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The AU\u2010HPLC\u2010QTOFMS technique was performed to fish for the potential active substances. Macroporous resin, preparative liquid chromatography, and high\u2010speed countercurrent chromatography were implemented for the accurate and targeted separation of active compounds. The inhibitory activities of target compounds to pancreatic lipase were detected by the inhibition experiments in vitro. The binding affinities and binding sites were analyzed using molecular docking.<\/jats:p><\/jats:sec><jats:sec><jats:title>Results<\/jats:title><jats:p>A total of eleven kinds of pancreatic lipase inhibitory substances were screened from <jats:italic><jats:styled-content style=\"fixed-case\">C. tangutica<\/jats:styled-content><\/jats:italic>. Seven triterpenoid saponins were screened for the first time as lipase inhibitors and successfully prepared with purities higher than 97%. Tanguticoside B, clematangoticoside J, hederoside H<jats:sub>1<\/jats:sub>, and rutin showed stronger inhibitory effects with IC<jats:sub>50<\/jats:sub> values of 1.539\u2009\u00b1\u20090.048, 1.661\u2009\u00b1\u20090.092, 1.793\u2009\u00b1\u20090.069, and 1.792\u2009\u00b1\u20090.094\u2009mmol\/l. Moreover, they have the lowest \u0394G values of \u221210.84, \u22129.97, \u221210.87, and \u22129.39\u2009kcal\/mol to pancreatic lipase.<\/jats:p><\/jats:sec><jats:sec><jats:title>Conclusion<\/jats:title><jats:p>The integrated strategy using AU\u2010HPLC\u2010QTOFMS, targeted separation, <jats:italic>in vitro<\/jats:italic> validation, and molecular docking was feasible for rapidly screening and directionally isolating pancreatic lipase inhibitors from <jats:styled-content style=\"fixed-case\"><jats:italic>C. tangutica<\/jats:italic><\/jats:styled-content>.<\/jats:p><\/jats:sec>","DOI":"10.1002\/pca.3422","type":"journal-article","created":{"date-parts":[[2024,7,15]],"date-time":"2024-07-15T21:34:25Z","timestamp":1721079265000},"page":"101-112","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":9,"title":["Rapidly screening of pancreatic lipase inhibitors from <scp><i>Clematis tangutica<\/i><\/scp> using affinity 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