Planta Med 2015; 81 - PB19
DOI: 10.1055/s-0035-1545174

Isolation and characterization of desmethoxyyangonin from Renealmia alpinia as a selective reversible inhibitor of human Monoamine Oxidase B

ND Chaurasiya 1, F León 2, I Gómez-Betancur 3, D Benjumea 3, SJ Cutler 2, LA Walker 1, 2, BL Tekwani 1, 2
  • 1National Center for Natural Products Research, and
  • 2Department of BioMolecular Sciences, School of Pharmacy, The University of Mississippi, University, MS 38677, USA
  • 3Programa de Ofidismo/Escorpionismo, Sede de Investigación Universitaria, Torre 2 Laboratorio 631, Facultad de Química Farmacéutica, Universidad de Antioquia, Medellin, Colombia

Renealmia alpinia (Zingiberaceae), a medicinal plant of tropical rainforests, is used to treat snakebites, as a febrifuge, analgesic, antiemetic, antiulcer, and anticonvulsant. The dichloromethane extract of R. alpinia leaves showed potent inhibition of recombinant human MAO-A and -B. Phytochemical studies yielded six known compounds including, pinostrobin, pinostrobin chalcone, sakuretin, sakuretin-4'-methyl, yashabushidiol, and desmethoxyyangonin. Desmethoxyyangonin displayed strong inhibition of MAO-A and -B (Ki values 0.922 and 0.031µM, respectively), with about 30 fold more selectivity against MAO-B. The kinetic analysis of the inhibition and equilibrium dialysis dissociation assay of the enzyme-inhibitor complex showed reversible binding of desmethoxyyangonin with MAO-A and -B. Selective reversible inhibitors of MAO-B have important therapeutic value for treatment of neurodegenerative disorders and Parkinson's Disease.

Fig. 1