Thymoquinone is the key compound in oil extracted from black cumin seed/nigella seed.

Thymoquinone’s Inflammatory Response Support Properties

Having a healthy inflammatory response is integral to the body’s defense mechanism against injury or infection. However, it can prove damaging when it occurs in healthy tissues for a prolonged period or in an imbalanced manner. Inflammation is a well-known symptom of several adverse health conditions, including cardiovascular disorders, gastrointestinal conditions, autoimmune diseases, metabolic diseases, neurological conditions, and lung diseases. 
Thymoquinone, the primary constituent present in Nigella sativa or black cumin seeds,is known for its antioxidant and immunomodulatory properties, which help maintain the body’s natural inflammatory response.* This article explains thymoquinone’s inflammatory response support properties, how it exerts its beneficial effects through several molecular pathways, and why you should consider including an advanced thymoquinone supplement in your diet. Use the links below to jump ahead to different topics on the page.    

Pharmacological Properties of Thymoquinone

Chemically, thymoquinone is 2-methyl-5-isopropyl-1, 4-benzoquinone — it is the most prominent bioactive constituent of the Nigella sativa seeds. Nigella or black cumin seeds contain several other beneficial constituents, including: 

  1. Terpenes. These are aromatic compounds with potential therapeutic benefits. The main terpenes in Nigella sativa seeds are p-cymene, α-thujene, α-pinene, β-pinene, thymoquinone, γ-terpinene, and sabinene.
  1. Alkaloids. Black cumin seed has two different types of alkaloids: isoquinoline alkaloids (nigellicimine, nigellicimine n-oxide) and pyrazol alkaloids (nigellidine, nigellicine). Alkaloids are known for their wide range of biological activities, including immunomodulatory and neuroprotective effects.*
  1. Phytosterols. Beta-sitosterol is the most abundant phytosterol in black cumin, followed by stigmasterol. These plant sterols may help maintain cardiovascular health and immune system function.*
  1. Tocols. β-tocotrienol and γ-tocopherol are forms of vitamin E and are among the key tocols present in thymoquinone, offering antioxidant protections and supporting skin and cellular health.* 
  1. Polyphenols. Black seed oil contains more polyphenols (α-tocopherol, β-tocopherol, γ-tocopherol) than most edible oils (except olive oil), which contribute significantly to its antioxidant properties.*

However, the therapeutic benefits of the seeds are primarily attributed to thymoquinone’s antioxidative and immunomodulatory effects.* The following table highlights thymoquinone’s primary pharmacological properties that contribute to its health benefits. 

Pharmacological Properties of Thymoquinone

  • Antioxidative effects1: The antioxidative effects of thymoquinone: 
    1. Enhances the body’s natural defense system.* 
    2. Induces beneficial apoptosis or cell death.* 
    3. Helps maintain a normal Akt/PKB signaling pathway, a critical regulator of cell survival and metabolism.* 
    4. Up-regulates antioxidant mechanisms that increase the activities of antioxidant enzymes, such as superoxide dismutase, catalase, and glutathione peroxidase.*
  • Immunomodulatory effects2: Thymoquinone’s immunomodulatory effects: 
    1. Helps prevent the biosynthesis of essential mediators in inflammatory processes.* 
    2. Limits the production of proinflammatory cytokines, such as interleukins and TNF-α.* 

The following sections further explain how thymoquinone’s inflammatory response support properties are exerted through molecular signaling pathways to promote various health functions.*

Thymoquinone’s Role in Down-Regulating Inflammatory Signaling Pathways*

Thymoquinone exerts its beneficial immunomodulatory effects through various molecular pathways*, particularly inflammatory signaling pathways, including:

  1. Activation of cyclooxygenase-2 (COX-2): Thymoquinone induces the expression of COX-2, an enzyme involved in the inflammatory response, through the PI3K-AKT signaling pathway.* 
  2. Nuclear factor erythroid 2-related factor 2 (Nrf2): Thymoquinone activates the Nrf2 pathway, thereby enhancing the body’s antioxidant defense system.*
  3. Phosphatidylinositol 3-kinase/protein kinase B (PI3K/AKT): Thymoquinone decreases the expression of PI3K/protein kinase B, a signmaling pathway that plays a role in cell growth and inflammatory responses.*
  4. Nuclear factor kappa-light-chain-enhancer of activated B (NF-Κβ): Thymoquinone inhibits the NF-Kβ signaling pathway, thereby reducing inflammatory cytokine production and protecting cellular health.*

How do Thymoquinone’s Inflammatory Response Support Properties Address Various Health Conditions? 

Inflammatory responses are a normal pathological process that starts in the tissues and organs of the body. Thymoquinone’s inflammatory response support properties exerted through complex signaling pathways and molecular mechanisms help address the underlying oxidative stress that causes inflammation.*

There is experimental evidence that thymoquinone increases the expression level of glutathione (GSH), the body’s master antioxidant.* GSH further helps limit reactive oxygen species (ROS)-induced oxidative stress damage and the associated inflammation. 

The capability of thymoquinone to support the body’s natural inflammatory response is primarily exerted through: 

  • Increasing the levels of Cyclooxygenase-2 (COX-2)*: COX-2, in turn, participates in the inflammatory response of peripheral blood inflammation. COX-2 is closely related to the expression of growth factors and inflammatory factors in the cells. 
  • Inhibiting MAPK and NF-Κβ signaling*: Thymoquinone limits the NF-Κβ signaling gene expression and limits the expression of inflammatory factors, such as IL-1β, TNF-α, IFN-γ, and IL-6, to promote healthy inflammatory responses.* 

The following table highlights thymoquinone’s inflammatory response support properties that promote various health functions.  

Thymoquinone’s Inflammatory Response Support Properties to Address Health Conditions

  • Cardiovascular disorders: Most cardiac and peripheral vascular conditions are caused due to the deposition of lipids in the arterial vascular wall. These deposits form plaques that enlarge and thicken, decreasing blood flow and vascular elasticity. Thymoquinone down-regulates angiotensin II expression, which limits oxidative stress and the associated inflammation in cardiac cells.*  
  • Pulmonary conditions: Elevated cellular proliferation and an aberrant cell cycle can trigger inflammatory mechanisms in the lungs. Thymoquinone inhibits abnormal cellular proliferation in the lungs by down-regulating the activity of the TNF-a and NF-κB pathways.*
  • Neurodegenerative disorders: Neurodegenerative conditions are caused by oxidative damage to neural tissues. One of the underlying causes of oxidative stress is an innate immune system inflammatory response that affects brain functions. Thymoquinone inhibits the NF-κB pathway, reduces superoxide dismutase and catalase activities, and attenuates the expression of proinflammatory cytokines to help maintain the normal inflammatory response.* 
  • Gastrointestinal conditions: Black seed oil has been traditionally used to alleviate symptoms of gastrointestinal disorders, such as bloating, vomiting, constipation, diarrhea, and heartburn. Thymoquinone’s properties stimulate the expression of antioxidant enzymes that mitigate adverse gastrointestinal conditions impacting the stomach, liver, gallbladder, intestine, and pancreas.* 

Absorption Challenges of Thymoquinone

Thymoquinone is preferred as an oral supplement over other routes, such as intravenous administration, due to its lipophilicity. However, oral administration is restricted by the solubility-related poor oral bioavailability and the relatively low solubility of thymoquinone in water. 

Thymoquinone’s poor bioavailability presents a major challenge hindering its efficacy as a therapeutic agent. Its low oral absorption has also led to limited clinical application. In response, several researchers have employed various pharmacological approaches, including nanotechnology, to enhance the bioavailability of thymoquinone. 

Thymoquinone is a hydrophobic molecule, and various studies have attempted to encapsulate thymoquinone into nanoformulations. The nanocarrier delivery of thymoquinone enables its targeted delivery at the desired point in the intestinal tract to achieve its desired benefit on inflammatory responses.*

An Advanced Thymoquinone Supplement Formulation 

Innovative nutrient delivery systems in advanced supplement formulations overcome thymoquinone’s bioavailability and absorption challenges, thereby achieving its benefits. Nanoparticle-based formulations have been found to have relatively higher bioavailability than unformulated thymoquinone. The movement of thymoquinone-loaded nanocarriers through the intestinal lymphatic system bypasses the initial digestion and metabolism to enhance relative bioavailability. 

The efficacy of a thymoquinone supplement is determined by its absorption and bioavailability. An advanced formulation containing a blend of botanical extracts delivered through a nano-delivery system enables optimal absorption of the active nutrients. 

ThymoQuell® is an advanced thymoquinone supplement developed by Tesseract Medical Research to beneficially influence inflammatory response and oxidative stress in the gastrointestinal tract.* ThymoQuell® Plus contains Tesseract’s advanced thymoquinone along with a blend of botanical extracts — turmeric oil and four powerful terpenes – geraniol, borneol, nerol, and farnesol, to promote normal inflammatory responses in the gastrointestinal tract through enhanced nutritional support.* 
Both formulations are powered by Tesseract’s proprietary CyLoc® – DexKey® nutrient delivery nanotechnology for optimal absorption and solubility of the active nutrients. The CyLoc® technology encases each thymoquinone molecule in its smart delivery system to maintain its integrity during transit through the stomach. The accompanying DexKey® reactors release the nutrient molecules at the desired point in the intestinal tract for maximum absorption and efficacy. 

The unprecedented absorption of thymoquinone enables micro-dosing, which means a lesser amount of the active nutrient can be used than previously required to achieve the desired therapeutic benefits.*

Frequently Asked Questions About Thymoquinone Supplements

Thymoquinone’s inflammatory response support properties highlight its crucial role in alleviating adverse inflammatory responses.* If you consider including a thymoquinone supplement in your diet, then you should know its safety, side effects, and intake amount. The following are frequently asked questions (FAQs) about thymoquinone supplements: 

How much thymoquinone should I take in a day?

The U.S. Food and Drug Administration (FDA) categorizes Nigella sativa seeds and the extracted oil as Generally Recognized as Safe (GRAS). Supplementation with the black seed oil at doses of 1.5, 3.0, and 4.5 mL/ day for 20 days is well-tolerated. However, it is recommended to consult with your healthcare practitioner to determine the amount of thymoquinone you should consume for its health benefits.  

When should I include a thymoquinone supplement in my diet? 

Before considering taking a thymoquinone supplement, you should understand its health benefits and side effects. Although the safety profile of thymoquinone is well-established and promotes multiple health functions, it is recommended to consult your healthcare practitioners before including a thymoquinone supplement in your diet. 

Can I take a thymoquinone supplement with prescription medications?

Thymoquinone can be potentially contraindicated with certain medications, such as blood thinners or renal medications. Consult with your healthcare practitioner before taking a thymoquinone supplement with prescription medications or any supplements that are a regular part of your daily regimen.   

The power of Tesseract supplements lies in enhancing palatability, maximizing absorption and bioavailability, and micro-dosing multiple nutrients in a single, highly effective capsule. Shop products on our website and learn more about how they support gastrointestinal health.*

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Citations:

1,2Liu, Yan et al. International journal of molecular sciences vol. 23,18 10246. 6 Sep. 2022, doi:10.3390/ijms231810246

3Khaikin, Elisabeth et al. Nutrients vol. 14,17 3501. 25 Aug. 2022, doi:10.3390/nu14173501

Al Czap, Founder | Tesseract

Al Czap has more than four decades of professional experience in preventative medicine. He founded Thorne Research in 1984 (sold in 2010) and he published Alternative Medicine Review for 17 years beginning in 1996. AMR was a highly acclaimed, peer-reviewed, and indexed medical journal. Al was the first to recognize the need for hypoallergenic ingredients and to devise methods of manufacture for and delivery of hypoallergenic products to underserved patient populations. His work has greatly impacted those with impaired immune and digestive systems and compromised health due to environmental exposures.

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