Identification of α-mangostin as a potent inhibitor of β-lactamase OXA-48

In this study, we investigated the inhibitory potential of α-mangostin against OXA-48 with an IC50 value of 0.52  μM. Enzyme activity assays demonstrated that α-mangostin inhibited OXA-48 reversibly through a non-competitive and dose-dependent inhibition mode. The docking analysis revealed that the 7-hydroxyl group of α-mangostin formed hydrogen bonds with Thr197 and Trp222, whereas the 5-hydroxyl group a nd the 4-carbonyl group interacted with Lys116 and Met115. Our study indicates that α-mangostin exhibits significant inhibition against OXA-48 and holds promise as a potential compound for the development of β-lactamase inhibitors.

Source: Medicinal Chemistry Research - January 27, 2024 Category: Chemistry Source Type: research