and Studies Reveal Antidiabetic Properties of Arylbenzofurans from the Root Bark of Stapf

Diabetes remains an important disease worldwide with about 500 million patients globally. In tropical Africa, is traditionally used in the treatment of diabetes. Biological and phytochemical investigation of the root bark extracts of the plant led to the isolation of a new prenylated arylbenzofuran named 7-(3-hydroxy-3-methylbutyl)moracin M () and two congeners, moracins P () and M (). When compared to acarbose (IC = 486 µM), all the isolated compounds are better inhibitors of α-glucosidase with IC values of 16.9, 16.6, and 40.9 µM, respectively. However, they were not active against α-amylase. The compounds also demonstrated moderate inhibition of dipeptidyl peptidase-4 (DPP4). Based on docking studies, all isolates (, , and ) exhibit binding affinities of -8.7, -9.5, and -8.5 kcal/mol, respectively against α-glucosidase enzyme (PDB: 3AJ7). They are stabilized within the α-glucosidase active site through hydrogen bonds, pi interactions, and hydrophobic interactions. This study provides scientific support for the traditional use of in the treatment of diabetes as well as adding to the repository of α-glucosidase inhibitory agents.