| Summary: | <i>Valeriana rigida</i> Ruiz & Pav. (<i>V. rigida</i>) has long been used as a herbal medicine in Peru; however, its phytochemicals and pharmacology need to be scientifically explored. In this study, we combined the offline 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH)-/ultrafiltration-high-performance liquid chromatography (HPLC) and high-speed counter-current chromatography (HSCCC)/pH-zone-refining counter-current chromatography (pH-zone-refining CCC) to screen and separate the antioxidants and aldose reductase (AR) inhibitors from the 70% MeOH extract of <i>V. rigida,</i> which exhibited remarkable antioxidant and AR inhibitory activities. Seven compounds were initially screened as target compounds exhibiting dual antioxidant and AR inhibitory activities using DPPH-/ultrafiltration-HPLC, which guided the subsequent pH-zone-refining CCC and HSCCC separations of these target compounds, namely 3-<i>O</i>-caffeoylquinic acid, 4-<i>O</i>-caffeoylquinic acid, 5-<i>O</i>-caffeoylquinic acid, 3,4-<i>O</i>-di-caffeoylquinic acid, 3,5-<i>O</i>-di-caffeoylquinic acid, 4,5-<i>O</i>-di-caffeoylquinic acid, and 3,4,5-<i>O</i>-tri-caffeoylquinic acid. These compounds are identified for the first time in <i>V. rigida</i> and exhibited remarkable antioxidant and AR inhibitory activities. The results demonstrate that the method established in this study can be used to efficiently screen and separate the antioxidants and AR inhibitors from natural products and, particularly, the root extract of <i>V. rigida</i> is a new source of caffeoylquinic acids with antioxidant and AR inhibitory activities, and it can be used as a potential functional food ingredient for diabetes.
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