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Glyoxalase 1 Inducer, trans-Resveratrol and Hesperetin–Dietary Supplement with Multi-Modal Health Benefits

Summary

A dietary supplement combining trans-resveratrol and hesperetin activates a cellular defense mechanism called Nrf2, which increases production of an enzyme (Glo1) that helps eliminate harmful byproducts of sugar metabolism. This supplement improved multiple aspects of health in studies, including better blood sugar control, reduced inflammation, and improved liver function. The combination works better than either ingredient alone, and the trans form of resveratrol is much more effective than the cis form.

Background

Methylglyoxal (MG) accumulation, known as dicarbonyl stress, occurs in overweight and obese individuals and those with diabetes. The dietary supplement trans-resveratrol and hesperetin (tRES+HESP), also known as GlucoRegulate, induces glyoxalase 1 (Glo1) expression through Nrf2 activation, counteracting MG accumulation and its pathological effects.

Objective

To explore health-beneficial gene expression induced by tRES+HESP beyond Glo1 in human endothelial cells, fibroblasts, and hepatocytes, and to compare the Glo1 inducer activity of trans-resveratrol versus cis-resveratrol.

Results

tRES+HESP increased expression of genes linked to dicarbonyl stress prevention, antioxidant defense, proteostasis, and decreased inflammation and extracellular matrix remodeling across all cell types. Trans-resveratrol showed ninefold lower EC50 than cis-resveratrol in Glo1 induction (2.52 µM vs 23.0 µM).

Conclusion

GlucoRegulate provides multi-modal health benefits through Nrf2-mediated gene expression affecting glucose metabolism, lipid metabolism, oxidative stress, and inflammatory responses, supporting potential applications in type 2 diabetes prevention and metabolic dysfunction-associated steatotic liver disease.
  • Published in:Antioxidants (Basel),
  • Study Type:In Vitro Cell Culture Study,
  • Source: PMID: 40867852, DOI: 10.3390/antiox14080956
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