Screening of Tyrosinase, Xanthine Oxidase, and α-Glucosidase Inhibitors from Polygoni Cuspidati Rhizoma et Radix by Ultrafiltration and HPLC Analysis

Abstract

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.

Identification and molecular docking of xanthine oxidase and α‐glucosidase inhibitors in Opuntia ficus‐indica fruit

“…The purified OFI extract showed better inhibitory activity against α-Glu than against acarbose (IC 50 = 345.67 µg/mL), whereas the inhibitory activity against XOD was less potent than that of allopurinol (IC 50 = 12.00 µg/mL). The results showed similar trends to the inhibitory effect of the extract from Polygoni Cuspidati Rhizoma et Radix on α-Glu and XOD (Chen et al, 2023). The extraction yield of polyphenols after OFI purification increased from 4.12% to 35.50%.…”

Screening Antioxidant Components in Different Parts of Dandelion Using Online Gradient Pressure Liquid Extraction Coupled with High-Performance Liquid Chromatography Antioxidant Analysis System and Molecular Simulations

“…In the field of antioxidant research, molecular docking analysis has been widely adopted, particularly for exploring how antioxidants interact with specific targets to elicit their functions [33,34]. This approach not only aids in understanding the molecular-level efficacy of antioxidants, but also lays a solid theoretical foundation for online antioxidant screening.…”

Screening of Key Components for Melanogenesis Inhibition of Polygonum cuspidatum Extract Based on the Spectrum–Effect Relationship and Molecular Docking

“…Polygonum cuspidatum (PC) extract has been included in the “Catalog of Used Cosmetic Ingredients (2021 Edition)” and is added to thousands of cosmetic products ( ) (accessed on 25 September 2023). Some studies have shown that PC extracts prepared by different methods have certain TYR inhibitory effects [ 11 , 12 , 13 ]. Although PC extract is widely used in whitening cosmetics, there are no quality standards for its application in cosmetics.…”

“…bevol.cn/index.html) (accessed on 25 September 2023). Some studies have shown that PC extracts prepared by different methods have certain TYR inhibitory effects [11][12][13]. Although PC extract is widely used in whitening cosmetics, there are no quality standards for its application in cosmetics.…”