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• XXT was eluted into 5 fractions by the macroporous absorption resin separation method. The fingerprints of different fractions were built and main chemical components were identified by UPLC-Q-TOF/MS technology. • The rat model of T2DM was successfully established and applied to assess the efficacy of different fractions from XXT. Results showed that XXT-1 and XXT-2 were the most active fractions. • The bioactive constituents of XXT were screened out by spectrum-effect relationship with grey relational analysis and pearson bivariate correlation analysis. Xiexin Tang (XXT) is a classic prescription for treating diabetes in clinical practices for thousands of years in China, which has been also proved by a large number of modern pharmacological studies. However, due to its complex composition, the bioactive ingredients of XXT is still unclear. In present researches, spectrum-effect relationship analysis is widely used to explore the material basis of traditional medical herbs, so this method was adopted in this study. Firstly, the extract of XXT was separated and enriched into 5 fractions by macroporous adsorption resin. Then, UPLC-Q-TOF/MS method was used for qualitative identification of components in each eluting part, and efficacy of each fraction was assessed by the T2DM rat model. Based on grey relational analysis and pearson bivariate correlation analysis, it was found that the components such as berberine, gallic acid, catechin, epicatechin, acteoside, berberastine and 1-O-galloyl-β-D-glucose might be the main effective basis of XXT to improve T2DM. [ABSTRACT FROM AUTHOR]