[Screening for active components of Sophorae Flos on inhibiting AGEs formation based on non-enzymatic glycation

Nan Jiang1, Fu-Jing Wang1, Liang Feng2

  • 1School of Pharmacy,Anhui University of Chinese Medicine Hefei 230012,China Department of Traditional Chinese Medicine,School of Traditional Chinese Pharmacy,China Pharmaceutical University Nanjing 211198,China.

Insights

Sophorae Flos contains rutin, which inhibits advanced glycation end products (AGEs) formation by reacting with methylglyoxal. This action helps prevent diabetes complications by reducing sugar-poison effects.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Traditional Chinese Medicine

Background:

  • Advanced glycation end products (AGEs) are implicated in diabetes complications, driven by 'sugar-poison' induced blood heat.
  • Sophorae Flos is traditionally used to clear pathogenic heat from the blood.
  • Identifying active components in Sophorae Flos that inhibit AGEs formation is crucial for understanding its therapeutic effects.

Purpose of the Study:

  • To establish a reaction system to identify active components in Sophorae Flos that inhibit AGEs formation.
  • To investigate the inhibitory effect of the flavonoid rutin on AGEs production.
  • To characterize the reaction products between rutin and methylglyoxal.

Main Methods:

  • A chromatographic non-enzymatic glycation system using bovine serum albumin (BSA) and methylglyoxal (MGO) was developed.
  • High-Performance Liquid Chromatography (HPLC) was used to analyze changes in Sophorae Flos components after reaction with MGO.
  • Liquid Chromatography-Electrospray Ionization-Tandem Mass Spectrometry (LC-ESI-MS/MS) was employed to identify reaction products.

Main Results:

  • HPLC analysis revealed changes in eight compounds of Sophorae Flos upon reaction with MGO, suggesting active component involvement.
  • Rutin demonstrated significant inhibition of AGEs production, with optimal effect at a 1:3 ratio with MGO, showing rapid inhibition within 24 hours.
  • LC-ESI-MS/MS identified seven new substances as mono- and di-MGO adducts of rutin, confirming rutin's direct reaction with MGO.

Conclusions:

  • Rutin is identified as the active component in Sophorae Flos responsible for inhibiting AGEs formation.
  • Rutin exerts its 'heat-clearing' effect by forming new compounds with methylglyoxal, thereby preventing the production of AGEs.
  • These findings provide a scientific basis for the traditional use of Sophorae Flos in managing conditions related to AGEs accumulation.

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