The dipeptidyl peptidase-4 inhibitory effect of flavonoids is hindered in protein rich environments

• DOI: 10.1039/c9fo00722a
• Publication Date: 2019-08-23T12:43:32Z
• Authors: Carina Proença; Marisa Freitas; Daniela Ribeiro; Sara M. Tomé; Alberto N. Araújo; Artur M. S. Silva; Pedro A. Fernandes; Eduarda Fernandes
• Keywords: Dipeptidyl peptidase; Ex vivo

Dipeptidyl peptidase-4 (DPP-4) inhibitors present a unique approach for the management of type 2 diabetes (T2D). In study, inhibition DPP-4 was evaluated large panel flavonoids, important components human diet, using in vitro and ex vivo models. The activity isolated enzyme assayed vitro. Subsequently, most active flavonoids were tested whole blood plasma. this contrary to fluorometric tests, did not show inhibitory against DPP-4. Due discrepancy results between approaches, plasma protein binding values determined, presenting from 43.9 100.0%. This work provides new insight into DPP-4, based on flavonoid scaffold. Additionally, obtained showed that effect hindered rich environments, like occurring blood, indicated need experimental refinement drug discovery targets.