Barley Phenolamides Effectively Scavenge Harmful Methylglyoxal In Vitro and in Mice

Abstract

Scope: Methylglyoxal (MGO), a harmful reactive dicarbonyl, is involved in the pathogenesis and development of diabetes and diabetic complications. The goal of this study is to determine whether bioactive phenolamides in barley, p-coumaroylagmatine (pCAA) and feruloylagmatine (FAA), which share a similar guanidine group to diabetic drug metformin, have the capacity to detoxify MGO. Methods and results: In this study, the MGO-trapping abilities of these two phenolamides both in vitro and in mice are evaluated. It is found that in vitro anti-MGO capacities of pCAA and FAA are comparable to that of metformin, and both phenolamides could rapidly scavenge MGO via forming mono-and di-MGO adducts validated by in-house synthesized standards and interpretation of respective LC-MS n (n = 2-3) data. Furthermore, mono-MGO conjugates of phenolamides are detected from feces and urine of mice after oral administration of the corresponding phenolamides. Conclusion: These findings suggest that barley phenolamides may have the potentials to be developed as alternative therapeutics to prevent the development of MGO-associated diabetes and diabetic complications.

'Nine Steaming Nine Sun‐drying' processing enhanced properties of Polygonatum kingianum against inflammation, oxidative stress and hyperglycemia

“…In addition, we found that biological activities of identified key metabolites that were enriched by NSND processing have consistently been proved in previous studies, 28,52,55,57,65,67,73‐78 supporting our findings (Table 3). Among them, gallocatechin and furoaloesone showed the largest binding energy with most of the targeted proteins.…”

“…We conducted molecular docking to further investigate the binding ability between key targets – that is, TNF, VEGF, STAT3, IL6, STOR, GCKR, GLIT4, HIF1, and INSR – that were closely related to oxidative stress, inflammation, and hyperglycemia, and 13 main metabolites that were significantly abundant in aqueous extracts of processed PK compared with crude PK. Results collectively demonstrated great ability of processed PK‐enriched metabolites to combat abnormal oxidative stress and inflammation status, as well as hyperglycemia, partly via regulating multi‐pathways, consistent with previous study 28,63‐70 …”

“…Results collectively demonstrated great ability of processed PK-enriched metabolites to combat abnormal oxidative stress and inflammation status, as well as hyperglycemia, partly via regulating multi-pathways, consistent with previous study. 28,[63][64][65][66][67][68][69][70] We found that the binding energy ranged from −3.3 to −9.4 kcal mol −1 between selected targets and metabolites. A total of 11 compounds had a docking score of less than −5.0 with core targets, indicating that they had strong binding activity with each other.…”