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In this study, an in vitro tyrosinase inhibition assay in combination with ultra performance liquid chromatography-orbitrap mass spectrometry (UPLC-orbitrap-MS) was developed for the rapid screening and identification of tyrosinase modulators from roots of Angelica keiskei . Of the 15 candidates considered, nine chalcones, xanthoangelols ( 1 ), B ( 2 ), D ( 3 ), E ( 4 ), G ( 5 ), H ( 6 ), 4-hydroxyderricin ( 7 ), xanthokeismin B ( 8 ) and (2 E )-1-[4-hydroxy-2-(2-hydroxy-2-propanyl)-2,3-dihydro-1-benzofuran-7-yl]-3-(4-hydroxyphenyl)-2-propen-1-one ( 9 ), five coumarins, umbelliferone ( 10 ), selinidin ( 11 ), isopimpinellin ( 12 ), phellopterin ( 13 ) and xanthyletin ( 14 ), and one other compound, ashitabaol A ( 15 ), were distinguished between the test samples and the controls with statistical significance, and the structure of each compound was determined by comparing with in-house standards and the literature. Among these, six compounds, xanthoangelol ( 1 ), xanthoangelol D ( 3 ), xanthoangelol H ( 6 ), 4-hydroxyderricin ( 7 ), laserpitin ( 16 ) and isolaserpitin ( 17 ), were isolated from roots of A. keiskei . Of the compounds isolated, compounds 1 , 7 and 16 were subjected to tyrosinase inhibitory assay, and the IC 50 values were 15.87 ± 1.21, 60.14 ± 2.29 and &gt;100 μM, respectively. The present study indicated that the combination of in vitro tyrosinase inhibition assay coupled with UPLC-MS/MS could be widely applied to the rapid screening of active substances from various natural resources.

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Characterizing Tyrosinase Modulators from the Roots of Angelica keiskei Using Tyrosinase Inhibition Assay and UPLC-MS/MS as the Combinatorial Novel Approach