeic acid substitution sites on di-CQAs was ranked as follows： C1 substitution > C5 substitution > C3 substitution， C4 substitution≥ C5 substitution. In addition， the XOD inhibitory activity of di-CQAs was positively correlated with the MSU-induced IL-1β inhibitory activity of them， suggesting that di-CQAs couldinhibit MSU-induced IL-1β via inhibiting XOD. This study provides theoretical basis for studying the biological activities of di-CQAs with different structures， and also gives a reference for the development of di-CQAs from Artemisia selengensis Turcz and other dietary food for the prevention of hyperuricemia and gout.