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Monoamine Oxidase Inhibition by Kavalactones from Kava (Piper Methysticum).
Planta Med. 2019 Oct; 85(14-15):1136-1142.PM

Abstract

Monoamine oxidases (MAOs) are key metabolic enzymes for neurotransmitter and dietary amines and are targets for the treatment of neuropsychiatric and neurodegenerative disorders. This study examined the MAO inhibition potential of kavain and other kavalactones from the roots of kava (Piper methysticum), a plant that has been used for its anxiolytic properties. (±)-Kavain was found to be a good potency in vitro inhibitor of human MAO-B with an IC50 of 5.34 µM. (±)-Kavain is a weaker MAO-A inhibitor with an IC50 of 19.0 µM. Under the same experimental conditions, the reference MAO inhibitor, curcumin, displays IC50 values of 5.01 µM and 2.55 µM for the inhibition of MAO-A and MAO-B, respectively. It was further established that (±)-kavain interacts reversibly and competitively with MAO-A and MAO-B with enzyme-inhibitor dissociation constants (Ki) of 7.72 and 5.10 µM, respectively. Curcumin in turn, displays a Ki value of 3.08 µM for the inhibition of MAO-A. Based on these findings, other kavalactones (dihydrokavain, methysticin, dihydromethysticin, yangonin, and desmethoxyyangonin) were also evaluated as MAO inhibitors in this study. Yangonin proved to be the most potent MAO inhibitor with IC50 values of 1.29 and 0.085 µM for MAO-A and MAO-B, respectively. It may be concluded that some of the central effects (e.g., anxiolytic) of kava may be mediated by MAO inhibition.

Authors+Show Affiliations

Pharmaceutical Chemistry, School of Pharmacy and Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.Pharmaceutical Chemistry, School of Pharmacy and Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.Pharmaceutical Chemistry, School of Pharmacy and Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.Pharmaceutical Chemistry, School of Pharmacy and Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

31539917

Citation

Prinsloo, Denise, et al. "Monoamine Oxidase Inhibition By Kavalactones From Kava (Piper Methysticum)." Planta Medica, vol. 85, no. 14-15, 2019, pp. 1136-1142.
Prinsloo D, van Dyk S, Petzer A, et al. Monoamine Oxidase Inhibition by Kavalactones from Kava (Piper Methysticum). Planta Med. 2019;85(14-15):1136-1142.
Prinsloo, D., van Dyk, S., Petzer, A., & Petzer, J. P. (2019). Monoamine Oxidase Inhibition by Kavalactones from Kava (Piper Methysticum). Planta Medica, 85(14-15), 1136-1142. https://doi.org/10.1055/a-1008-9491
Prinsloo D, et al. Monoamine Oxidase Inhibition By Kavalactones From Kava (Piper Methysticum). Planta Med. 2019;85(14-15):1136-1142. PubMed PMID: 31539917.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Monoamine Oxidase Inhibition by Kavalactones from Kava (Piper Methysticum). AU - Prinsloo,Denise, AU - van Dyk,Sandra, AU - Petzer,Anél, AU - Petzer,Jacobus P, Y1 - 2019/09/20/ PY - 2019/9/21/pubmed PY - 2019/12/18/medline PY - 2019/9/21/entrez SP - 1136 EP - 1142 JF - Planta medica JO - Planta Med VL - 85 IS - 14-15 N2 - Monoamine oxidases (MAOs) are key metabolic enzymes for neurotransmitter and dietary amines and are targets for the treatment of neuropsychiatric and neurodegenerative disorders. This study examined the MAO inhibition potential of kavain and other kavalactones from the roots of kava (Piper methysticum), a plant that has been used for its anxiolytic properties. (±)-Kavain was found to be a good potency in vitro inhibitor of human MAO-B with an IC50 of 5.34 µM. (±)-Kavain is a weaker MAO-A inhibitor with an IC50 of 19.0 µM. Under the same experimental conditions, the reference MAO inhibitor, curcumin, displays IC50 values of 5.01 µM and 2.55 µM for the inhibition of MAO-A and MAO-B, respectively. It was further established that (±)-kavain interacts reversibly and competitively with MAO-A and MAO-B with enzyme-inhibitor dissociation constants (Ki) of 7.72 and 5.10 µM, respectively. Curcumin in turn, displays a Ki value of 3.08 µM for the inhibition of MAO-A. Based on these findings, other kavalactones (dihydrokavain, methysticin, dihydromethysticin, yangonin, and desmethoxyyangonin) were also evaluated as MAO inhibitors in this study. Yangonin proved to be the most potent MAO inhibitor with IC50 values of 1.29 and 0.085 µM for MAO-A and MAO-B, respectively. It may be concluded that some of the central effects (e.g., anxiolytic) of kava may be mediated by MAO inhibition. SN - 1439-0221 UR - https://www.unboundmedicine.com/medline/citation/31539917/Monoamine_Oxidase_Inhibition_by_Kavalactones_from_Kava__Piper_Methysticum__ L2 - http://www.thieme-connect.com/DOI/DOI?10.1055/a-1008-9491 DB - PRIME DP - Unbound Medicine ER -