Ingredient Analysis

High-resolution screening of α-glucosidase inhibitors from Polygoni Cuspidate Rhizoma et Radix*

  • CHEN Wen-long ,
  • HE Jian ,
  • TAO Qi-qi ,
  • CHEN Zhi-chao ,
  • ZHOU Ling-jia ,
  • CHEN Zhi-xu ,
  • JIANG Zheng-jin ,
  • ZHANG Ting-ting
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  • 1. Institute of Pharmaceutical Analysis, College of Pharmacy, Jinan University, Guangzhou 510632, China;
    2. China Resources Sanjiu Medical & Pharmaceutical Co., Ltd., Shenzhen 518110, China

Received date: 2024-06-17

  Online published: 2025-05-29

Abstract

Objective: To study the bioactive components of the hypoglycemic effect of the traditional Chinese medicine Polygoni Cuspidate Rhizoma et Radix through its ability to inhibit α-glucosidase activity. Methods: Four modules: high-performance liquid chromatography system, the nanofraction collector, the channel of bioassay and high-resolution mass spectrometry were integrated to build a high-throughput bioassay profiling analysis platform. The preparative liquid chromatography was introduced to apply segmented enrichment to the extract of Polygoni Cuspidate Rhizoma et Radix, and the rapid screening of α-glucosidase inhibitors from Polygoni Cuspidate Rhizoma et Radix was realized by optimizing the chromatographic separation conditions, microfluidic fractionation collection parameters and bioassaying of enzyme activity in multi-well plates. Results: 28 α-glucosidase inhibitors were identified from Polygoni Cuspidate Rhizoma et Radix. The inhibitory activities of catechin-3-O-galloyl and procyanidin B2-3''-O-gallate were determined with the IC50 values of (9.49±1.93) μmol · L-1 and (69.94±8.14) μmol · L-1, respectively. Conclusion: This study has enabled high-throughput and high-resolution screening of α-glucosidase inhibitors in traditional Chinese medicine, providing a valuable tool for elucidating the active components and mechanisms of Polygoni Cuspidate Rhizoma et Radix to lower hyperglycemia.

Cite this article

CHEN Wen-long , HE Jian , TAO Qi-qi , CHEN Zhi-chao , ZHOU Ling-jia , CHEN Zhi-xu , JIANG Zheng-jin , ZHANG Ting-ting . High-resolution screening of α-glucosidase inhibitors from Polygoni Cuspidate Rhizoma et Radix*[J]. Chinese Journal of Pharmaceutical Analysis, 2025 , 45(1) : 81 -91 . DOI: 10.16155/j.0254-1793.2024-0404

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