Borage seed oil is derived from the seeds of the plant, Borago officinalis (borage). [1]
Borage seed oil has one of the highest amounts of γ-linolenic acid (GLA) of seed oils — higher than blackcurrant seed oil or evening primrose oil, to which it is considered similar. GLA is typically composed of about 24% of the oil.
GLA is converted to dihomo-γ-linolenic acid (DGLA), a precursor to a variety of the 1-series prostaglandins and the 3-series leukotrienes. It inhibits leukotriene synthesis to provide therapy in rheumatologic illness. [1] Borage seed oil, therefore, may have anti-inflammatory and anti-thrombotic effects. It has been studied for its potential to treat inflammatory disorders, arthritis, atopic eczema, and respiratory inflammation. [1]
In herbal medicine, borage seed oil has been used for skin disorders such as eczema, seborrheic dermatitis, and neurodermatitis; it has also been used for rheumatoid arthritis, stress, premenstrual syndrome, diabetes, attention deficit-hyperactivity disorder (ADHD), acute respiratory distress syndrome (ARDS), alcoholism, pain and swelling (inflammation), and for preventing heart disease and stroke. [2] There is insufficient scientific evidence to determine the effectiveness of borage for a majority of these uses. [2]
Several clinical studies have shown the oil to be ineffective at treating atopic eczema. [3] [4] Its efficacy to treat eczema was not better than placebo when taken orally. [5]
Borage oil may contain the pyrrolizidine alkaloid amabiline, [6] [7] [8] which is hepatotoxic leading to a risk of liver damage. [1]
Patients should use borage oil that is certified free of toxic unsaturated pyrrolizidine alkaloids (UPAs). [1] Consumption of 1-2 g of borage seed oil daily can result in an intake of toxic UPAs approaching 10 ug. [1] The German Federal Health Agency specifies consumption to be limited to 1 ug of UPA daily. [1]
Borage oil may be unsafe during pregnancy because preliminary studies suggest borage oil has a teratogenic effect and that its prostaglandin E agonist action may cause premature labor. [1] [9]
Seizures have been reported as a complication of ingestion of borage oil in doses of 1,500 to 3,000 mg daily, [10] although a mixed review of borage oil's effect on seizure thresholds indicates that borage oil quality varies. [11] A specific extraction process may offer purified products with 50%+ GLA content.
Borage seed oil might prolong bleeding time, increase the risk of bruising and bleeding, and increase the risk of bleeding during and after surgery. [2]
Because borage oil can theoretically lower the seizure threshold due to its GLA content, it could therefore trigger a seizure in users of phenothiazines or tricyclic antidepressants. [1]
Use of NSAIDs with borage oil may theoretically decrease the effects of borage oil, as NSAIDs interfere with the synthesis of prostaglandin E. [1]
Ketoprofen is one of the propionic acid class of nonsteroidal anti-inflammatory drugs (NSAID) with analgesic and antipyretic effects. It acts by inhibiting the body's production of prostaglandin.
Non-steroidal anti-inflammatory drugs (NSAID) are members of a therapeutic drug class which reduces pain, decreases inflammation, decreases fever, and prevents blood clots. Side effects depend on the specific drug, its dose and duration of use, but largely include an increased risk of gastrointestinal ulcers and bleeds, heart attack, and kidney disease.
Essential fatty acids, or EFAs, are fatty acids that are required by humans and other animals for normal physiological function that cannot be synthesized in the body. As they are not synthesized in the body, the essential fatty acids – alpha-linolenic acid (ALA) and linoleic acid – must be obtained from food or from a dietary supplement. Essential fatty acids are needed for various cellular metabolic processes and for the maintenance and function of tissues and organs. These fatty acids also are precursors to vitamins, cofactors, and derivatives, including prostaglandins, leukotrienes, thromboxanes, lipoxins, and others.
Cyclooxygenase (COX), officially known as prostaglandin-endoperoxide synthase (PTGS), is an enzyme that is responsible for biosynthesis of prostanoids, including thromboxane and prostaglandins such as prostacyclin, from arachidonic acid. A member of the animal-type heme peroxidase family, it is also known as prostaglandin G/H synthase. The specific reaction catalyzed is the conversion from arachidonic acid to prostaglandin H2 via a short-living prostaglandin G2 intermediate.
Borage, also known as starflower, is an annual herb in the flowering plant family Boraginaceae native to the Mediterranean region. Although the plant contains small amounts of pyrrolizidine alkaloids, some parts are edible and its seeds provide oil.
Eicosanoids are signaling molecules made by the enzymatic or non-enzymatic oxidation of arachidonic acid or other polyunsaturated fatty acids (PUFAs) that are, similar to arachidonic acid, around 20 carbon units in length. Eicosanoids are a sub-category of oxylipins, i.e. oxidized fatty acids of diverse carbon units in length, and are distinguished from other oxylipins by their overwhelming importance as cell signaling molecules. Eicosanoids function in diverse physiological systems and pathological processes such as: mounting or inhibiting inflammation, allergy, fever and other immune responses; regulating the abortion of pregnancy and normal childbirth; contributing to the perception of pain; regulating cell growth; controlling blood pressure; and modulating the regional flow of blood to tissues. In performing these roles, eicosanoids most often act as autocrine signaling agents to impact their cells of origin or as paracrine signaling agents to impact cells in the proximity of their cells of origin. Some eicosanoids, such as prostaglandins, may also have endocrine roles as hormones to influence the function of distant cells.
Anti-inflammatory or antiphlogistic is the property of a substance or treatment that reduces inflammation or swelling. Anti-inflammatory drugs, also called anti-inflammatories, make up about half of analgesics. These drugs remedy pain by reducing inflammation as opposed to opioids, which affect the central nervous system to block pain signaling to the brain.
Cyclooxygenase-2 inhibitors, also known as coxibs, are a type of nonsteroidal anti-inflammatory drug (NSAID) that directly target cyclooxygenase-2 (COX-2), an enzyme responsible for inflammation and pain. Targeting selectivity for COX-2 reduces the risk of peptic ulceration and is the main feature of celecoxib, rofecoxib, and other members of this drug class.
γ-Linolenic acid or GLA is an n−6, or omega-6, fatty acid found primarily in seed oils. When acting on GLA, arachidonate 5-lipoxygenase produces no leukotrienes and the conversion by the enzyme of arachidonic acid to leukotrienes is inhibited.
Borago, or borage, is a genus of five species of herbs native to the Mediterranean, with one species, Borago officinalis, cultivated and naturalized throughout the world.
Oenothera biennis, the common evening-primrose, is a species of flowering plant in the family Onagraceae, native to eastern and central North America, from Newfoundland west to Alberta, southeast to Florida, and southwest to Texas, and widely naturalized elsewhere in temperate and subtropical regions. Evening primrose oil is produced from the plant.
Dihomo-γ-linolenic acid (DGLA) is a 20-carbon ω−6 fatty acid. In physiological literature, it is given the name 20:3 (ω−6). DGLA is a carboxylic acid with a 20-carbon chain and three cis double bonds; the first double bond is located at the sixth carbon from the omega end. DGLA is the elongation product of γ-linolenic acid. GLA, in turn, is a desaturation product of linoleic acid. DGLA is made in the body by the elongation of GLA, by an efficient enzyme which does not appear to suffer any form of (dietary) inhibition. DGLA is an extremely uncommon fatty acid, found only in trace amounts in animal products.
There is a wide variety of fatty acids found in nature. Two classes of fatty acids are considered essential, the omega-3 and omega-6 fatty acids. Essential fatty acids are necessary for humans but cannot be synthesized by the body and must therefore be obtained from food. Omega-3 and omega-6 are used in some cellular signaling pathways and are involved in mediating inflammation, protein synthesis, and metabolic pathways in the human body.
David Frederick Horrobin was a British-Canadian entrepreneur, medical researcher, author and editor. He is best known as the founder of the biotechnology company Scotia Holdings and as a promoter of evening primrose oil as a medical treatment, Horrobin was founder and editor of the journals Medical Hypotheses and Prostaglandins, Leukotrienes and Essential Fatty Acids, the latter journal co-founded with his then graduate student Morris Karmazyn.
Tolmetin is a nonsteroidal anti-inflammatory drug (NSAID) of the heterocyclic acetic acid derivative class.
Flunoxaprofen, also known as Priaxim, is a chiral nonsteroidal anti-inflammatory drug (NSAID). It is closely related to naproxen, which is also an NSAID. Flunoxaprofen has been shown to significantly improve the symptoms of osteoarthritis and rheumatoid arthritis. The clinical use of flunoxaprofen has ceased due to concerns of potential hepatotoxicity.
Acemetacin is a non-steroidal anti-inflammatory drug (NSAID) used for the treatment of osteoarthritis, rheumatoid arthritis, lower back pain, and relieving post-operative pain. It is manufactured by Merck KGaA under the tradename Emflex. It is no longer available in the UK, however is available in other countries as a prescription-only drug.
Thesinine is a pyrrolizidine alkaloid first isolated from Thesium minkwitzianum from which it derives its name. It is also found in the flowers and seeds of borage.
Amabiline is a pyrrolizidine alkaloid first isolated in 1967 from Cynoglossum amabile. It is also found in the seeds and flowers of borage and in borage seed oil.
Prostaglandin inhibitors are drugs that inhibit the synthesis of prostaglandin in human body. There are various types of prostaglandins responsible for different physiological reactions such as maintaining the blood flow in stomach and kidney, regulating the contraction of involuntary muscles and blood vessels, and act as a mediator of inflammation and pain. Cyclooxygenase (COX) and Phospholipase A2 are the major enzymes involved in prostaglandin production, and they are the drug targets for prostaglandin inhibitors. There are mainly 2 classes of prostaglandin inhibitors, namely non- steroidal anti- inflammatory drugs (NSAIDs) and glucocorticoids. In the following sections, the medical uses, side effects, contraindications, toxicity and the pharmacology of these prostaglandin inhibitors will be discussed.