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Published on: June 28, 2019
[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.
Abstract:
Sugar-poison caused blood-heat is the pathological basis of many complications of diabetes. Advanced glycation end products( AGEs) are considered as the potential glycotoxic factor that can cause blood-heat. Sophorae Flos hold the effect of removing pathogenic heat from blood. In this study,chromatographic non-enzymatic glycation reaction system of bovine serum albumin( BSA)/methylglyoxal( MGO) and Sophorae Flos was established to identify active components in Sophorae Flos inhibiting AGEs formation. The HPLC was used to analyze chromatograms before and after the incubation of Sophorae Flos and methylglyoxal. Changes of chromatographic peaks of eight compounds was found. It is speculated that this change may be due to new substance produced by the reaction of active components in Sophorae Flos and methylglyoxal,and these active components may be flavonoid component rutin. Further investigation for the effects of rutin and MGO reaction( 1 ∶ 1,1 ∶ 3,3 ∶ 1) for 6 days on the formation of AGEs was performed. The results showed that the inhibition activity of rutin on AGEs production was most obvious when the reaction ratio was 1 ∶3,and the most inhibition was in 24 h and stabilized after 3 d. The product of the reaction of rutin with MGO was identified by LC-ESI-MS/MS,which indicated that the newly formed seven substances were the mono-and di-MGO adducts of rutin. This study showed that rutin is the active component on Sophorae Flos for removing pathogenic heat from blood by forming new compounds to inhibit the formation of sugar poison products,which provides reference for rational application of Sophorae Flos.
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.

