By using extraction yield, total polyphenolic content, antidiabetic activities (PTP-1B and α-glycosidase), and antioxidant activity (ABTS and DPPH) as indicated markers, the extraction conditions of the prescription Kursi Wufarikun Ziyabit (KWZ) were optimized by response surface methodology (RSM). Independent variables were ethanol concentration, extraction temperature, solid-to-solvent ratio, and extraction time. The result of RSM analysis showed that the four variables investigated have a significant effect () for , , , , and with value of 0.9120, 0.9793, 0.9076, 0.9125, and 0.9709, respectively. Optimal conditions for the highest extraction yield of 39.28%, PTP-1B inhibition rate of 86.21%, α-glycosidase enzymes inhibition rate of 96.56%, and ABTS inhibition rate of 77.38% were derived at ethanol concentration 50.11%, extraction temperature 72.06°C, solid-to-solvent ratio 1 : 22.73 g/mL, and extraction time 2.93 h. On the basis of total polyphenol content of 48.44% in this optimal condition, the quantitative analysis of effective part of KWZ was characterized via UPLC method, 12 main components were identified by standard compounds, and all of them have shown good regression within the test ranges and the total content of them was 11.18%.
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