Cyclic Polyketides with alpha-Glucosidase Inhibitory Activity from Endiandra kingiana Gamble and Molecular Docking Study

• Main Authors: Azmi, Mohamad Nurul, Saad, Nur Amirah, Abu Bakar, Mohamad Hafizi, Omar, Mohammad Tasyriq Che, Aziz, Ahmad Nazif, Wahab, Habibah A., Siddiq, Sadia, Choudhary, M. Iqbal, Litaudon, Marc, Awang, Khalijah
• Format: Article
• Published: ACG Publications 2021
• Subjects: QD Chemistry; QK Botany; RM Therapeutics. Pharmacology; RS Pharmacy and materia medica
• Online Access: http://eprints.um.edu.my/34323/
• Institution: Universiti Malaya

A phytochemical investigation of the methanolic extract of Endiandra kingiana (bark) led to the isolation of four major compounds which are kingianic acid A ( 1), tsangibeilin B (2), kingianin A (3) and kingianin F (4). The structures were determined by 1D- and 2D-NMR analysis in combination with HRMS experiments. The compounds were screened for their in vitro alpha-glucosidase inhibition activity. Among them, compounds 3-4 showed potent alpha-glucosidase inhibition activity with IC50 value at 11.9 +/- 2.0 mu M and 19.7 +/- 1.5 mu M, respectively. The molecular docking study found that both compounds were bound into the active site of the N-terminal of MGAM, and thus agreed with the in vitro alpha-glucosidase enzyme inhibition activity results.