Humulus lupulus L.

Last updated: 14 Apr 2017

Scientific Name

Humulus lupulus L.


Humulus cordifolius Miq., Humulus lupulus var. cordifolius (Miq.) Maxim. ex Franch. & Sav., Humulus lupulus var. lupulus, Humulus volubilis Salisb. [Illegitimate], Humulus vulgaris Gilib., Lupulus amarus Gilib., Lupulus communis Gaertn., Lupulus humulus Mill., Lupulus scandens Lam. [Illegitimate]. [1]

Vernacular Name

English European hop, hop, hops, [2] common hop, bine [3]
China Pi jiu hua [2][4]
North America Common hop(s), hop(s), houblon, lupulo [2].

Geographical Distributions

Humulus lupulus is originated from Gansu, North Sichuan, Xinjiang, North Africa, North and North East Asia, Europe, and East North America. [4]

Botanical Description

H. lupulus is a perennial plant that belongs to Cannabaceae family. [4]

The petiole is usually shorter than leaf blade; leaf blade 3-5(-7)-lobed, sometimes simple, 4-11 × 4-8 cm, abaxially glabrous or with scattered soft pubescence but without rigid spinulose hairs on veins, adaxially with few or no cystolith hairs marginally when young, base cordate, margin coarsely serrate, apex acute. [4]

Female flowers 2 per bract at least in middle of inflorescence; bracts imbricate into a globose spike. Infructescences are globose, 3-4 cm in diameter; bracts ovoid, 1.5-2 cm, dry, membranous, apex acute. Achenes are flat and included in bracts. [4]


H. lupulus is cultivated throughout China, especially in East Shandong (Qingdao) and Xinjiang. [4]

Chemical Constituent

Female inflorescences of H. lupulus was found to contain xanthohumol compounds (e.g. 5"-isopropyl-5"-hydroxydihydrofurano[2",3":3',4']-2',4-dihydroxy-6'-methoxychalcone; 5"-(2"'-hydroxyisopropyl)-dihydrofurano[2",3":3',4']-2',4-dihydroxy-6'-methoxychalcone; and dehydrocycloxanthohumol). [5]

H. lupulus was found to contain essential oil, humulones, and lupulones. [6]

H. lupulus was found to contain humulone, lupulone, cohumulone, colupulone, adhumulone, and adlupulone. [7]

H. lupulus was found to contain alpha-acids, beta-acids, prenylated chalcones, desmethylxanthohumol, and xanthohumol. [8]

Plant Part Used

Strobiles. [9]

Traditional Use

H. lupulus has been used since the Roman times in brewing beer and other alcoholic beverages and as a traditional gastrointestinal, nerve, and sedative tonic. H. lupulus is stated to possess sedative, hypnotic, antispasmodic, and topical bactericidal properties [10]. Traditional uses of H. lupulus include neuralgia, insomnia, excitability, topically for skin ulcerations, and primarily for restlessness associated with nervous tension [11].

Preclinical Data


Antimicrobial activity

Lupulone, humulone, isohumulone, and humulinic acid are active constituents isolated from H. lupulus extract that exhibited antibacterial properties in laboratory animals, specifically against Gram-positive bacteria. These constituents caused membrane leakage in Bacillus subtilis 168. [12]

Chloroform extract of H. lupulus cones was found to exhibit antibacterial activity against the Gram-positive bacteria (Bacillus subtilis andStaphylococcus aureus) and the fungus (Trichophyton mentagrophytes var.interdigitale), but almost no activity against the Gram-negative bacterium (Escherichia coli) and the yeast (Candida albicans) used in the screening. [13]

Trans-isohumulone isolated from H. lupulus was found to exhibit a greater antibacterial activity against Lactobacillus brevis compare to humulone, colupulone, and trans-humulinic acid. [14]

In vitro studies showed synergistic effects of H. lupulus constituents and several antibiotics in inhibiting Gram-positive bacteria and enhancing the inhibition of the antibiotics on Gram-negative bacteria. [15]

Antiviral activity

Xanthohumol, isoxanthohumol, and iso-alpha acids isolated from H. lupulus were found to have low to moderate antiviral activity against several types of viruses. [16]

Xanthohumol isolated from H. lupulus was found to inhibit the HIV-1 reverse transcriptase, [17] the viral cytopathic effects and production of HIV-1 p24 antigen in C8166 lymphocytes. In addition to this, it was also shown to have inhibitory effect on the viral replication in peripheral blood mononuclear cells [18].

Xanthohumol showed strong anti-BVDV (Bovine viral diarrheal virus, a surrogate for Hepatitis C virus) effect in a cell culture system. Apart from inhibition of the viral cytopathic effects, it inhibited BVDV E2 protein expression and reduced the viral RNA levels in a dose-dependent manner. When compared with drugs used for the treatment of chronic hepatitis C, xanthohumol’s antiviral effect was superior to ribavirin but weaker than alpha-interferon (IFN) [19]. Interestingly, the combination of xanthohumol and IFN exhibited stronger antiviral activity [20].

Sedative activity

CO2 extract of H. lupulus and its fraction containing alpha-acids was tested on the central nervous system of rats. Both tested substances were able to prolong pentobarbital sleeping time, without affecting the latency to the loss of the righting reflex. This effect was dose-dependent, starting from a minimal dose of 10 mg/kg. [21]

Sedative action of H. lupulus has been shown in many laboratory studies. H. lupulus has been reported to increase narcotic-induced sleeping time [22][23] and improve sleep disturbances when given in combination with other sedative herbs [11].

In vitro study reported that the H. lupulus component of Ze 91019 interact with serotonin and melatonin receptor subtypes which could explain its sedative effect. [24]

Estrogenic activity

The female flowers of H. lupulus have been reported to have a mild estrogenic activity, attributed to the presence of 8-prenylnaringenin (PN), isoxanthohumol, 6-PN and geranylated flavonoids. In in vitro study, 8-PN was reported to bind to both α- and β-estrogen receptors (ER) with higher affinity for the ER-alpha receptors [25]. 8-PN also has been regarded as an oestrogen agonist in female reproductive organs. It induced mitotic activity in the vaginal epithelium [26] and increased uterine weight of ovariectomised rats [27].

Anticancer activity

A few in vitro studies have been reported that flavonoid constituents found in H. lupulus (including xanthohumol, dehydrocycloxanthohumol and isoxanthohumol) had antiproliferative activity (dose dependent) in certain human breast cancer, [28][29] thyroid cancer, [30] and prostate cancer [31].

Flavanoid compounds isolated from H. lupulus was found to exhibit antiproliferative effect on various cancer cell lines may be due, in part, to inhibition of cytochrome P450 enzymes (including CYP1A1, CYP1B1 and CYP1A2) that activate carcinogens. [32]

Xanthohumol, isoxanthohumol [33] and 8-prenylnaringenin [34] isolated from H. lupulus were found to exhibit anticancer activity in human breast cancer cell lines by reduction of oestrogen formation (by inhibiting aromatase), cell proliferation and induce apoptosis.

In addition, xanthohumol isolated from H. lupulus has been shown in many in vitro studies to exert anticarcinogenic effects at different stages of carcinogenesis. It induced quinone reductase, an enzyme involved in detoxification of reactive metabolites, [35] protected DNA damage against procarcinogens, [36] act as an antioxidant and anti-inflammatory agent and a free radical scavenger [37][38].

Xanthohumol [39] and 8-prenylnaringenin [40] isolated from H. lupulus also inhibited induced angiogenesis by suppressing endothelial cell invasion, migration and proliferation.

In another study on human colon cancer cell lines, proanthocyanidins isolated from H. lupulus were reported to exert cytotoxic effect by increasing the levels of intracellular reactive oxygen species, protein carbonyls and cytoskeletal disruption. [41]

Antiobesity activity

In vivo studies reported that isohumolones isolated from H. lupulus were able to reduce body weight and plasma triglycerol levels. It was shown that isohumolones modulated lipid metabolism via activation of peroxisome proliferator-activated receptors (PPARs). [42][43][44][45]

Gastroprotective activity

The stimulating effects of H. lupulus on gastric secretion have been reported in laboratory animals [46][47]. H. lupulus reportedly exerts a strong spasmolytic action on smooth muscles when used as an extract [48].

Anaphrodisiac activity

An in vivo study reported that 8-prenylnaringenin isolated from H. lupulus exerted a dose-dependent anaphrodisiac effect on naïve male rats. [49]


No documentation.

Clinical Data

Clinical findings

Sedative activity

Human studies of the sedative action generally refer to H. lupulus being used in combinations with other sedative herbs. The efficacy of Valerian-H. lupulus combination (Ze 91019) in treating insomnia was shown in several studies. [50][51]

Estrogenic activity

Human studies evaluating the benefit of H. lupulus in treating menopausal symptoms showed that 100 micrograms of 8-prenylnaringenin daily for 12-16 weeks able to improve menopausal discomforts. [52][53]

Antiobesity activity

The weight reduction effect of isohumolones isolated from H. lupulus was further tested in human and showed that 48 mg isohumolones per day for 12 weeks significantly decreased body weight of prediabetic patients. [54]

Antidiabetic activity

Isohumolones were also reported to have anti-hypertensive and anti-glycaemic effects in human studies. [54]


Based on evidence that constituents contained in H. lupulus strobiles have estrogenic activity, use with caution in individuals susceptible to hormonally related cancers, such as breast, ovarian and prostate. [24]

Side effects

No documentation.

Pregnancy/Breast Feeding

No documentation.

Age limitation

No documentation.

Adverse reaction

No documentation.

Interaction & Depletion

Interaction with drug

A laboratory study reported that H. lupulus may affect the way certain medications are broken down in the body. This may alter the effects of these medications and possibly the dose(s) needed for treatment. Use with caution. [32]

Studies report that H. lupulus may cause sedation, which may enhance the effects of alcoholic beverages. These drugs include beer, wine, hard liquor, and mixed drinks. Use with caution. [55]

Studies report that H. lupulus may cause sedation, which may enhance the effects of these medications and possibly the dose needed for treatment. These drugs include alprazolam, diazepam, lorazepam, clorazepate dipotassium, chlordiazepoxide, oxazepam, buspirone, butabarbital, diphenhydramine, doxepin, hydroxyzine, meprobamate, amitriptyline, amobarbital, amoxapine, clomipramine, desipramine, doxepin, imipramine, nortriptyline, trimipramine, maprotiline, mirtazapine, trazodone, bupropion, venlafaxine, nefazodone, citalopram, fluoxetine, fluvoxamine, paroxetine, phenobarbital, pentobarbital, mephobarbital, secobarbital, thiopental, methohexital, sertraline, phenelzine, tranylcypromine, norethindrone, ethynodiol diacetate, norgestrel, norgestimate, ethinyl estradiol, drospirenone, desogestrel, levonorgestrel, conjugated estrogens, estradiol, estrone, esterified estrogens, estropipate, ethinyl estradiol, raloxifene, transdermal estradiol, vaginal estrogens, and isocarboxazid. Use with caution. [22][25][55][56][57]

Interaction with other Herbs

No documentation.


No documentation.


No documentation.

Poisonous Management

No documentation.

Line drawing

No documentation.


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