The effect of Hop ( Humulus lupulus L. ) on early menopausal symptoms and hot flashes: A randomized placebo-controlled trial

Aghamiri, Vida; Mirghafourvand, Mojgan; Mohammad‐Alizadeh‐Charandabi, Sakineh; Nazemiyeh, Hossein

doi:10.1016/j.ctcp.2015.05.001

Cited by 69 publications

(41 citation statements)

References 28 publications

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“…20,21 Many biological activities of hops have been connected to a series of bioactive prenylated flavanones and chalcones such as 6-prenylnarigenin (6-PN), 8-prenylnarigenin (8-PN), isoxanthohumol (IX), and xanthohumol (XH) (Figure 2). 22,23 The predominant prenylated chalcone, XH, has been shown to be an effective chemopreventive agent, inducing the detoxification enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1) in both in vitro and in vivo studies.…”

Section: Introductionmentioning

confidence: 99%

Hop (Humulus lupulus L.) Extract and 6-Prenylnaringenin Induce P450 1A1 Catalyzed Estrogen 2-Hydroxylation

Wang

Dunlap

Howell

et al. 2016

Chem. Res. Toxicol.

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Humulus lupulus L. (hops) is a popular botanical dietary supplement used by women as a sleep aid and for postmenopausal symptom relief. In addition to its efficacy for menopausal symptoms, hops can also modulate the chemical estrogen carcinogenesis pathway and potentially protect women from breast cancer. In the present study, an enriched hop extract and the key bioactive compounds [6-prenylnarigenin (6-PN), 8-prenylnarigenin (8-PN), isoxanthohumol (IX), and xanthohumol (XH)] were tested for their effects on estrogen metabolism in breast cells (MCF-10A and MCF-7). The methoxyestrones (2-/4-MeOE1) were analyzed as biomarkers for the nontoxic P450 1A1 catalyzed 2-hydroxylation and the genotoxic P450 1B1 catalyzed 4-hydroxylation pathways, respectively. The results indicated that the hop extract and 6-PN preferentially induced the 2-hydroxylation pathway in both cell lines. 8-PN only showed slight up-regulation of metabolism in MCF-7 cells, whereas IX and XH did not have significant effects in either cell line. To further explore the influence of hops and its bioactive marker compounds on P450 1A1/1B1, mRNA expression and ethoxyresorufin O-dealkylase (EROD) activity were measured. The results correlated with the metabolism data and showed that hop extract and 6-PN preferentially enhanced P450 1A1 mRNA expression and increased P450 1A1/1B1 activity. The aryl hydrocarbon receptor (AhR) activation by the isolated compounds was tested using xenobiotic response element (XRE) luciferase construct transfected cells. 6-PN was found to be an AhR agonist that significantly induced XRE activation and inhibited 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) induced XRE activity. 6-PN mediated induction of EROD activity was also inhibited by the AhR antagonist CH223191. These data show that the hop extract and 6-PN preferentially enhance the nontoxic estrogen 2-hydroxylation pathway through AhR mediated up-regulation of P450 1A1, which further emphasizes the importance of standardization of botanical extracts to multiple chemical markers for both safety and desired bioactivity.

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Section: Introductionmentioning

confidence: 99%

Hop (Humulus lupulus L.) Extract and 6-Prenylnaringenin Induce P450 1A1 Catalyzed Estrogen 2-Hydroxylation

Wang

Dunlap

Howell

et al. 2016

Chem. Res. Toxicol.

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“…More recently it was proposed to be used by women for the attenuation of menopausal symptoms [6,7]. Along these lines, we recently observed biological effects of the hops extract regarding ovariectomy-induced deterioration of the bone.…”

Section: Introductionmentioning

confidence: 94%

“…However, studies on biological consequences of this observation in human mammary gland tissue are not available, although three smaller trials on hops extracts in the management of menopausal discomfort are available. None of these studies measured mammary gland density, which would be indicative for unwanted side effects in the mammary gland following the application of the extract [6,19,20]. Overall human intervention studies provide mild evidence for clinical efficacy of hops extract in the management of menopausal symptoms, but did not address the issue of breast cancer risk.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of estrogenic potency of a standardized hops extract on mammary gland biology and on MNU-induced mammary tumor growth in rats

Keiler

Macejova

Dietz

et al. 2017

The Journal of Steroid Biochemistry and Molecular Biology

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Supplements with estrogenic activities are intensively investigated as potential alternatives for the treatment of menopausal symptoms. These investigations include studies on their safety regarding potential breast cancer risks. Therefore, the aim of this study was to assess whether or not a standardized hops (Humulus lupulus) extract, containing 0.42% of the estrogenic flavanone, 8-prenylnaringenin, would stimulate growth of methyl-nitrosourea (MNU) induced mammary cancer in ovariectomized (OVX) Sprague-Dawley (SD) rats or would impact on the proliferative activity within the normal mammary gland of Wistar rats. To induce tumorigenesis SD-rats received an intraperitoneal injection of 50 mg/kg body weight of MNU on postnatal days PND 50 and 52. 28 days later animals were OVX or were SHAM operated (positive control) and randomly allocated and maintained for 140 days on either a phytoestrogen-free placebo diet (SHAM and negative control) or on the hops fortified diet. For the investigations in the normal mammary gland young adult Wistar rats were bilaterally OVX and randomly allocated to a control group fed to a phytoestrogen-free diet, or to a diet supplemented either with E2-benzoate or the hops extract. As a major result, the tumor incidence was 15% (3 tumors totally) in OVX controls, whereas it was 85% (39 tumors totally) in SHAM operated positive controls. No tumors were detectable in the hops group. In addition, no estrogenic activity of the hops extract was detectable in uterus and liver of these animals. In investigations on the normal mammary gland, no impact of hops extract on the expression of estrogen dependent proliferation markers or of progesterone receptor became apparent. In conclusion, the lack of growth stimulation of MNU-induced breast cancer in OVX SD-rats and the lack of stimulation proliferative events in the normal mammary gland of OVX Wistar rats by standardized hops extracts provides an important piece of evidence regarding the safety of these extracts in the management of menopausal symptoms.

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“…The first time hop extract was administered in tablet form. For 90 days, the participants were taking one tablet containing 500 mg of extract standardized to 100 μg 8-PN daily [39]. The Greene scale (for the characteristics of early vasomotor symptoms) and reports written by patient (observations concerning hot flashes) were used to assess the effectiveness of hops in the treatment of early complaints of menopause, which mainly involve hot flashes.…”

Section: The Effectiveness Of 8-prenylnaringenin In Alleviating Symptmentioning

confidence: 99%

8-Prenylnaringenin from hop (Humulus lupulus L.) – a panacea for menopause?

2017

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8-Prenylnaryngenin (8-PN) is the strongest known phytoestrogen (PE). Its main source is the female inflorescences of hops (Humulus lupulus L.). 8-PN, which, in contrast to other PEs, is proven to have stronger activity and higher affinity for the α subtype of estrogen receptor (ER). Therefore, it may be an effective substitute for hormone replacement therapy (HRT). The studies in postmenopausal women have shown its particular effectiveness in reducing hot flashes. However, a strong stimulation of uterus by 8-PN may be associated with the occurrence of adverse effects (eg. bleeding) and increase the risk of carcinogenesis. The H. lupulus extracts preparations are currently supplements which makes control of the doses used and thus increases the occurrence of uncontrolled self-treatment difficult. This paper presents the current knowledge on 8-PN and discusses the potential risks associated with use of hops to alleviate the symptoms of menopause.

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The effect of Hop ( Humulus lupulus L. ) on early menopausal symptoms and hot flashes: A randomized placebo-controlled trial

Cited by 69 publications

References 28 publications

Hop (Humulus lupulus L.) Extract and 6-Prenylnaringenin Induce P450 1A1 Catalyzed Estrogen 2-Hydroxylation

Hop (Humulus lupulus L.) Extract and 6-Prenylnaringenin Induce P450 1A1 Catalyzed Estrogen 2-Hydroxylation

Evaluation of estrogenic potency of a standardized hops extract on mammary gland biology and on MNU-induced mammary tumor growth in rats

8-Prenylnaringenin from hop (Humulus lupulus L.) – a panacea for menopause?

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