Evidence that the β-acids fraction of hops reduces central GABAergic neurotransmission

Zanoli, Paola; Zavatti, Manuela; Rivasi, Marianna; Brusiani, F.; Losi, Gabriele; Puia, Giulia; Avallone, Rossella; Baraldi, Mario

doi:10.1016/j.jep.2006.07.008

Cited by 40 publications

(35 citation statements)

References 20 publications

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“…Though the alpha-bitter acids proved to be the most active constituents, the beta-bitter acids and the hop oil clearly contributed to the sedating activity of hop extracts (Schiller et al, 2006;Zanoli et al, 2007). According to Zanoli & Zanatti (2008), α-acids fraction can be considered as the major responsible constituent for the enhanced pentobarbital effect and for the antidepressant property observed after the administration of hop extract.…”

Section: Correlation Among Anxiolytic Activity and Chemical Constituentsmentioning

confidence: 98%

“…A research group had attributed the sedative effect of hops to 2-methyl-3-butene-2-ol, derived from hop constituents during storage but probably also formed in vivo by metabolization of α-acids. This compound, when intraperitoneally injected in rats, reduced motility without inducing a myorelaxant effect (Zanoli et al, 2007;Heinrich et al, 2004). However, according to Schiller et al (2006), this compound cannot be the constituent responsible for the sedating activity of hop preparations.…”

Section: Correlation Among Anxiolytic Activity and Chemical Constituentsmentioning

confidence: 99%

“…According to Zanoli & Zanatti (2008), α-acids fraction can be considered as the major responsible constituent for the enhanced pentobarbital effect and for the antidepressant property observed after the administration of hop extract. The β-acids fraction exerted an antidepressant activity as well, but reduced pentobarbital hypnotic activity (Zanoli et al, 2007;Zanoli & Zanatti, 2008). Hydroethanolic extract analyzed in this study exhibited anxiolytic activity (data not shown), which could be attributed to the high content of oxidized bitter acids, that seems to be high enough to contribute to anxiolytic activity of this extract and thus could be attributed to oxidized alfa-acids, such as, cohumulinone 5 and humulinone 7 derivatives presents in major concentration.…”

Section: Correlation Among Anxiolytic Activity and Chemical Constituentsmentioning

confidence: 99%

“…The main constituents found in essential oils of H. lupulus are humulene and myrcene (Zanoli et al, 2007;Chadwick, 2006). Prenylated flavonoids, other major components of this species, may be divided into two major groups, prenylated chalcones and prenylated flavanones such as, 6-prenylnaringenin, 8-prenylnaringenin and 8-geranylnaringenin (Nikolic et al, 2005;Vogel & Heilmann, 2008).…”

Section: Introductionmentioning

confidence: 99%

“…Content of α-acids, β-acids, desmethylxanthohumol, and xanthohumol can vary with cultivation and climatic conditions . Proanthocyanidins, also named condensed tannins (Li & Deinzer, 2006;Callemien & Collin, 2008), phenolic acids (ferulic and chlorogenic acids) (Zanoli et al, 2007;Li & Deinzer, 2006;Callemien & Collin, 2008) and flavonoid aglycones and glycosides, (Segawa et al, 2006;Arraez-Roman et al, 2006) are also found in H. lupulus. Proanthocyanidins exhibited a wide range of biological activities, such as antioxidants offering protection against cardiovascular and neurodegenerative diseases and immune disorders (Garcia-Villalba et al, 2006).…”

Section: Introductionmentioning

confidence: 99%

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Bitter acids from hydroethanolic extracts of Humulus lupulus L., Cannabaceae, used as anxiolytic

Negri¹,

Santi²,

Tabach³

2010

Rev. bras. farmacogn.

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RESUMO:Humulus lupulus L., Cannabaceae, é usada como sedativo e ansiolítico na medicina popular. O método de HPLC-DAD-ESI-MS n representa uma ferramenta poderosa para a análise de produtos naturais, desde que ela fornece o espectro de UV e informações estruturais sobre os constituintes da mistura. O objetivo deste trabalho foi o de caracterizar os constituintes encontrados no extrato hidroalcoólico. Os constituintes 1-9 foram tentativamente caracterizados através do UV/DAD e ionização por electrospray (MS/MS) depois da separação usando fase reversa, tempo de retenção e dados da literatura. Os principais compostos fenólicos (baseados na área dos picos) foram caracterizados como ácido hulupínico (9), coulupona (8), dois alfaácidos amargos oxidados (principais constituintes), um deles sendo um derivado da coumulinona oxidada (5) e o outro um derivado da humulinona oxidada (7), junto com uma procianidina B (3) e os flavonoides rutina (4) e o canferol-7-O-rutinosídeo (6). Esta planta conhecida devido às suas propriedades ansiolíticas e por ser um componente da cerveja, mostrou derivados oxidados de alfa-ácidos, como principais constituintes do extrato hidroalcoólico. Unitermos: Humulus lupulus, flavonoides glicosídeos, derivados de alfa-ácidos amargos oxidados, HPLC/DAD/MS/MS.ABSTRACT: Humulus lupulus L., Cannabaceae, is commonly used as light sedative and anxiolytics in folk medicine. HPLC-DAD-ESI-MS n represents a powerful tool for the analysis of natural products, since it can simultaneously provide a UV chromatogram and significant structural information about compounds in complex mixture. The aim of this work was characterize the constituents present in hydroethanolic extract. Compounds 1-9 were tentatively characterized on the basis of UV, MS/MS, after reversed phase separation, retention time and literature data. The main phenolic compounds (based on peak area) were characterized as hulupinic acid (9), cohulupone (8), two oxidized hop alfa-bitter acids (principal constituents), one being a oxidized cohumulinone (5) and the other an oxidized humulinone (7) derivatives, together with a procyanidin dimer B (3), flavonoids rutin (4) and kaempferol-7-O-rutinoside (6). This plant known, due to anxiolytic property and beer flavoring, showed oxidized hop bitter acids, as principal constituents, in its hydroethanolic extract.

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Section: Correlation Among Anxiolytic Activity and Chemical Constituentsmentioning

confidence: 98%

Section: Correlation Among Anxiolytic Activity and Chemical Constituentsmentioning

confidence: 99%

Section: Correlation Among Anxiolytic Activity and Chemical Constituentsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Bitter acids from hydroethanolic extracts of Humulus lupulus L., Cannabaceae, used as anxiolytic

Negri¹,

Santi²,

Tabach³

2010

Rev. bras. farmacogn.

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Physiological effects of hop and barley derived beer components

Li,

Pischetsrieder,

Gmeiner

2024

Lebensmittelchemie

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Humulus lupulus L.: Evaluation of Phytochemical Profile and Activation of Bitter Taste Receptors to Regulate Appetite and Satiety in Intestinal Secretin Tumor Cell Line (STC‐1 Cells)

Lela,

Carlucci,

Kioussi

et al. 2024

Molecular Nutrition Food Res

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ScopeInflorescences of the female hop plant (Humulus lupulus L.) contain biologically active compounds, most of which have a bitter taste. Given the rising global obesity rates, there is much increasing interest in bitter taste receptors (TAS2Rs). Intestinal TAS2Rs can have beneficial effects on obesity when activated by bitter agonists. This study aims to investigate the mechanism of action of a hydroalcoholic hop extract in promoting hormone secretion that reduces the sense of hunger at the intestinal level through the interaction with TAS2Rs.Methods and resultsThe results demonstrate that the hop extract is a rich source of bitter compounds (mainly α‐, β‐acids) that stimulate the secretion of anorexigenic peptides (glucagon‐like peptide 1 [GLP‐1], cholecystokinin [CCK]) in a calcium‐dependent manner while reducing levels of hunger‐related hormones like ghrelin. This effect is mediated through interaction with TAS2Rs, particularly Tas2r138 and Tas2r120, and through the activation of downstream signaling cascades. Knockdown of these receptors using siRNA transfection and inhibition of Trpm5, Plcβ‐2, and other calcium channels significantly reduces the hop‐induced calcium response as well as GLP‐1 and CCK secretion.ConclusionsThis study provides a potential application of H. lupulus extract for the formulation of food supplements with satiating activity capable of preventing or combating obesity.

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Evidence that the β-acids fraction of hops reduces central GABAergic neurotransmission

Cited by 40 publications

References 20 publications

Bitter acids from hydroethanolic extracts of Humulus lupulus L., Cannabaceae, used as anxiolytic

Bitter acids from hydroethanolic extracts of Humulus lupulus L., Cannabaceae, used as anxiolytic

Physiological effects of hop and barley derived beer components

Humulus lupulus L.: Evaluation of Phytochemical Profile and Activation of Bitter Taste Receptors to Regulate Appetite and Satiety in Intestinal Secretin Tumor Cell Line (STC‐1 Cells)

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