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Kavalactones from Kava (Piper methysticum) root extract as modulators of recombinant human glycine receptors.
Biol Chem. 2019 08 27; 400(9):1205-1215.BC

Abstract

Roots of kava (Piper methysticum) plant are used in almost all Pacific Ocean cultures to prepare a drink with sedative, anesthetic and euphoric properties. One of the main active ingredients of the extract are kava lactones. Here, kava root CO2 extract and three kavalactones, DL-kavain, dihydrokavain and yangonin (isolated from whole extract by column chromatography) were tested for their inhibitory action on recombinant homomeric human α1 glycine receptors expressed in HEK293 cells. Kava CO2 root extract, as well as the individual components DL-kavain, dihydrokavain and yangonin inhibited glycine receptor activity in a dose-dependent manner. DL-kavain was the most potent inhibitor (IC50 = 0.077 ± 0.002 mm), followed by yangonin (IC50 = 0.31 ± 0.04 mm) and dihydrokavain (IC50 = 3.23 ± 0.10 mm) which were 4- and 40-fold less active than DL-kavain, respectively. Application of kava root extract did not reduce maximum currents, but increased EC50 of glycine. Simultaneous application of kava extract and strychnine showed additive inhibition, suggesting that binding of kavalactones and strychnine on the receptor is mutually exclusive. Overall, kavalactones exert a moderate inhibitory effect on the human α1 glycine receptor with DL-kavain being the most potent constituent.

Authors+Show Affiliations

Department of Biochemistry, German University in Cairo, Main Entrance of Al Tagamoa Al Khames, New Cairo 11835, Egypt.Department of Biochemistry, German University in Cairo, Main Entrance of Al Tagamoa Al Khames, New Cairo 11835, Egypt.Department of Biochemistry, German University in Cairo, Main Entrance of Al Tagamoa Al Khames, New Cairo 11835, Egypt.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

31141476

Citation

Hegazy, Nada Hany, et al. "Kavalactones From Kava (Piper Methysticum) Root Extract as Modulators of Recombinant Human Glycine Receptors." Biological Chemistry, vol. 400, no. 9, 2019, pp. 1205-1215.
Hegazy NH, Breitinger HG, Breitinger U. Kavalactones from Kava (Piper methysticum) root extract as modulators of recombinant human glycine receptors. Biol Chem. 2019;400(9):1205-1215.
Hegazy, N. H., Breitinger, H. G., & Breitinger, U. (2019). Kavalactones from Kava (Piper methysticum) root extract as modulators of recombinant human glycine receptors. Biological Chemistry, 400(9), 1205-1215. https://doi.org/10.1515/hsz-2019-0112
Hegazy NH, Breitinger HG, Breitinger U. Kavalactones From Kava (Piper Methysticum) Root Extract as Modulators of Recombinant Human Glycine Receptors. Biol Chem. 2019 08 27;400(9):1205-1215. PubMed PMID: 31141476.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Kavalactones from Kava (Piper methysticum) root extract as modulators of recombinant human glycine receptors. AU - Hegazy,Nada Hany, AU - Breitinger,Hans-Georg, AU - Breitinger,Ulrike, PY - 2019/01/15/received PY - 2019/05/17/accepted PY - 2019/5/30/pubmed PY - 2020/2/18/medline PY - 2019/5/30/entrez KW - inhibition KW - ion channels KW - kavapyrones KW - neuronal receptors KW - plant extract SP - 1205 EP - 1215 JF - Biological chemistry JO - Biol Chem VL - 400 IS - 9 N2 - Roots of kava (Piper methysticum) plant are used in almost all Pacific Ocean cultures to prepare a drink with sedative, anesthetic and euphoric properties. One of the main active ingredients of the extract are kava lactones. Here, kava root CO2 extract and three kavalactones, DL-kavain, dihydrokavain and yangonin (isolated from whole extract by column chromatography) were tested for their inhibitory action on recombinant homomeric human α1 glycine receptors expressed in HEK293 cells. Kava CO2 root extract, as well as the individual components DL-kavain, dihydrokavain and yangonin inhibited glycine receptor activity in a dose-dependent manner. DL-kavain was the most potent inhibitor (IC50 = 0.077 ± 0.002 mm), followed by yangonin (IC50 = 0.31 ± 0.04 mm) and dihydrokavain (IC50 = 3.23 ± 0.10 mm) which were 4- and 40-fold less active than DL-kavain, respectively. Application of kava root extract did not reduce maximum currents, but increased EC50 of glycine. Simultaneous application of kava extract and strychnine showed additive inhibition, suggesting that binding of kavalactones and strychnine on the receptor is mutually exclusive. Overall, kavalactones exert a moderate inhibitory effect on the human α1 glycine receptor with DL-kavain being the most potent constituent. SN - 1437-4315 UR - https://www.unboundmedicine.com/medline/citation/31141476/Kavalactones_from_Kava__Piper_methysticum__root_extract_as_modulators_of_recombinant_human_glycine_receptors_ L2 - https://www.degruyter.com/document/doi/10.1515/hsz-2019-0112 DB - PRIME DP - Unbound Medicine ER -