Ebselen's effect on Myeloma- PeopleBeatingCancer

Ebselen’s effect on Myeloma-

What is ebselen’s effect on myeloma? According to the study linked below, ebelson causes apoptosis in myeloma cells. Remember that the study is in vitro aka in a test tube.

What are the anti-cancer properties of ebselen?

Antioxidant Activity

Ebselen acts as a glutathione peroxidase (GPx) mimic, reducing hydrogen peroxide and organic peroxides to water and alcohol, thereby protecting cells from oxidative damage.
In cancer cells, where redox imbalance is a hallmark, ebselen’s modulation of reactive oxygen species (ROS) can induce cytotoxicity.

2. Inhibition of Thioredoxin Reductase (TrxR)

Ebselen inhibits TrxR, an enzyme crucial for maintaining redox homeostasis in cancer cells.
TrxR inhibition can lead to increased oxidative stress and apoptosis in cancer cells, which are more dependent on antioxidant systems than normal cells.

3. Modulation of Cellular Signaling Pathways

Ebselen has been shown to interfere with various signaling pathways, such as:
- NF-κB Pathway: Ebselen inhibits NF-κB, which plays a role in inflammation and cancer progression.
- PI3K/Akt Pathway: This pathway, often upregulated in cancer, can be suppressed by ebselen, inhibiting cell proliferation and survival.

4. Induction of Apoptosis

Ebselen can trigger apoptosis in cancer cells by disrupting mitochondrial function and increasing intracellular ROS levels.
It also modulates pro-apoptotic and anti-apoptotic proteins, such as Bax and Bcl-2, favoring cell death in tumors.

5. Anti-Metastatic Effects

Ebselen has shown the ability to inhibit matrix metalloproteinases (MMPs), which are enzymes involved in tumor invasion and metastasis.
By reducing MMP activity, ebselen may help prevent cancer cell migration and invasion.

6. Selective Cytotoxicity

Cancer cells often exhibit higher oxidative stress than normal cells, making them more susceptible to agents that disrupt redox balance. Ebselen selectively targets cancer cells by exploiting this vulnerability.

7. Synergistic Effects with Other Therapies

Ebselen has shown potential in combination therapies by enhancing the efficacy of traditional chemotherapeutic agents and reducing their side effects. Its antioxidant properties may also protect normal tissues from oxidative damage caused by radiation or chemotherapy.

8. Other Enzyme Inhibition

Ebselen inhibits cyclooxygenases (COX) and lipoxygenases (LOX), which are involved in inflammation and cancer progression.
It can also block protein tyrosine phosphatases (PTPs), which regulate signaling pathways involved in cell growth and differentiation.

Preclinical and Clinical Studies

While preclinical studies in cell lines and animal models demonstrate ebselen’s anticancer potential, clinical data are limited. More research is needed to validate its safety and efficacy in humans.

Challenges and Considerations

Bioavailability: Ebselen’s pharmacokinetics and delivery to tumor tissues need optimization.
Side Effects: Selenium-based compounds can exhibit toxicity at higher doses, necessitating careful dose optimization.

I am a long-term MM survivor. I have posted about dozens of non-conventional therapies for MM patients such as ebselen. Unfortunately, I have not found any sources or dosing information for it. Nothing on Amazon, nothing on the internet.

Have you heard anything about ebselen and cancer? Or myeloma? Email me at David.PeopleBeatingCancer@gmail.com with your questions or comments.

Thank you,

David Emerson

MM Survivor
MM Cancer Coach
Director PeopleBeatingCancer

Ebselen

“Ebselen (also called PZ 51, DR3305, and SPI-1005), is a synthetic organoselenium drug molecule with anti-inflammatory, anti-oxidant and cytoprotective activity. It acts as a mimic of glutathione peroxidase and can also react with peroxynitrite.^[1] It is being investigated as a possible treatment for reperfusion injury and stroke,^[2]^[3] hearing loss and tinnitus,^[4] and bipolar disorder.^[5]^[6]

Additionally, ebselen may be effective against Clostridium difficile infections^[7] and has been shown to have antifungal activity Aspergillus fumigatus.^[8]

Induction of Apoptosis in Human Multiple Myeloma Cell Lines by Ebselen via Enhancing the Endogenous Reactive Oxygen Species Production

“In this study, we examined the effect of ebselen on multiple myeloma (MM) cell lines in vitro. The results showed that ebselen significantly enhanced the production of reactive oxygen species (ROS) accompanied by cell viability decrease and apoptosis rate increase…

Due to its ability to scavenge reactive oxygen species (ROS), ebselen has been described as an anti-inflammatory and antioxidative agent which has potential chemoprevene effect on various diseases associated with oxidative stress. Previous studies had shown that ebselen can protect important organs or systems

(cardiovascular [2],
hepatic [3],
gastrointestinal [4, 5],
renal [2, 6], and
neural systems [7–9]) f

from lipid peroxidation and oxidative damage…

Ebselen Can Induce MM Cell Apoptosis

To test the effects of concentration and time of ebselen on apoptosis of MM cells, we measured apoptosis by flow cytometry using Annexin V-FITC/PI staining. It was found that ebselen was able to increase the percentages of apoptosis of cells in a concentration (Figure 2(a)) and time (Figure 2(b)) dependent manner (Figure 2(c)). When MM cells were treated with 10 μM ebselen for 24 hours, the apoptosis rate nearly doubled. The percentage of apoptotic cells was increased to 4 to 8 times when treated with 50 and 100 μM ebselen…

ebselen’s effect on myeloma ebselen’s effect on myeloma

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