Role of simulated in vitro gastrointestinal digestion on biotransformation and bioactivity of astragalosides from Radix Astragali

J Pharm Biomed Anal. 2023 Jul 5:231:115414. doi: 10.1016/j.jpba.2023.115414. Epub 2023 Apr 23.

Abstract

Radix Astragali (RA) is commonly used in Asian herbal therapy or food supply, and astragalosides and flavonoids are its major components with diverse pharmaceutical effects. To provide new information on the potential cardiovascular benefits of RA administered orally, the bioaccessibility of these compounds with relevant in vitro digestion parameters was determined for four digestion phases (oral, gastric, small and large intestines) by ultrahigh-performance liquid chromatography quadrupole time-of-flight-mass spectrometry (UPLC-Q-TOF/MS). Meanwhile, we compared the effects of digestion products on advanced glycation end products (AGEs)-induced intracellular reactive oxygen species (ROS) levels in a human arterial endothelial cells (HAECs) model, and studied the potential of RA against oxidative stress-related cardiovascular disease. The changes of saponins and flavonoids composition and antioxidant activity after digestion in intestines were mainly due to the astragaloside IV (AS-IV) biosynthesis involving saponins acetyl isomerization and deacetylation, and the flavonoid glycosides converted to aglycone by deglycosylation processes. All these results suggest that acetyl biotransformation of RA in small intestine directly influenced the response to oxidative stress, and might provide a reference for elucidation of the multi-component action after oral RA in cardiovascular health care.

Keywords: Acetyl isomerization; Cardiovascular health care; Flavonoids; In vitro digestion; Radix Astragali; Saponins.

MeSH terms

  • Biotransformation
  • Chromatography, High Pressure Liquid / methods
  • Digestion
  • Drugs, Chinese Herbal* / chemistry
  • Endothelial Cells / chemistry
  • Flavonoids / analysis
  • Humans
  • Saponins* / chemistry

Substances

  • Huang Qi
  • Saponins
  • Drugs, Chinese Herbal
  • Flavonoids