Positive allosteric modulation of native and recombinant GABAA receptors by hops prenylflavonoids

European Journal of Pharmacology
Ali Y BenkheroufM Uusi-Oukari

Abstract

Hops are a major component of beer that is added during brewing. In addition to its wide range of bioactivity, it exhibits neuroactive properties as a sedative and sleeping aid. The compounds responsible for this activity are yet to be revealed and understood in terms of their pharmacological properties. Here we evaluated the potential of several hops flavonoids in modulating the GABAergic activity and assessed their selectivity to GABAA receptors subtypes. GABA-potentiating effects were measured using [3H]ethynylbicycloorthobenzoate (EBOB) radioligand binding assay in native and recombinant α1β3γ2, α2β3γ2 and α6β3δ receptors expressed in HEK293 cells. Flumazenil sensitivity of GABA-potentiating effects and [3H]Ro 15-4513 binding assay were used to examine the flavonoids binding to benzodiazepine site. The prenylflavonoids xanthohumol (XN), isoxanthohumol (IXN) and 8-prenylnaringenin (8PN) potentiated GABA-induced displacement of [3H]EBOB binding in a concentration-dependent manner. The IC50 for this potentiation in native GABAA receptors were 29.7 µM, 11.6 µM, 7.3 µM, respectively. In recombinant receptors, the sensitivity to prenylflavonoid potentiation of GABA-induced displacement of [3H]EBOB binding followed the order α6β3δ...Continue Reading

Citations

Sep 18, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Tomasz TroninaAgnieszka Bartmańska
Nov 13, 2020·Frontiers in Neuroscience·Ali Y BenkheroufMikko Uusi-Oukari
Jul 3, 2021·Nutrients·Gustavo Ignacio Vazquez-CervantesBenjamín Pineda

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