2016
DOI: 10.1021/acs.chemrestox.5b00497
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Metformin Scavenges Methylglyoxal To Form a Novel Imidazolinone Metabolite in Humans

Abstract: Methylglyoxal (MG) is a highly reactive dicarbonyl compound involved in the formation of advanced glycation endproducts (AGE). Levels of MG are elevated in patients with type-2 diabetes mellitus (T2DM), and AGE have been implicated in the progression of diabetic complications. The antihyperglycemic drug metformin (MF) has been suggested to be a scavenger of MG. The present work examined and characterized unequivocally the resulting scavenged product from the metformin–MG reaction. The primary product was chara… Show more

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Cited by 79 publications
(76 citation statements)
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“…It reacts with MG to form mainly hydroimidazolone and also triazepinone adducts (159). These adducts are detected i n vi vo but they are quantitatively minor compared to the flux of MG formation (18,85). The peak plasma concentration of metformin is 23 µM at the 1.5g dose but may be ca.4 mM in the jejunum after ingestion (66).…”
Section: Et Formi Nmentioning
confidence: 99%
“…It reacts with MG to form mainly hydroimidazolone and also triazepinone adducts (159). These adducts are detected i n vi vo but they are quantitatively minor compared to the flux of MG formation (18,85). The peak plasma concentration of metformin is 23 µM at the 1.5g dose but may be ca.4 mM in the jejunum after ingestion (66).…”
Section: Et Formi Nmentioning
confidence: 99%
“…In a recent study, Kinsky et al . examined urine samples from 92 metformin-treated T2DM patients and reported a strong positive correlation between oral metformin concentration and metformin-MGO conjugate levels in urine [22], suggesting that metformin scavenges and enhances renal excretion of MGO. In addition to its known mechanism of actions, such studies suggest a secondary therapeutic effect of metformin as an AGE scavenger.…”
Section: Clinically Approved Agents With Aldehyde Scavenging Capacitiesmentioning
confidence: 99%
“…Serum MG levels were observed to decrease in diabetic patients under intensive treatment with common antidiabetic drugs when compared with routine care, an effect that may be obtained by simple glucose lowering or by drug pleiotropic effects in MG scavenging . In fact, metformin was observed to directly scavenge MG and to increase GLO1 activity preventing diabetic complications . In addition, the DPP‐IV inhibitor Gemigliptin showed anti‐glycation properties in vitro and in diabetic rats and the GLP‐1 analogue Liraglutide showed neuroprotective effects in neuroblastoma cells exposed to MG .…”
Section: The Promise Of New Therapeutic Targetsmentioning
confidence: 99%