New insight in the neuropharmacological activity of Humulus lupulus L.

Zanoli, Paola; Rivasi, Marianna; Zavatti, Manuela; Brusiani, F.; Baraldi, Mario

doi:10.1016/j.jep.2005.05.040

Cited by 78 publications

(54 citation statements)

References 24 publications

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“…Sedative actions for both valerian and hops extract are reported, most frequently prolongation of sleeping time induced by sedatives or narcotics (Upton, 1999;Schiller, 2002;Zanoli et al, 2005). The mechanism of action has not been unequivocally determined so far.…”

Section: Discussionmentioning

confidence: 99%

A randomized, double blind, placebo‐controlled, prospective clinical study to demonstrate clinical efficacy of a fixed valerian hops extract combination (Ze 91019) in patients suffering from non‐organic sleep disorder

Koetter

Schrader²,

Käufeler

et al. 2007

Phytotherapy Research

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Valerian and hops are traditionally used as sleep aids. Since the fixed extract combination (Ze 91019) as a whole is considered the active compound, the clinical efficacy must be demonstrated for this extract combination. The present clinical study aimed to demonstrate superiority of the fixed extract combination in comparison with placebo in patients suffering from non-organic insomnia (ICD 10, F 51.0-51.2). Objective sleep parameters were registered by means of a transportable home recorder system (QUISI). The primary outcome was the reduction in sleep latency (SL2) which had to be prolonged at baseline (>/=30 min) as an inclusion criteria. The treatment period lasted for 4 weeks with either placebo, single valerian extract (Ze 911) or the fixed valerian hops extract combination (Ze 91019). The amount of the single valerian extract was identical to that amount contained in the fixed extract combination, i.e. 500 mg valerian extract siccum. In the extract combination 120 mg hops extract siccum was added. Both the extracts were prepared with 45% methanol m/m with a drug-extract ratio of 5.3:1 (valerian) and 6.6:1 (hops), respectively. The fixed extract combination was significantly superior to the placebo in reducing the sleep latency whilst the single valerian extract failed to be superior to the placebo. The result underlined the plausibility for adding hops extract to the valerian extract.

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Section: Discussionmentioning

confidence: 99%

A randomized, double blind, placebo‐controlled, prospective clinical study to demonstrate clinical efficacy of a fixed valerian hops extract combination (Ze 91019) in patients suffering from non‐organic sleep disorder

Koetter

Schrader²,

Käufeler

et al. 2007

Phytotherapy Research

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“…Hops showed significant inhibition of GAD activity (Awad et al, 2007). H. lupulus extracts induced the response of the ionotropic (GABAA receptors) (Aoshima et al, 2006) and its fraction containing α-acids: in dose-dependently prolonged pentobarbital induced sleeping time (Zanoli et al, 2005). Xanthohumol had been reported as modulator of the GABAA receptor response (Meissner & Haberlein, 2006).…”

Section: Correlation Among Anxiolytic Activity and Chemical Constituentsmentioning

confidence: 99%

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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“…16 Data from in vivo studies in rats have shown that a hops extract and its fraction containing alpha-bitter acids (humulones) exert significant sedative and antidepressant effects, whilst hops beta-acids (lupulones) appear to also exhibit antidepressant activity with fewer sedative effects, probably by affecting gamma-aminobutyric acid (GABA) neurotransmission activity. 17,18 Moreover, in vitro binding experiments on selected central nervous system (CNS) receptors using a fixed combination valerian-hops extract and its individual components have shown that hops interact with certain serotonin (5-HT6) and melatonin (ML1) receptor subtypes, which are involved in various CNS functions related to stress activity, relaxation, circadian rhythms and sleep. 19 Despite the popularity of hops, particularly in central Europe, as a sedative and mood-enhancing herbal medicinal product, there is a marked paucity of high-quality, placebo-controlled clinical studies on the efficacy of hops in reducing stress-related symptomatology.…”

Section: Introductionmentioning

confidence: 99%

Effects of a hops (Humulus lupulus L.) dry extract supplement on self-reported depression, anxiety and stress levels in apparently healthy young adults: a randomized, placebo-controlled, double-blind, crossover pilot study

Kyrou

Christou

Panagiotakos

et al. 2017

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The Humulus lupulus L. plant (hops) is used as a herbal medicinal product for anxiety/mood disorders. Our aim was to study the effects of a hops dry extract on self-reported depression, anxiety and stress levels in young adults. DESIGN: Apparently healthy young adults from our university completed the Depression Anxiety Stress Scale-21 (DASS-21) and those reporting at least mild depression, anxiety and stress were invited to complete the study intervention. This followed a randomized (1:1), placebo-controlled, double-blind, crossover design with two 4-week intervention periods (hops or placebo; two 0.2 gr capsules once daily) separated by a 2-week wash-out. Anthropometric measurements, DASS-21 assessments and measurements of morning cortisol plasma levels were performed at the beginning and the end of the 4-week treatment periods. RESULTS: 36 participants (Females/Males: 31/5; age: 24.7±0.5 years) completed the study intervention (attrition: 6/42). No significant changes in body weight and composition or morning circulating cortisol were noted with the hops or placebo. Significantly decreased DASS-21 anxiety, depression and stress scores were documented with hops (9.2±7.3 vs. 5.1±5.9, 11.9±7.9 vs. 9.2±7.4, and 19.1±8.1 vs. 11.6±8.1; all p values <0.05), which were significantly greater compared to those caused by the placebo (all p values <0.05). CONCLUSION: In otherwise healthy young adults reporting at least mild depression, anxiety HORMONES 2017, 16(2):171-180

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New insight in the neuropharmacological activity of Humulus lupulus L.

Cited by 78 publications

References 24 publications

A randomized, double blind, placebo‐controlled, prospective clinical study to demonstrate clinical efficacy of a fixed valerian hops extract combination (Ze 91019) in patients suffering from non‐organic sleep disorder

A randomized, double blind, placebo‐controlled, prospective clinical study to demonstrate clinical efficacy of a fixed valerian hops extract combination (Ze 91019) in patients suffering from non‐organic sleep disorder

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

Effects of a hops (Humulus lupulus L.) dry extract supplement on self-reported depression, anxiety and stress levels in apparently healthy young adults: a randomized, placebo-controlled, double-blind, crossover pilot study

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