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Zarmouh NO, Mazzio EA, Elshami FM, et al. Evaluation of the Inhibitory Effects of Bavachinin and Bavachin on Human Monoamine Oxidases A and B. Evid Based Complement Alternat Med. 2015;2015:852194doi: 10.1155/2015/852194.
Zarmouh, N. O., Mazzio, E. A., Elshami, F. M., Messeha, S. S., Eyunni, S. V., & Soliman, K. F. (2015). Evaluation of the Inhibitory Effects of Bavachinin and Bavachin on Human Monoamine Oxidases A and B. Evidence-based complementary and alternative medicine : eCAM, 2015852194. https://doi.org/10.1155/2015/852194
Zarmouh, Najla O, et al. "Evaluation of the Inhibitory Effects of Bavachinin and Bavachin on Human Monoamine Oxidases A and B." Evidence-based complementary and alternative medicine : eCAM vol. 2015 (2015): 852194. doi: https://doi.org/10.1155/2015/852194
Zarmouh NO, Mazzio EA, Elshami FM, Messeha SS, Eyunni SV, Soliman KF. Evaluation of the Inhibitory Effects of Bavachinin and Bavachin on Human Monoamine Oxidases A and B. Evid Based Complement Alternat Med. 2015;2015:852194. doi: 10.1155/2015/852194. Epub 2015 Oct 19. PMID: 26557867; PMCID: PMC4629031.
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Evid Based Complement Alternat Med. 2015;2015:852194. doi: 10.1155/2015/852194. Epub 2015 Oct 19.

Evaluation of the Inhibitory Effects of Bavachinin and Bavachin on Human Monoamine Oxidases A and B.

Evidence-based complementary and alternative medicine : eCAM

Najla O Zarmouh, Elizabeth A Mazzio, Faisel M Elshami, Samia S Messeha, Suresh V K Eyunni, Karam F A Soliman

Affiliations

  1. College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL 32307, USA.

PMID: 26557867 PMCID: PMC4629031 DOI: 10.1155/2015/852194

Abstract

Monoamine oxidase B inhibitors (MAO-BIs) are used in the early management of Parkinson's disease (PD). Long-term suspected side effects of MAO-B classical inhibitors established the need for safer alternative therapeutic agents. In our study, the flavanone bavachinin (BNN) and its analog bavachin (BVN) found in the seeds of Psoralea corylifolia L. ethanolic extract (PCSEE) were investigated for their human MAO-A and MAO-B (hMAO-A and hMAO-B) inhibition. Both PCSEE and BNN effectively reduced hMAO-B activity more than hMAO-A while BVN had activating effects. BNN showed selective hMAO-B inhibition (IC50 ~ 8.82 μM) more than hMAO-A (IC502009;~ 189.28 μM). BNN in the crude extract was determined by HPLC, also validated by TLC showing a yield of 0.21% PCSEE dry weight. BNN competitively inhibited hMAO-A and hMAO-B, with a lower hMAO-B K i than hMAO-A K i by 10.33-fold, and reduced hMAO-B K m /V max efficiency ratio to be comparable to the standard selegiline. Molecular docking examination of BNN and BVN predicted an indirect role of BNN C7-methoxy group for its higher affinity, selectivity, and reversibility as an MAO-BI. These findings suggest that BNN, which is known to be a potent PPAR-γ agonist, is a selective and competitive hMAO-B inhibitor and could be used in the management of PD.

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