Benefits of Hops
side effects and drug interactions
Hops (Humulus lupulus L.)

Hops, belonged to the family of Cannabacea, are believed to benefit conditions such
as anxiety and insomnia. A few animal studies have demonstrated its effects on
sleep quality or anxiety, but more advanced studies are definitely needed to prove its
possible uses for such conditions. On the other hand, some marketers have
suggested hops combined with valerian for maximum sedative or relaxing effects.
Hops contain phytoestrogen; intake of hopes may alter our hormonal conditions.

The female flowers of the hop plant have long been used as a preservative and a
flavoring agent in beer, but they are now being included in some herbal preparations
for women for "breast enhancement." [4] Most commercial hops extracts are
standardized to 5.2% bitter acids and/or to 4% flavonoids per dose.

POTENTIAL HEALTH BENEFITS OF HOPS

Hops have potential use or benefits on anxiety and insomnia.

The justification to use hops on anxiety and insomnia are mainly based on
experiences from our ancestors. There are extremely limited amounts of scientific
evidence to support the claim of its benefits on sleep quality, anxiety, insomnia or
related conditions:

Dr. K-H Schiller from Hoexter demonstrated that hop preparations reduced the
spontaneous locomotor activity, increased the ketamine-induced sleeping time and
reduced body temperature, confirming a central sedating effect. However, he couldn't
found any indication of anxiolytic activities of the preparation. Anyway, he believed that
hop oil and beta-bitter acid play a central role on sedating activities of his
preparations. [15]

Zanoli P, et al, from  University of Modena and Reggio Emilia, Italy noticed hop
extracts and its fraction both could prolong pentobarbital sleeping time, without
affecting the latency to the loss of the righting reflex in a study of rats. The effect was
dose-dependent, starting from a minimal dose of 10 mg/kg. Neither the extract nor
its alpha-acid fraction affected the locomotor activity in the open field test or exerted
an anxiolytic effect in rats submitted to the elevated plus-maze test. They also
observed an antidepressant activity of the extracts or faction prepared. [16]

Hops may have anti-inflammation effects and benefit arthritis.

Researchers from Germany showed the inhibitory effects of various ethanolic hop
extracts containing glucosides on COX-1 activity. The inhibitory potential of the
glucosides decreased with increasing length of the acyl side chain. [13]

Hops compounds may have potential chemopreventive activity against breast and
ovarian cancers.

Researchers from Oregon State University isolated a few flavonoids from hops and
tested for their antiproliferative activity in human breast cancer (MCF-7), colon cancer
(HT-29) and ovarian cancer (A-2780) cells in vitro. They found chalcone and
flavanone isomer of xanthohumol may have benefits of cutting cancer risks in the
study. [3,5] While, researchers from University of Illinois at Chicago analyzed the
anti-cancer activities of hops by studying its antioxidative activities and its effect on
the detoxification of a potentially toxic quinone (menadione). They found hop extract
has a strong induction of quinone reductose in Hepa 1c1c7 cells. Quinone
reductase is a detoxifying enzyme, protecting against quinone-induced toxicity. [7]

Finally, Japanese researchers suggested the anti-cancer activities of hop extracts
are related to the inhibition of the production of nitric oxide. It is known that nitric oxide
(NO) plays an important role in many inflammatory responses and is also involved in
carcinogenesis. They then demonstrated the inhibitory effect of extracts from
Humulus lupulus L. on both the production of NO and the expression of inducible NO
synthase (iNOS) in mouse macrophage RAW 264.7 cells. Thus, the chalcones,
including xanthohumol, significantly inhibited the production of NO by suppressing
the expression of iNOS. [8]

Hops have phyto-estrogen.

Researchers from King's College, UK, identified a potent phytoestrogen in hops,
8-prenylnaringenin, which has an activity greater than other established plant
estrogens. 8-Prenylnaringenin competed strongly with 17ss-estradiol for binding to
both the alpha- and ss-estrogen receptors. [4] Its strong estrogenic activity was also
reflected in its relative binding affinity to estrogen receptors from rat uteri.  This
phytoestrogen can also be detected in beer containing hops, but the levels are low.
[2]

Hops may have benefits of anti-microbial and anti-HIV-1 activities.

Researchers from Netherlands have shown the activities of hop extracts and oils
against Gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus) and
fungus (Trichophyton mentagrophytes var. interdigitale) by chromatographic
methods. [1]

It has been believed that xanthohumol contritbutes to most of the anti-microbial
benefits of hop extracts or related products. Xanthohumol was shown to inhibit the
Gram-positive bacteria Staphylococcus aureus and Streptococcus mutans. Antiviral
activity was demonstrated against bovine viral diarrhea virus, cytomegalovirus,
herpes simplex virus type 1 and 2 and human immunodeficiency virus 1. Inhibition of
two Trichophyton spp. was indicative of antifungal activity. Finally, Xanthohumol
potently inhibited the replication of Plasmodium falciparum, the causative agent of
malaria. This effect was linked to the inhibition of glutathione-mediated degradation
and detoxification of haemin, a by-product of the parasitic digestion of haemoglobin.
[14] Researchers from Chinese Academy of Sciences noticed that xanthohumol was
effective against HIV-1 in a study of C8166 lymphocytes. Xanthohumol inhibited HIV-1
induced cytopathic effects, the production of viral p24 antigen and reverse
transcriptase in C8166 lymphocytes at non-cytotoxic concentration. Xanthohumol
also inhibited HIV-1 replication in PBMC with EC50 value of 20.74 microg/ml. [9]

Side Effects, Drug Interactions and Warnings of Hops

Handling of hops may cause allergies (skin rash), dry cough and breathing
difficulties [6]. Hops may cause mild central nervous system depression with
symptoms of drowsiness, slowed breathing and thinking. In serious cases or
overdoses, its side effects may include seizure, hyperthermia, restlessness,
vomiting, and stomach disturbance [9]. It is unclear how intake of hops alters the
hormone-sensitive conditions such as certain types of cancers.

Because of its sedative action, user should not use hops together with other CNS
depressors including benzodiazepines, narcotics, barbiturates, and some herbal
sedatives. As it contains phyto-estrogen, users should avoid hops products if they
are on hormone replacement therapy or related medications. [11,12] Some animal
studies shows that hops may lower blood sugar levels. Hops may amplify the effects
of diabetic medications or other supplements (such as ginseng, bilberry, gymnema,
fish oil etc.) leading to hypoglycemia. Check with your doctor before taking any
supplements.

THIS ARTICLE IS FOR YOUR INFORMATION ONLY. DO NOT USE ANY SUPPLEMENT
WITHOUT YOUR DOCTOR'S RECOMMENDATION. ALL RIGHTS RESERVED ZHION
2008.

[1] Langezaal CR, Chandra A, Scheffer JJ. Antimicrobial screening of essential oils
and extracts of some Humulus lupulus L. cultivars.Pharm Weekbl Sci. 1992 Dec
11;14(6):353-6. [2] Milligan SR, et al, Identification of a potent phytoestrogen in
hops (Humulus lupulus L.) and beer. J Clin Endocrinol Metab. 1999
Jun;84(6):2249-52. [3] Miranda CL, et al, Antiproliferative and cytotoxic effects of
prenylated flavonoids from hops (Humulus lupulus) in human cancer cell lines.
Food Chem Toxicol. 1999 Apr;37(4):271-85. [4] Milligan SR et al, The endocrine
activities of 8-prenylnaringenin and related hop (Humulus lupulus L.) flavonoids.J
Clin Endocrinol Metab. 2000 Dec;85(12):4912-5. [5] Yilmazer M, et al, In vitro
biotransformation of xanthohumol, a flavonoid from hops (Humulus lupulus), by
rat liver microsomes.Drug Metab Dispos. 2001 Mar;29(3):223-31. [6] Spiewak R,
Dutkiewicz J.Occupational airborne and hand dermatitis to hop (Humulus lupulus)
with non-occupational relapses.Ann Agric Environ Med. 2002;9(2):249-52. [7]
Dietz BM, et al, Xanthohumol isolated from Humulus lupulus Inhibits
menadione-induced DNA damage through induction of quinone reductase. Chem
Res Toxicol. 2005 Aug;18(8):1296-305. [8] Zhao F, et al, Inhibitors of nitric oxide
production from hops (Humulus lupulus L.). Biol Pharm Bull. 2003
Jan;26(1):61-5. [9] Wang Q, et al, Xanthohumol, a novel anti-HIV-1 agent
purified from Hops Humulus lupulus. Antiviral Res. 2004 Dec;64(3):189-94. [10]
Kurasawa T, et al, Effect of humulus lupulus on gastric secretion in a rat
pylorus-ligated model. Biol Pharm Bull. 2005 Feb;28(2):353-7. [11] Overk CR, et
al, Comparison of the in vitro estrogenic activities of compounds from hops
(Humulus lupulus) and red clover (Trifolium pratense). J Agric Food Chem. 2005
Aug 10;53(16):6246-53. [12] Chadwick LR, et al, The pharmacognosy of Humulus
lupulus L. (hops) with an emphasis on estrogenic properties. Phytomedicine. 2006
Jan;13(1-2):119-31. Epub 2005 Jul 1. [13] Bohr G, et al, Anti-inflammatory
acylphloroglucinol derivatives from Hops (Humulus lupulus). J Nat Prod. 2005
Oct;68(10):1545-8. [14] Gerhauser C. Broad spectrum anti-infective potential of
xanthohumol from hop (Humulus lupulus L.) in comparison with activities of other
hop constituents and xanthohumol metabolites. Mol Nutr Food Res. 2005
Sep;49(9):827-31. [15] Schiller H, et al, Sedating effects of Humulus lupulus L.
extracts. Phytomedicine. 2006 Jul 21. [16] Zanoli P, et al, New insight in the
neuropharmacological activity of Humulus lupulus L. J Ethnopharmacol. 2005 Oct
31;102(1):102-6.
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