The 18+ Benefits of Hops (Humulus lupulus)

Hop On The Health-Train With Humulus Lupulus

 
beer hops
 

Have you ever wondered what gave beer its bitter, "hoppy" taste and aroma?

Well, the answer is hops. 😋

In this post, we'll be discussing the benefits of hops, how it works on the body, and some non-alcoholic benefits of beer

Contents:

  1. Basics
  2. Benefits of Hops
  3. My Experience With Hops
  4. Where To Get Hops
  5. Caveats
  6. Mechanism Of Action
  7. More Research

Basics

 
hops bud flowers
 

Hops (Humulus lupulus) has been used throughout history as a common way to preserve beer, giving it its aroma and flavor. R

Actually, beer was originally produced without the addition of hops, but it was observed that during summer months "unhopped" beer did not last as long as its "hopped" counterpart due to bacterial contamination. R

Hops is rich in flavanoids, Xanthohumol (XN) being one of the most abundant. R

Its polyhenol antioxidant activity is higher than green tea's polyphenols (at the same concentrations). R

It also has other important compounds in it (ie myrcene, humulene, and caryophyllene8PN, and THIAA). R

 
 

Benefits Of Hops

1. Protects The Brain

By increasing NRF2, NQO1, and HO1, XN can vastly help with neuroinflammation and aging of the brain. R R R 

It also helps with neuroinflammation by its ability to bind to GABA-A receptors and to stabilize calcium levels in the brain. R R R

It can reduce glutamate levels in the hippocampus. R

XN can help with Alzheimer's Disease (AD), by inhibiting beta-site APP cleaving enzyme 1 (BACE1, the protein that creates toxic beta-amyloid plaque) by increasing the neurotransmitter Acetylcholine (ACh) in the brain, via inhibiting acetylcholinesterase (ACh), R

XN can also help with stroke by reducing stroke size and improving behavior after stroke by reducing inflammation and improving hypoxia (such as increasing HIF-1alpha). R

XN also can induce neurons to grow (neurogenesis) and can increase Nerve Growth Factor (NGF). R R

XN can also help with cognition by lowering plasma palmitate levels in the brain. R

2. Reduces Anxiety

Independent of GABA activity, XN can improve anxiety by inhibiting glutamic acid decarboxylase (GAD). R R

For example, in a 4 week clinical pilot study, hops supplementation was able to reduce mild depression, anxiety and stress symptoms. R

3. Demolishes Insomnia

 
insomnia valerian hops
 

Hops can relieve insomnia and enhance circadian rhythms. R

By activating melatonin receptors, hops can decrease body temperature, helping improve sleep. R

In clinical trials, LZComplex3 (a combination of hops, lactiumZizyphus, magnesium and vitamin B6) can dramatically improve sleep quality. R

When combined with valerian root, hops effects on increasing deep sleep are even more effective. R R R R R R

The combination of valerian root + hops is as effective as benadryl (Diphenhydramine) at reducing sleep latency. R 

For example, NSF-3 (a combination of hops, valerian, and passion flower) showed in a randomized controlled trial to be as effective as ambien (zolpidem) at improving sleep. R

4. Prevents Obesity

XN can inhibit adipogenesis (increase fat cell death) and therefore can be used to prevent obesity. R R

For example, in animal models being fed a high-fat diet with hop extract, XN was able to prevent weight gain. R

XN's effects on eliminating fat cells can be enhanced by guggulsterone and honokiol. R R

XN also reduces overeating and water intake, as well as reducing the accumulation of white fat. R

5. Improves Mitochondrial Function

By reducing oxidative stress on the mitochondria, XN can improve mitochondrial function and metabolism. R

6. Combats Diabetes

XN enhances the metabolism of glucose and uptake of glucose into cells. R R R

For example, in obese mice XN supplementation in high doses could reduce weight and increase glucose metabolism. R

By acting on the farnesoid X receptor (FXR), XN can prevent diabetes. R

7. Enhances The Vascular System

Higher HDL cholesterol levels are associated with lower risks of cardiovascular disease, such as atherosclerosis. R

By inhibiting cholesteryl ester transfer protein (CETP) and enhancing apolipoprotein E (ApoE) activity, XN may be able to increase HDL levels. R R

For example, in Western-type diet-fed ApoE-deficient mice, XN was able to ameliorate atherosclerotic plaque formation. R

This may make hops beneficial for those who have ApoE4 alleles.

XN prevents oxidization of low-density lipoprotein (Ox-LDL). R R

When combined with α-tocopherol, XN is more effective at preventing Ox-LDL from copper. R

XN may be used in the prevention or treatment of anemia and disorders of microcirculation and coagulation. R

For example, hops may prevent blood clots (thrombosis) and arrhythmia. R R

8. Protects The Gut 

Hops protects the gut. R

It can reduces spasms in the gut. R

Tetrahydro iso-Alpha Acids (THIAA, which is found in hops) can prevent leaky gut by increasing zonula occludens-1 (ZO-1) and occludin, two key tight junctions proteins. R

9. Reduces Lungs Inflammation

 
 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5345976/

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5345976/

 

XN can protect the lungs against inflammation and acute lung injury. R

10. Supports The Liver

Hops may help protect the liver from developing Non-Alcoholic Fatty Liver Disease (NAFLD). R R

By activating NRF2 and regulating p53, hops can protect the liver from oxidative stress and oxygen-deprived damage. R R R

XN inhibits the synthesis of triglycerides (TG) in the liver. R 

XN also produces some of its benefits on cholesterol synthesis in the liver by its ability to bind to the liver X receptor (LXR-alpha). R

XN can also reduce liver scarring in animal models of Type 1 diabetes. R

11. Improves Kidney Function

Flavonols in hops may help with hyperuricemia and gout, as they can reduce uric acid levels. R

12. Enhances The Skin

By reducing inflammation, hops can improve:

  • Acne R
  • Allergic contact dermatitis R
  • Eczema R
  • Melanoma R
  • Skin Aging R
  • Skin Infections R
  • Skin Structure (collagens, elastin, and fibrillins) R
  • Sun Protection R
  • Wound Healing R

Hyaluronic acid (HA, found in hops) promotes collagen synthesis, repairs/hydrates tissues, and prevents wrinkle formation. R

HA combined with Vitamin E has synergistic effects on smoothing skin. R

13. Has Antimicrobial Properties

Hops has anti-microbial activity against:

  • Bacillus subtilis R
  • Bovine viral diarrhea virus (BVDV) 
  • Eimeria acervulina R
  • Eimeria tenella R
  • Hepatitis C virus (HCV) R
  • Herpes viruses (HSV-1, HSV-2 and CMV) R
  • HIV (strong - inhibits replication and lowers its effects on the immune system) R
  • Methicillin resistant Staphylococcus aureus (MRSA) R
  • Mycobacterium abscessus R
  • Mycobacterium smegmatis R
  • Mycobacterium tuberculosis R
  • Plasmodium falciparum (causative agent of malaria) R
  • Saccharomyces cerevisiae R
  • Staphylococcus aureus R
  • Staphylococcus epidermidis R
  • Streptococcus pyogenes R
  • Streptococcus bovis R
  • Streptococcus mutans R
  • Trichophyton spp R

Hops also inhibits some biofilms. R R

It kills most lactic acid bacteria (at least in beer), but not gram negative bacteria (like Escherichia coli). R R

It does not seem to affect the composition of intestinal microbiota (in rats, at least). R 

Interestingly, hops seems to have some insecticidal effects. R

14. Abolishes Cancer

 
hops cancer
 

XN can prevent and treat cancers by inhibiting the initiation and development of carcinogenesis, proliferation, migration, and angiogenesis, while inducting apoptosis. R R

Xn can prevent DNA damage. R R R R R

It inhibits angiogenesis (growth) in tumors by inhibition of VEGF and IL-8. R R R R

Hops shows beneficial activity in:

  • Brain Cancer R R
  • Breast Cancer R R R
  • Cervical Cancer R
  • Colon Cancer R R
  • Laryngeal Cancer R
  • Leukemia R
  • Liver Cancer R
  • Lung Cancer R
  • Ovarian Cancer R
  • Pancreatic Cancer R R
  • Prostate Cancer R
  • Skin Cancer R
  • Thyroid Cancer R

Linalool (can also be found in hops) and XN can enhance chemotherapy drugs and radiotherapies, making tumor cells more sensitive to these therapies. R R R

15. Acts On The Immune System

Hops has immunosuppressive effects and reduces TH1 cytokines, while increasing levels of IL-10. R R R

By modulation of the immune system, XN may help with arthritis. R

16. Protects Bones

Hops may prevent bone disease. R

XN inhibits bone resorption (osteoclastogenesis) and collagen loss as XF is metabolized into the estrogenic compounds prenylnaringenins. R R

17. Effects Sex Organs And Hormones

Xn can reduces growth of tissue in endometriosis. R

Hops can inhibit aromatase, an enzyme that converts androstenedione and estrone to estrogen. R

It's important to note that, XN can get converted in the body to 6-Prenylnaringenin (6PN) and 8-Prenylnaringenin (8PN), which are strong phytoestrogens, but THIAA can inhibit binding to the estrogen receptor alpha (ER-alpha and ER-beta). R R

8PN also can increase prolactin levels and breast size, but reduces Luteinizing hormone (LH) and follicle stimulating hormone (FSH). R R R

Nonetheless, studies have shown that hops itself (looking at it as a whole) binds well to estrogen receptors (ER-alpha) and may be beneficial for menopause. R

For example, numerous clinical trials have shown hops to significantly reduce the frequency of hot flashes. R R

18. Acts On The Thyroid

XN can stimulate the uptake of iodide in thyroid cells. R

XN can reduce T4 levels. R

My Experience With Hops

I've had beer before, but I'm gluten intolerant, so it sucked. 😅

I also don't drink alcohol

I've found combinations of hops+valerian root to be very effective at putting me to sleep and waking up rested. 

Hops in general makes me feel relaxed, probably due to its GABA receptor activity. R

Where To Get Hops

 
 

Beer is technically the most important dietary source of XN, but it's not that much anyway, so supplementing hops would have a higher level of XN. R

Beers with more hops, appear to have less damage on the liver vs those with less hops. R

It's important to note that the sedative effects of hops can also be found in non-alcoholic beers. R R

XN can be better absorbed into cells when taken with phosphatidylcholine. R

Caveats

Toxicological studies in humans and animals have revealed that XN has low toxicity. R R

For example, (1000 mg/kg body weight) in mice for 3 weeks showed no adverse effects. R

Chronic mega-doses may be related to infertility and liver inflammation. R 

XN treatment of male rats prior to mating significantly increases the sex ratio of male to female offspring. R

8-PN may adversely affect sperm. R

In 2 case studies, a hops-containing supplement (MenoCool) has shown to increase abdominal pain/cramps and vaginal hemorrhage in post-menopausal women. R

Hops may interact with drugs that metabolize via cytochrome P450. R

Occupational exposure to hop dust is associated with respiratory disease vs agricultural workers. R

Mechanism Of Action

Simple:

  • Increases ACh R
  • Increases Adiponectin R
  • Increases ALPL R
  • Increases AMPK R R
  • Increases ApoE R
  • Increases BGLAP R
  • Increases Caspase-3 R
  • Increases CDC2 R
  • Increases DR-4/5 R
  • Increases ERK1/2 R
  • Increases FXR R R
  • Increases GABA R
  • Increases GCLC R
  • Increases GCLM R
  • Incresaes GLUT2 R
  • Increases GSH R
  • Increases GSK3β R
  • Increases HIF1alpha R
  • Increases HO-1 R
  • Increases IL-2 (reduces in cancer) R R
  • Increases IL-10 R
  • Increases LXR R
  • Increases NGF R
  • Increases NQO1 R
  • Increases NRF2 R R
  • Increases PARP R
  • Increases Occludin R
  • Increases p21 R
  • Increases p53 R
  • Increases Raf-1 R
  • Increases Runx2 R
  • Increases SOD R
  • Increases Trx-1 R
  • Increases ZO-1 R
  • Reduces ABCG2 R
  • Reduces AChE R
  • Reduces α-glucosidase R
  • Reduces ApoB R
  • Reduces aP2 R R
  • Reduces Aromatase R
  • Reduces ASC R
  • Reduces BAC1 R
  • Reduces BCRP R
  • Reduces Caspase-1 R
  • Reduces C/EBP-α R R
  • Reduces CETP R
  • Reduces COX-2 R
  • Reduces CYP1A2 R
  • Reduces CYP2C8 R
  • Reduces CYP2C9 R
  • Reduces CYP2C19 R
  • Reduces CYP450 R
  • Reduces CXCR4 R
  • Reduces DGAT R R
  • Reduces EGFR R
  • Reduces GAD R
  • Reduces Glutamate R 
  • Reduces HMGB1 R
  • Reduces HES-1 R
  • Reduces ICAM1 R
  • Reduces IFN-γ R
  • Reduces IL-1β R
  • Reduces IL-6 R
  • Reduces IL-8 R
  • Reduces IL-12 R
  • Reduces iNOS R
  • Reduces KEAP1 R
  • Reduces MCP-1 R
  • Reduces MD2 R
  • Reduces MDR1 R
  • Reduces MMP1 R R
  • Reduces MMP2 R
  • Reduces MMP8 R
  • Reduces MMP9 R R
  • Reduces MPO R
  • Reduces NF-kb R R
  • Reduces NLRP3 R
  • Reduces NO R
  • Reduces NOTCH1 R R
  • Reduces PGE2 R
  • Reduces PPAR-γ (XN reduces it, THIAA increases it) R R R R
  • Reduces ROS (increases intracellularly in cancer cells) R
  • Reduces Selectin E R
  • Reduces STAT3 R
  • Reduces Survivin R
  • Reduces TG R
  • Reduces TLR4 R R
  • Reduces TNF-α R
  • Reduces TOPO1 R
  • Reduces Txnip R
  • Reduces VEGF R R
 
 http://onlinelibrary.wiley.com/doi/10.1002/jib.160/pdf

http://onlinelibrary.wiley.com/doi/10.1002/jib.160/pdf

 

Advanced:

  • The main constituents of hops include xanthohumol and tetrahydro-iso-alpha acids.R
  • XN may be converted into isoxanthohumol (IX) in the stomach which again may be converted to 8-Prenylnaringenin (8PN). R R R
  • XN can also undergo direct metabolic conversion to desmethylxanthohumol (DMX), which is later converted into either 6-prenylnaringenin (6PN) or into 8PN. R
  • It's estrogenic effect's half life is over 20 hours. R
  • XN can accumulate rapidly in intestinal cells and most of the XN molecules are bound to cellular proteins. R
  • When treated with XN, multi-drug resistance 1 (MDR1), epidermal growth factor receptor (EGFR), and signal transducer and activator of transcription 3 (STAT3) decreases in MCF-7/ADR cells, while the death receptor (DR)-4 and DR-5 expression increases, while augmenting the anticancer activity of tumor necrosis factor related apoptosis-inducing ligand (TRAIL). R R
  • It kills B-chronic lymphocytic leukemia cells by apoptosis, and apotopsis via increased intracellular ROS in K562 chronic myeloid cells.
  • It inhibits Bcr-Abl expression at both mRNA and protein levels inducing apoptosis in leukemic cells via modification of cysteine residues of the IκBα kinase and NFκB. R R R
  • XN reduces the expression of the LPS receptor components such as Toll-like receptor-4 (TLR4) and myeloid differentiation protein 2 (MD2) and results in the suppression of NFκB activation. R R
  • XN has profound immunosuppressive effects on T cell proliferation, development of IL-2 activated killer (LAK) cells, cytotoxic T lymphocytes (CTLs), and production of Th1 cytokines (IL-2, IFN-gamma and TNF-alpha). R
  • XN induces apoptosis of bone marrow-derived DCs via acid sphingomyelinase stimulation and caspase activation. R
  • β-Site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) mediates cleavage of β-APP and facilitates learning, memory, and synaptic plasticity and XN can inhibit BACE1. R R
  • XN does not show progestogenic or androgenic bioactivity, and the endocrine properties of hops and hop products are due to the estrogenic activity of 8PN. R
  •  XN possesses potent antiplatelet activity via inhibition of the PI3-kinase/Akt, p38 MAPK, and PLCγ2-PKC pathways, and the inhibition on thromboxane A2 formation and [Ca2+]. R
  • It inhibits suicidal erythrocyte death induced by oxidative stress and energy depletion. R
  • One of the mechanisms of antimicrobial action of hop extracts is thought to be due to changes in the permeability of the cell wall and membrane, which leads to the subsequent inhibition of respiration and of DNA and RNA synthesis. R
  • Hop extract at 5 μg/mL inhibited CYP2C8 (93%), CYP2C9 (88%), CYP2C19 (70%), and CYP1A2 (27%). R

More Research

  • As sister plants, marijuana (Cannabis sativa) and hops share similar genomes. R
  • Hops can be used as an eco-friendly repellent for insects/pests of stored foods. R