Ebselen is a drug that contains selenium and has anti-inflammatory and antioxidant properties. It may prevent and improve memory, arthritis, and cancer. But, did you know that it is currently being examined in clinical trials as a treatment for bipolar disorder? Keep reading to find out more about the uses, side effects, and dosage of ebselen.
Disclaimer: By writing this post, we are not recommending this drug. Some of our readers who were already taking the drug requested that we commission a post on it, and we are simply providing information that is available in the scientific and clinical literature. Please discuss your medications with your doctor.
What Is Ebselen?
It has multiple effects on the body, such as preventing inflammation and protecting cells against the harmful effects of oxidants .
Mechanism of Action
Oxidants (hydroxyl radicals and hydrogen peroxide) can damage proteins, fats, and DNA. This speeds up aging and leads to age-related diseases, including stroke, Parkinson’s and Alzheimer’s disease .
Ebselen blocks the activity of oxidants and reduces cell damage via multiple mechanisms, such as the following:
- Mimics activity of an antioxidant enzyme (glutathione peroxidase): Ebselen converts harmful products made by oxidants back to harmless products (such as converting selenic acid to selenol). It also converts oxidants, such as hydrogen peroxide to water .
- Prevents cell death (apoptosis) caused by injury or toxic exposure by blocking proteins involved in apoptosis (thiol groups) .
- Crosses the blood-brain barrier and blocks an enzyme in the brain involved in the breakdown of acetylcholine (acetylcholinesterase), which may improve memory [2, 6].
- Irreversibly blocks an enzyme involved in cell communication and growth (Inositol Monophosphatase) in a similar way to lithium (approved treatment for bipolar disorder) .
- Prevents the spread of brain cancer cells (glioblastoma cells) by [7, 8]:
- Decreasing the production of pro-inflammatory compounds (cytokines IL-6, IL-8)
- Disrupting the cancer cells’ resistance to death
- Blocks an enzyme that helps tumors survive (glutamate dehydrogenase).
- Prevents iron overload in the heart, a major cause of heart failure .
- Decreases production of proteins involved in Alzheimer’s disease (amyloid precursor protein and β-secretase) and reduces toxic protein accumulation (amyloid plaques) in the brain .
- Increases serotonin production, which prevents the formation of tumors in the gut and affects mood .
Potential Uses of Ebselen
1) May Help with Stroke Recovery
In a study, 300 stroke patients were given either ebselen or placebo for 2-weeks. Ebselen greatly improved stroke symptoms compared to placebo after 1 month, if patients received it within 24 hours of the stroke .
In a study, 286 stroke patients received either ebselen or placebo for 2 weeks. Ebselen prevented brain damage from stroke 2 weeks, 1 month, and 3 months after treatment .
In rabbits, ebselen protected the brain from damage when it was given shortly after stroke .
2) May Help With Bipolar Disorder
Lithium is an effective treatment for bipolar disorder but has unwanted side effects and can be toxic even with normal doses .
In the first study of 16 healthy participants, ebselen mimicked the effects of lithium in the brain (by reducing levels of an enzyme, Inositol Monophosphatase). It also increased the recognition of emotions like disgust and happiness, reduced impulsivity, and improved decision-making, all important for bipolar disorder .
In another study of 20 healthy participants, ebselen reduced the glutamate and the enzyme Inositol Monophosphatase in the brain in a similar way to lithium .
Ebselen increased the recognition of positive emotions and decreased impulsive behavior in a study on 20 healthy participants, highlighting its potential to be used for bipolar disorder .
3) May Prevent Noise-Induced Hearing Loss
In a study, 83 healthy adults received ebselen at 200 mg, 400 mg, and 600 mg or placebo twice daily for 4 days before listening to music for 4 hours. Ebselen prevented noise-induced hearing loss better than placebo, with the most effective dosage being 400 mg .
4) May Reduce Impulsivity
Ebselen decreased impulsive actions during a gambling task in a study on 20 healthy participants. Ebselen-treated participants recognized positive emotions more than negative emotions, compared to placebo-treated participants, suggesting that ebselen may be used in impulsive and mood disorders .
5) May Improve Memory and Help With Alzheimer’s Disease
An imbalance between the antioxidants and oxidants is another early marker of Alzheimer’s disease. Ebselen decreased oxidative stress in mice. It also decreased the production of toxic proteins in the brain (by reducing the compounds needed to make Aβ proteins) .
6) May Help With Arthritis
Ebselen decreased the movement of white blood cells (polymorphonuclear leukocytes, T-lymphocytes) to joints and reduce inflammation in rats. These effects can be beneficial in treating arthritis, where joint inflammation can cause serious damage [23, 24, 25].
7) May Help With Diabetes
8) May Protect Against Osteoporosis
Osteoporosis is a disease where bones become fragile and more susceptible to damage.
In mice, ebselen reduced the breakdown of bone tissue by decreasing the production of cells that degrade bones .
9) May Help Fight Cancer
Ebselen reduced tumor growth by a remarkable 58% in mice with human pancreatic tumors .
Ebselen increased cancer cell death by increasing the production of harmful oxidants (reactive oxygen species). It also decreased tumor growth and invasion in kidney and pancreatic cancer cells [32, 30].
10) May Prevent Inflammation
Inflammation results in the production of harmful oxidants (free radicals) in the body. Since ebselen is an antioxidant, it can also help reduce inflammation .
It reduced inflammation in muscles and restored the function of small blood vessels in rats .
11) May Protect the Liver
Ebselen prevented liver injury caused by a bacterial toxin (staphylococcal enterotoxin B) by reducing inflammation and cell death in mice .
In multiple rat studies, ebselen prevented:
- Alcohol-induced liver damage by reducing oxidative stress and inflammation .
- Liver injury caused by activated liver immune cells (Kupffer cells) by decreasing the production of pro-inflammatory cytokines and oxidants [41, 42].
- Bile acid-induced liver injury .
12) May Protect Male Reproductive Organs
Manganese increases sperm abnormalities and decreases sperm motility and count. It also reduces the levels of testosterone and luteinizing hormone.
In rats, ebselen reversed the toxic effects of manganese on male fertility, thus protecting male reproductive organs .
Ebselen reduced cadmium-induced damage to testes in mice by decreasing oxidative stress .
13) May Prevent the Spread of Zika Virus
ZIKA virus infection increases oxidative stress and inflammation in mouse testes.
In mice, ebselen reduced oxidative stress and pro-inflammatory response in the testes. It also prevented the sexual spread of the ZIKA virus .
14) May Reduce Chemotherapy Side Effects
15) May Protect Against Malaria
In human cells, ebselen blocked the growth of a mosquito species that causes malaria (Plasmodium falciparum) .
In rat cells, ebselen reduced the ability of a mosquito species to cause malaria in mice (P. berghei) .
16) May Help Fight Bacterial Infections
In roundworms, ebselen was effective in treating a drug-resistant bacterial infection (methicillin-resistant S. aureus) better than current antibiotics (vancomycin and linezolid). It also showed increased the effects of antibiotics, helping to combat the infection [50, 51].
17) May Help Fight Fungal Infections
Ebselen was effective in rapidly killing fungi within 2 hours of treatment, including :
- Cryptococcus, which can be especially dangerous in people with a very weak immune response
In fact, it was more effective than common antifungal drugs (fluconazole, flucytosine, and amphotericin) in killing fungi in roundworms .
18) May Help Fight Viruses
- Herpes simplex type 1, which often causes cold sores (and more rarely genital herpes)
- Hepatitis C
- Vesicular stomatitis, which humans often contract from animals
19) May Preserve Stem Cells
Ebselen preserved the survival, shape, and function of stem cells in low temperatures by protecting them from harmful oxidants. It also improved stem cell function in human cornea tissues (the transparent part of the eye), indicating that ebselen is a useful preservative agent during cornea transplantations .
Ebselen is listed as a safe drug but without proven use by the National Institute of Health Clinical Collection .
Few patients in clinical trials reported drowsiness .
In yeast, ebselen may damage DNA and turn off genes that help reduce the damage .
High doses of ebselen can kill specific cells (HepG2 cells, hybridoma cells) .
In rabbits, ebselen enhanced the activity of tissue plasminogen activator (tPA), the current treatment for stroke .
Ebselen contains selenium, which can interact with different medications in various ways, listed below :
- Selenium stimulates the immune system, so drugs such as corticosteroids that suppress the immune system should be avoided.
- Selenium reduces blood clotting, so taking it with other anticoagulants like aspirin can increase bruising and bleeding.
- Selenium taken with beta-carotene, Vitamin C, and Vitamin E may decrease the effectiveness of medications that lower cholesterol levels (statins and niacin).
- Selenium may slow down how fast the body breaks down sedatives, increasing their effects and side effects.
Ebselen In Combination With Other Compounds
Ebselen and silver helped to overcome bacterial infections caused by drug-resistant bacteria .
For the prevention of hearing loss, patients were given 200 mg, 400 mg, or 600 mg twice daily .
Ebselen was administered as capsules at a total dose of 3600 mg in the span of 24 hours in clinical trials in healthy volunteers. This should not be taken as the therapeutic dose, as higher doses are used in healthy volunteers to investigate how safe the drug is and how it is metabolized in the body [16, 21].
Limitations and Caveats
Most studies on ebselen were done on animals.
Although ebselen is a clinically safe drug, there is no real proof of use yet.