Health Care Professional Information

Scientific Name
Humulus lupulus L.
Clinical Summary

Hops are the female inflorescences of the plant Humulus lupulus L. They are used primarily in beer brewing to add bitterness and flavor. Hops is also used as an herbal medicine for mood disturbance and insomnia (1) and to treat menopausal symptoms. In vitro studies have shown that hops has chemopreventive (2), (3), (4) antitumor (5), antiangiogenic (6), anti-inflammatory (19) and antidiabetic (7) properties. Hops also reduces hyperlipidemia (8) and obesity (9) in mice.

In human studies, a hops-valerian combination product improved sleep quality (10) (16), and insulin sensitivity in patients with type-2 diabetes (7). Data from an observational study suggest benefits of a combination of hops, rosemary extract and oleanolic acid in reducing arthritic pain (11). However, it is not clear whether hops alone would exert similar effects.
A hops extract was shown to alleviate hot menopausal symptoms (13) (17), and may improve bone health (18) in postmenopausal women.

Derivates of hops have phytoestrogenic effects (7) (12); until more research is done, patients with hormone-sensitive cancers should avoid it.

Food Sources

Female inflorescences of Humulus lupulus L.

Purported Uses
  • Arthritis
  • Fibromyalgia
  • Insomnia
  • Menopausal symptoms
  • Diabetes
Constituents
  • Chalcones: Xanthohumol and desmethylxanthohumol
  • Flavonones: Isoxanthohumol, 8-prenylnaringenin, 6-prenylnaringenin
  • Isohumulones
    (2) (7) (8)
Mechanism of Action

Isomerized hops extracts (IHEs) increase plasma HDL levels and decrease atherosclerosis index (AI) in mice on high fat, high cholesterol diet via PPAR-alpha activation (14). These extracts also reduced plasma triglyceride levels and induced hepatomegaly (8). Other studies show IHE rich in isohumulone can inhibit PGE2 production and reduce the formation aberrant crypt foci in the colon of mice. Xanthohumol, a flavonoid from hop exhibits antiangiogenic effect by inhibiting the NF-kB and Akt pathway (6). A product containing hops extract reduces levels of C-reactive protein in patients with inflammatory diseases (12). Prenyl flavonoids from hops, xanthohumol, isoxanthohumol, and 8-prenylnaringen (8-PN) inhibit aromatase activity and breast cancer cell proliferation, and increase breast cancer cell apoptosis in vitro (5). They also inhibited prostate cancer cell proliferation in vitro (3). However, isoxanthohumols are converted in the distal human gut into the phytoestrogen 8-prenylnaringen (8-PN) via the action of intestinal microflora (12). This process also occurs in the liver and is regulated by the cytochrome P450 enzymes (15).

Pharmacokinetics

Isoxanthohumol, a prenylated flavonoid in hops, is converted in the distal human gut into the phytoestrogen 8-prenylnaringen (8-PN) via the action of intestinal microflora. Isoxanthohumols are excreted in the feces and urine (12).

Contraindications

Patients with hormone-sensitive cancer should avoid hops extracts due to their phytoestrogenic effects (7) (12).

Herb-Drug Interactions
  • Cytochrome P450 substrates:  Drugs that induce CYP1A2 may increase the estrogenic effect of hops extracts (15).
  • Paracetamol: Some hops species may slow clearance of paracetamol, thereby increasing its analgesic effects (20)
Herb Lab Interactions
  • Isomerized hops extracts (IHEs) may increase plasma HDL levels (14).
  • Hops extract in combination with rosemary extract and oleanolic acid may reduce C-reactive protein in patients presenting with elevated levels (11).
Literature Summary and Critique

Lukaczer D, Darland G, Tripp M, et al. A pilot trial evaluating Meta050, a proprietary combination of reduced iso-alpha acids, rosemary extract and oleanolic acid in patients with arthritis and fibromyalgia. Phytother Res. Oct 2005;19(10):864-869.
An eight-week observational trial of a proprietary blend (Meta050) of hops extract, rosemary extract, and oleanolic acid was conducted in patients suffering from osteoarthritis, rheumatoid arthritis and fibromyalgia. A dose of 440 mg of the product Meta050 was given three times a day for the first 4 weeks and then changed to 880mg twice per day in most patients for the concluding 4 weeks. Fifty-four patients completed the trial. There was a statistically significant reduction in pain post-treatment for the OA patients. Pain scores decreased 50% (P<0.0001) as measured by standard visual analog (VAS), and 40% (P<0.0001) as measured by the arthritis impact measurement scale (AIMS2). There was no significant improvement in fibromyalgia scores. In patients who initially presented with elevated high-sensitivity C-reactive protein, a decreasing trend was observed. The authors note that these observations suggest that 440mg three times per day of Meta050 may provide pain-relieving effects in osteoarthritis patients. Financial support for the study was provided by the manufacturer of Meta050.

Heyerick A, Vervarcke S, Depypere H, Bracke M, et al. A first prospective, randomized, double-blind, placebo-controlled study on the use of a standardized hop extract to alleviate menopausal discomforts. Maturitas. May 20 2006;54(2):164-175.
Sixty-seven women with menopausal symptoms participated in a 12-week prospective, randomized, double-blind, placebo-controlled trial using supplemental hops extract standardized to 100 or 250mcg 8-prenylnaringen (8-PN). Patient responses were assessed by means of a modified Kupperman Index (KI) and a patient questionnaire. The daily dose of 100ug 8-PN significantly reduced discomfort and complaints compared to placebo at 6 weeks (P=0.023), but not at 12 weeks (P=0.086). A statistically significant decrease in the incidence of hot flushes was evident in both treatment groups after 6 weeks compared to placebo. A dose-response relationship could not be established as a 2.5 fold increase in dose was less active than the lower dose after 6 and 12 weeks, and the 250mcg dose was only marginally more effective than placebo. The authors suggest that hops extracts may be beneficial for hot flash management. The study was designed and funded by the manufacturers of the proprietary supplement MenoHop used in the study.

Dosage (Inside MSKCC Only)
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References
  1. Piersen CE. Phytoestrogens in botanical dietary supplements: implications for cancer. Integr Cancer Ther. Jun 2003;2(2):120-138.
  2. Dietz BM, Kang YH, Liu G, et al. Xanthohumol isolated from Humulus lupulus Inhibits menadione-induced DNA damage through induction of quinone reductase. Chem Res Toxicol. Aug 2005;18(8):1296-1305.
  3. Delmulle L, Bellahcene A, Dhooge W, et al. Anti-proliferative properties of prenylated flavonoids from hops (Humulus lupulus L.) in human prostate cancer cell lines. Phytomedicine. Nov 2006;13(9-10):732-734.
  4. Nozawa H, Nakao W, Zhao F, Kondo K. Dietary supplement of isohumulones inhibits the formation of aberrant crypt foci with a concomitant decrease in prostaglandin E2 level in rat colon. Mol Nutr Food Res. Aug 2005;49(8):772-778.
  5. Monteiro R, Faria A, Azevedo I, Calhau C. Modulation of breast cancer cell survival by aromatase inhibiting hop (Humulus lupulus L.) flavonoids. J Steroid Biochem Mol Biol. Jun-Jul 2007;105(1-5):124-130.
  6. Albini A, Dell'Eva R, Vene R, et al. Mechanisms of the antiangiogenic activity by the hop flavonoid xanthohumol: NF-kappaB and Akt as targets. FASEB J. Mar 2006;20(3):527-529.
  7. Yajima H, Ikeshima E, Shiraki M, et al. Isohumulones, bitter acids derived from hops, activate both peroxisome proliferator-activated receptor alpha and gamma and reduce insulin resistance. J Biol Chem. Aug 6 2004;279(32):33456-33462.
  8. Shimura M, Hasumi A, Minato T, et al. Isohumulones modulate blood lipid status through the activation of PPAR alpha. Biochim Biophys Acta. Sep 5 2005;1736(1):51-60.
  9. Yajima H, Noguchi T, Ikeshima E, et al. Prevention of diet-induced obesity by dietary isomerized hop extract containing isohumulones, in rodents. Int J Obes (Lond). Aug 2005;29(8):991-997.
  10. Morin CM, Koetter U, Bastien C, Ware JC, Wooten V. Valerian-hops combination and diphenhydramine for treating insomnia: a randomized placebo-controlled clinical trial.Sleep. Nov 1 2005;28(11):1465-1471.
  11. Lukaczer D, Darland G, Tripp M, et al. A pilot trial evaluating Meta050, a proprietary combination of reduced iso-alpha acids, rosemary extract and oleanolic acid in patients with arthritis and fibromyalgia. Phytother Res. Oct 2005;19(10):864-869.
  12. Possemiers S, Bolca S, Grootaert C, et al. The prenylflavonoid isoxanthohumol from hops (Humulus lupulus L.) is activated into the potent phytoestrogen 8-prenylnaringenin in vitro and in the human intestine. J Nutr. Jul 2006;136(7):1862-1867.
  13. Heyerick A, Vervarcke S, Depypere H, Bracke M, De Keukeleire D. A first prospective, randomized, double-blind, placebo-controlled study on the use of a standardized hop extract to alleviate menopausal discomforts. Maturitas. May 20 2006;54(2):164-175.
  14. Miura Y, Hosono M, Oyamada C, Odai H, Oikawa S, Kondo K. Dietary isohumulones, the bitter components of beer, raise plasma HDL-cholesterol levels and reduce liver cholesterol and triacylglycerol contents similar to PPARalpha activations in C57BL/6 mice. Br J Nutr. Apr 2005;93(4):559-567.
  15. Guo J, Nikolic D, Chadwick LR, Pauli GF, van Breemen RB. Identification of human hepatic cytochrome P450 enzymes involved in the metabolism of 8-prenylnaringenin and isoxanthohumol from hops (Humulus lupulus L.). Drug Metab Dispos. Jul 2006;34(7):1152-1159.
  16. Dimpfel W, Suter A. Sleep improving effects of a single dose administration of a valerian/hops fluid extract - a double blind, randomized, placebo-controlled sleep-EEG study in a parallel design using electrohypnograms. Eur J Med Res. 2008 May 26;13(5):200-4.
  17. Erkkola R, Vervarcke S, Vansteelandt S, et al. A randomized, double-blind, placebo-controlled, cross-over pilot study on the use of a standardized hop extract to alleviate menopausal discomforts. Phytomedicine. 2010 May;17(6):389-96.
  18. Holick MF, Lamb JJ, Lerman RH,et al. Hop rho iso-alpha acids, berberine, vitamin D3 and vitamin K1 favorably impact biomarkers of bone turnover in postmenopausal women in a 14-week trial. J Bone Miner Metab. 2010 May;28(3):342-50.
  19. Akazawa H, Kohno H, Tokuda H, et al. Anti-inflammatory and anti-tumor-promoting effects of 5-deprenyllupulonol C and other compounds from Hop (Humulus lupulus L.). Chem Biodivers. 2012 Jun;9(6):1045-54.
  20. Jakovljevic V, Popovic M, Raskovic A, et al. Effect of aroma and magnum hops extracts and paracetamol on antioxidant liver parameters in mice. Eur J Drug Metab Pharmacokinet. 2009 Jan-Mar;34(1):37-41.

Consumer Information

How It Works

Bottom Line: Hops extracts have not been shown to have anticancer effects in humans.

Hops are traditionally used in beer brewing as flavoring agents. Studies done in laboratory and in animals have shown that hops extract has anticancer effects. It has not been studied in cancer patients. Human studies with hops indicate benefits for patients with type-2 diabetes, osteoarthritis, and insomnia. Hops extracts may have estrogenic effect and has been used to reduce hot flashes in menopausal women. Women with hormone-sensitive cancer should avoid hops until more research is done.

Purported Uses
  • Arthritis
    When used in combination with rosemary leaf and oleanolic acid, hops extract reduced pain in patients with osteoarthritis. More studies are needed.
  • Sleeping aid
    When used in combination with valerian, hops extracts improved sleep in patients with mild insomnia. More data are needed.
  • Menopausal symptoms
    Hops extract decreased hot flashes in menopausal women but further studies are warranted.
  • Diabetes
    In a small study, hops extract lowered blood glucose and improved insulin sensitivity in patients with type-2 diabetes. Larger studies are required to confirm such effects.
Research Evidence

Arthritis
In an 8-week observational trial, patients with osteoarthritis, rheumatoid arthritis and fibromyalgia were given a combination of hops extract, rosemary extract and oleanolic acid in dosages beginning at 440mg three times a day for the first 4 weeks and increased to 880mg twice per day, in most patients, for the final 4 weeks. Researchers noted a significant decrease in pain for the osteoarthritis patients after the treatment period.

Menopausal symptoms
Sixty-seven women suffering from hot flashes were given hops extract containing either 100 or 250mcg active ingredient. Women who received 100mcg active ingredient had significantly reduced discomfort and complaints compared to those in placebo group Both groups experienced a significant decrease in hot flashes at 6 weeks. The higher dose of active ingredient was less effective after both 6 and 12 weeks.

Do Not Take If
  • You have hormone-sensitive cancer.
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