Polygoni Cuspidati Rhizoma et Radix (PCR), the rhizome and root of Polygonum cuspidatum Sieb. et Zucc., has been used as an herbal medicine for a long time. In this study, the ultrafiltration combined with high performance liquid chromatography (UF-HPLC) method was developed to screen tyrosinase (TYR), α-glucosidase (α-GLU), and xanthine oxidase (XOD) inhibitors from PCR. Firstly, the inhibitory activity of 50% methanol PCR extract on TYR, α-GLU, XOD, and acetylcholinesterase (ACHE) was tested. The extract showed a good inhibition on the enzymes, except for ACHE. Therefore, UF-HPLC experiments were carried out to screen TYR, α-GLU, and XOD inhibitors from PCR extract. Seven potential bioactive components were discovered, including methylgallate (1), 1,6-di-O-galloyl-D-glucose (2), polydatin-4′-O-D-glucoside (3), resveratrol-4′-O-D-glucoside (4), polydatin (5), malonyl glucoside resveratrol (6), and resveratrol-5-O-D-glucoside (7). Most of them were found as enzyme inhibitors from PCR for the first time, except polydatin (5), which had been reported as an α-GLUI in PCR in the literature. Finally, molecular docking analysis was applied to validate the interactions of these seven potential active components with the enzymes. Compounds 1–7 were proven as TYR inhibitors, compounds 2, 4–7 were identified as XOD inhibitors, and compounds 4–6 were confirmed as α-GLU inhibitors. In short, the current study provides a good reference for the screening of enzyme inhibitors through UF-HPLC, and provides scientific data for future studies of PCR.

Polygoni Vivipari Rhizoma (PVR), the dried root of Polygonum viviparum, has been used as herbal medicine in China for a long time. In the present study, a new method based on multi-step matrix solid-phase dispersion (MSPD), ultrafiltration and high performance liquid chromatography (HPLC) for screening alpha-glucosidase inhibitors (AGIs) from PVR was proposed. First, three different PVR extractions were prepared by multi-step MSPD with 15% methanol, 60% methanol and 100% methanol. Second, the alpha-glucosidase inhibition tests for the three extracts were carried out, and the 60% methanol extraction showed the best activity. Then, the AGIs screening experiment was performed with ultrafiltration and HPLC analysis using the 60% methanol extraction. Seven binding components (quercetin−3−O−vicianoside, quercetin 3−O−neohesperidoside, rutin, hyperoside, quercetin 3−O−glucuronide, luteolin−7−O−neohesperidoside, kaempferol 3−glucuronide) were found. These seven components were further validated as the AGIs by molecular docking analysis. The developed method was a rapid and efficient tool for screening AGIs from PVR, which provided scientific data for the bioactive components study of PVR.

A rapid HPLC-UV method for the determination of three organic acids (neochlorogenic acid, chlorogenic acid, and cryptochlorogenic acid) in Polygoni Vivipari Rhizoma (PVR) by one marker was developed. The sample was prepared by effervescence-assisted matrix solid-phase dispersion (EA-MSPD). The separation of compounds was performed on a Poroshell column. The equal absorption wavelength was set as follows: 292 nm (0∼7 min) and 324 nm (7∼10 min). The analytical time including sample extraction and HPLC separation time was 12 min. The analytical method validation such as accuracy (recoveries 99.85%–106.29% and RSD < 2.9%), precision (RSD < 1.3%), reproducibility (RSD < 1.7%), and stability tests (RSD < 0.7% in 24 h) proved that the established HPLC method was suitable for determination of three organic acids in PVR. The contents of three analytes obtained by the external standard method with three markers and the equal absorption wavelength method with one marker were similar (RSD ≤ 2.0%). The developed method, which is rapid and reference compound saving, is an improved quality evaluation method of PVR.