​Harpagophytum procumbens (Devil’s Claw)

Harpagophytum procumbens (Devil’s Claw)

Product Name: Дьявольский коготь, Harpagophytum procumbens, Teufelskralle, Garra del diablo, Griffe du diable, مخلب الشيطان, เล็บปีศาจ, Iblis panjasi, Шайтан тырмак, Şeytan caynağı, Панҷаи шайтона, Velnio nagas, Velna naga, Дияволячий кіготь, שן שטן

Synonyms: Дьявольский коготь, Devil’s claw, Teufelskralle, Garra del diablo, Griffe du diable, مخلب الشيطان, เล็บปีศาจ, коготь демона, коготь зла, grapple plant, wood spider, Sekelharpagophytum, secondary tuber root, secondary storage root

Used Parts: root, tuber, aerial shoots (root — the most commonly used part).

Main Indications for the Use of Harpagophytum procumbens: Osteoarthritis, deforming spondylarthrosis, rheumatoid arthritis, gouty arthritis, myalgia, dorsalgia, lumbalgia, sciatica, tendinitis, chronic pain syndrome, ankylosing spondylitis.

Use of Harpagophytum procumbens in Mixtures and Complexes: Fibromyalgia, chronic osteochondrosis, radiculopathy, tunnel neuropathies, degenerative-dystrophic joint diseases, myofascial pain syndrome, trigeminal neuralgia, post-viral arthralgia.

Pharmacological Properties of Harpagophytum procumbens: Anti-inflammatory, analgesic, antirheumatic, antinociceptive, spasmolytic, sedative, antioxidant, hypoglycemic, chondroprotective, hepatoprotective, immunomodulatory, mild choleretic, moderately antipyretic, anti-edema.

Dosage of Pharmaceutical Forms — Harpagophytum procumbens

Powder — Harpagophytum procumbens

Indications (Powder): Osteoarthritis, rheumatoid arthritis, deforming spondylarthrosis, dorsalgia, myalgia, sciatica.

Standard Dosage (Powder): 1.5 grams of powder 2 times a day, with warm water 30 minutes before meals. Course — 21 days.

Enhanced Dosage (Powder): 2 grams of powder 3 times a day for deforming osteoarthritis, lumbalgia, ankylosing spondylitis, and chronic dorsalgia.

Maximum Dosage (Powder): No more than 6 grams per day, for pronounced pain syndrome in polyosteoarthritis and refractory forms of spondyloarthritis.

Preventive Dosage (Powder): 1 gram once a day for 14 days every 2 months for patients over 50 years of age with chronic forms of osteochondrosis and rheumatism.

Pediatric Dosage (Powder): Data on the safety and efficacy of use in children under 12 years of age have not been scientifically registered. The possibility of use in adolescents with a body weight over 40 kg should be discussed individually.

Contraindications (Powder): Gastric ulcer, ulcerative colitis, cholelithiasis, pregnancy, lactation. Data on contraindications for use in childhood have not been scientifically registered.

Side Effects (Powder): With overdose, the following are possible: diarrhea, nausea, dyspepsia, headache. Isolated cases of increased blood pressure have been recorded.

Adjustment for Patient Body Weight (Powder): Patients with body weight below 60 kg — reduce the dose by 20%. Patients with weight above 90 kg — increase the dose by 15%.

Preparation method (Powder): Dried root of Harpagophytum procumbens is used. The raw material is washed, dried at a temperature of 45 °C in the shade until absolutely dry. Then it is ground in a mill to obtain a powder with particles of no more than 0.3 mm in diameter. Sifted, packaged in sealed containers.

Storage Conditions and Shelf Life (Powder): Store in an airtight container made of dark glass or a metallized bag at a temperature of 5 to 25 °C, away from light sources and EMI. Shelf life — 18 months. After opening, use within 45 days.

Dry Extract — Harpagophytum procumbens

Indications (Dry Extract): Osteoarthritis, gouty arthritis, chronic spinal pain syndrome, rheumatoid arthritis, myofascial pain syndrome.

Standard Dosage (Dry Extract): 250 milligrams of standardized extract (not less than 5% harpagoside) 2 times a day orally, 20 minutes before meals.

Enhanced Dosage (Dry Extract): 300–350 milligrams 3 times a day for severe forms of rheumatoid arthritis, hip osteoarthritis, and ankylosing spondylitis.

Maximum Dosage (Dry Extract): 1000 milligrams per day. Recommended only under specialist supervision for pronounced pain syndrome in the spine and large joints.

Preventive Dosage (Dry Extract): 125 milligrams once a day, in a 10-day course per month for chronic rheumatism and degenerative processes of the spine in patients over 45 years of age.

Pediatric Dosage (Dry Extract): Data on use in children under 14 years of age are absent. Use by adolescents is possible with a weight over 50 kg — no more than 100 mg per day.

Contraindications (Dry Extract): Gastric ulcer, exacerbation of gastritis, hypotension, pregnancy, lactation. Data on contraindications in pediatrics have not been registered.

Side Effects (Dry Extract): Dyspeptic disorders, allergic reactions (rash, itching), rarely — dizziness and tachycardia with overdose may be observed.

Adjustment for Patient Body Weight (Dry Extract): Body weight less than 60 kg — reduce the dose by 25%. Body weight more than 90 kg — increase the dose by 20%.

Preparation method (Dry Extract): 100 grams of dry roots are poured with 1 liter of purified water and extracted at a temperature of 80 °C for 2 hours. The decoction is evaporated to obtain an extract of thick consistency. It is dried by freeze-drying to obtain a dry extract. Standardized according to harpagoside content (not less than 5%).

Storage Conditions and Shelf Life (Dry Extract): Store in a tightly closed container, in a dry, dark place at a temperature of 10–25 °C, protected from moisture. Shelf life — 24 months. After opening — use within 30 days.

Alcohol-Based Tincture — Harpagophytum procumbens

Indications (Tincture): Osteoarthritis, deforming spondylarthrosis, dorsalgia, chronic radiculitis, sciatica, myalgia.

Standard Dosage (Tincture): 20 drops of tincture in 50 ml of water 2 times a day 15 minutes before meals. Course — 21 days.

Enhanced Dosage (Tincture): 30 drops 3 times a day for chronic pain syndrome in degenerative-dystrophic diseases of the spine, ankylosing spondylitis, and pronounced arthrogenic component.

Maximum Dosage (Tincture): No more than 40 drops 3 times a day. Short-term therapy (no more than 7 days) is allowed for acute lumbago or dorsalgia against the background of hypothermia.

Preventive Dosage (Tincture): 15 drops once a day in the morning, for 10 days once every 2 months in patients over 50 years of age with osteochondrosis, chronic rheumatism, and myofascial syndromes.

Pediatric Dosage (Tincture): Not recommended for children under 16 years of age due to ethanol content. Data on use in children and adolescents have not been registered.

Contraindications (Tincture): Alcoholism, pregnancy, lactation, gastric and duodenal ulcer, organic liver lesions. Scientific data on use in childhood are absent.

Side Effects (Tincture): Dizziness, headache, nausea, palpitations, especially when exceeding the dosage or when combined with alcohol.

Adjustment for Patient Body Weight (Tincture): For body weight less than 60 kg — reduce the dose by 25%. For weight more than 90 kg — increase the dose by 15–20%.

Preparation method (Tincture): 100 grams of crushed dry root are poured with 500 ml of 40% ethyl alcohol and infused in a dark glass container at a temperature of 20–25 °C for 14 days, shaking daily. After this, the tincture is filtered through gauze, squeezed out, and stored in a tightly closed dark glass bottle.

Storage Conditions and Shelf Life (Tincture): Store in a dark, cool place at a temperature of 5 to 20 °C, away from sources of fire and direct sunlight. Shielding from EMI is not required. Shelf life — 24 months. After opening the bottle — use within 60 days.

Oil Infusion — Harpagophytum procumbens

Indications (Oil Infusion): Osteoarthritis, spondylosis, lumbalgia, myalgia, fibromyalgia, inflammatory joint diseases.

Standard Dosage (Oil Infusion): Topically, rub 2–3 ml into the area of affected joints or muscles 2 times a day. Duration of course — 14–21 days.

Enhanced Dosage (Oil Infusion): Rub 5 ml 3 times a day for pronounced inflammatory process in joints, dorsalgia, spondylarthrosis, and pain syndrome in fibromyalgia.

Maximum Dosage (Oil Infusion): Up to 20 ml per day, distributed over the affected areas. Use for no more than 7 days in a row in case of exacerbation with a pronounced pain component.

Preventive Dosage (Oil Infusion): 2 ml once a day, in 10-day courses monthly for patients over 55 years of age with chronic arthrosis, spondylosis, and muscle contractures.

Pediatric Dosage (Oil Infusion): With caution, external use is possible in children over 12 years of age, in the absence of allergies. Maximum — 1 ml per day on a limited area of skin, no more than 7 days.

Contraindications (Oil Infusion): Damage to the skin in the application area, individual intolerance to components. Data on contraindications during pregnancy and in childhood have not been registered.

Side Effects (Oil Infusion): Skin irritation, allergic rash, erythema, contact dermatitis with individual sensitivity.

Adjustment for Patient Body Weight (Oil Infusion): Not required, as it is applied topically. Adjustment is possible only according to the area of application.

Preparation method (Oil Infusion): 100 grams of dry crushed root are poured with 200 ml of organic coconut oil. Infused in a water bath at a temperature of 45–50 °C for 3 hours, stirring occasionally. After this, kept at room temperature for 48 hours, filtered through a filter and poured into sterilized bottles.

Storage Conditions and Shelf Life (Oil Infusion): Store at a temperature of 5–20 °C, in a dark, tightly closed container, away from sunlight. Shielding from EMI is desirable. Shelf life — 12 months. After opening, use within 30 days.

Ointment — Harpagophytum procumbens

Indications (Ointment): Osteoarthritis, rheumatoid arthritis, lumbalgia, dorsalgia, myalgia, spondylarthrosis, trigeminal neuralgia.

Standard Dosage (Ointment): Topically, apply a thin layer of ointment 2 times a day to the area of pain or inflammation, rubbing in for 2–3 minutes. Course — up to 21 days.

Enhanced Dosage (Ointment): Apply 3–4 times a day for acute joint pain, spondylarthrosis, pronounced myofascial syndrome, and post-traumatic inflammation.

Maximum Dosage (Ointment): Up to 5 applications per day, no more than 25 g of ointment per day. Short-term — no more than 5 days in a row.

Preventive Dosage (Ointment): Once a day at night, in courses of 10 days per month for patients with chronic osteoarthritis, neuralgia, rheumatism, and spondylosis.

Pediatric Dosage (Ointment): Use is possible in children over 10 years of age with a body weight of more than 35 kg, no more than once a day, only on limited areas of skin, under adult supervision.

Contraindications (Ointment): Allergy to components, active skin inflammations, open wounds. During pregnancy and lactation — only by doctor's prescription. Scientific data on contraindications in children under 10 years of age are absent.

Side Effects (Ointment): Contact dermatitis, skin irritation, itching, hyperemia in the application area.

Adjustment for Patient Body Weight (Ointment): Patients with body weight less than 60 kg — use the ointment on a limited area, no more than 2–3 grams per application. For weight more than 90 kg, an increase in dose to 5 grams is possible.

Preparation method (Ointment): For 100 grams of ointment: dry extract of Harpagophytum procumbens — 5 g, cold-pressed coconut oil — 60 g, purified beeswax — 25 g, lavender essential oil — 2 g, lecithin — 3 g, vitamin E — 2 g, purified water — 3 g. Melt coconut oil and wax in a water bath at a temperature of 50–55 °C, add the extract, mix thoroughly. Gradually introduce lecithin, essential oil, vitamin E, and water. Beat until a homogeneous emulsion is obtained, cool, and pour into sterile jars.

Storage Conditions and Shelf Life (Ointment): Store at a temperature of 5–10 °C in a tightly closed dark glass container. Protect from direct light and moisture. Shelf life — 6 months. After opening — use within 30 days.

Cosmetic Cream — Harpagophytum procumbens

Indications (Cosmetic Cream): Osteoarthritis, chronic myositis, muscle pain, fibromyalgia, inflammatory joint diseases.

Standard Dosage (Cosmetic Cream): Apply 1–2 ml of cream to the painful area 2 times a day, morning and evening. Do not rub in vigorously. Course — 14 days.

Enhanced Dosage (Cosmetic Cream): Up to 3 ml of cream 3 times a day for chronic rheumatoid arthritis, severe forms of fibromyalgia, and prolonged myalgia against the background of viral load.

Maximum Dosage (Cosmetic Cream): 5 ml per area, no more than 3 times a day. Use is allowed for up to 10 days in the acute phase of pain syndrome.

Preventive Dosage (Cosmetic Cream): 1 ml once a day in the evening for patients over 50 years of age with chronic pain in the lower back, joints, and muscles. Course — 10 days every 2 months.

Pediatric Dosage (Cosmetic Cream): Use is possible in children over 12 years of age with a body weight of 40 kg or more. Recommended no more than 1 ml of cream per day, short-term, no more than 7 days in a row.

Contraindications (Cosmetic Cream): Allergy to the extract, acute skin inflammations, skin infections, open wounds. Data on contraindications during pregnancy, lactation, and in childhood have not been registered.

Side Effects (Cosmetic Cream): Rarely — itching, burning sensation, erythema. With prolonged use on sensitive skin — flaking.

Adjustment for Patient Body Weight (Cosmetic Cream): Adjustment by body weight is not required, as the cream is applied topically and dosed according to the area of the lesion.

Preparation method (Cosmetic Cream): For 100 g of cream: water-glycerin extract of Harpagophytum procumbens — 5 g, coconut oil — 20 g, witch hazel hydrolate — 25 g, shea butter — 15 g, vegetable emulsifier — 8 g, allantoin — 1 g, panthenol — 2 g, natural preservative — 0.5 g, purified water — up to 100 g. The oil and aqueous phases are heated separately to 65 °C, then combined, active components are introduced at 40 °C, beaten with a mixer to a creamy texture, and packaged in sterile jars.

Storage Conditions and Shelf Life (Cosmetic Cream): Store at a temperature of 4–8 °C, in a sealed dark package. Avoid sunlight and strong heating. Shelf life — 3 months. After opening — use within 21 days.

Toxicity and Biosafety of Harpagophytum procumbens

Toxicological studies of Harpagophytum procumbens have demonstrated a high level of biosafety upon oral administration. In a study conducted on rats, the acute oral LD₅₀ value of Harpagophytum procumbens extract was determined to be over 16,000 mg/kg body weight, which indicates an extremely low acute toxicity of the plant. With prolonged use in animals, no signs of organ toxicity, hematological, or biochemical disturbances were observed.

Furthermore, phytochemical components such as harpagoside do not demonstrate mutagenic or carcinogenic potential in in vitro and in vivo tests. Thus, Harpagophytum procumbens is considered pharmacologically safe when recommended dosages are observed.

Nevertheless, when used in high doses for a long period of time, the appearance of dyspeptic reactions and hypersensitivity is possible.

Reference: https://www.ncbi.nlm.nih.gov/p...

Pharmacodynamics — Harpagophytum procumbens

The pharmacodynamic properties of Harpagophytum procumbens are due to the presence of iridoid glycosides (primarily harpagoside), phenolic compounds, and phytosterols in its composition, which determine the modulating effect on inflammatory and pain processes. The main pharmacological action is associated with the inhibition of cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) enzymes, which leads to a decrease in the synthesis of prostaglandins and leukotrienes — mediators of the inflammatory response. This provides a systemic anti-inflammatory and antinociceptive effect.

Furthermore, iridoids are capable of influencing the modulation of interleukin levels and tumor necrosis factor-α (TNF-α), which indicates an immunomodulatory effect and participation in the regulation of the cytokine cascade. This makes it possible to use the taxon for the systemic regulation of chronic inflammation processes. Local application helps improve microcirculation, reduce edema, and restore tissue metabolism.

Of particular interest is the antioxidant mechanism, which is realized through increasing the activity of superoxide dismutase and glutathione reductase. The reduction in the production of reactive oxygen species contributes to the stabilization of cell membranes, including in the tissues of the musculoskeletal system. Such properties provide pharmacological protection at the cellular level under conditions of oxidative stress.

In vitro studies have also shown moderate inhibitory activity against factors involved in cartilage tissue degradation, including metalloproteinases. This indicates the potential ability of Harpagophytum procumbens components to slow down destructive processes in connective tissue. The indirect effect on monoamine metabolism enzymes in neuronal structures may explain the mild sedative and spasmolytic effect observed with systemic use.

Systemic targets of action are: the peripheral and central nervous system, the immune system, connective tissue structures of the joint apparatus, the capillary bed, as well as enzymatic links of inflammation regulation. The action is realized both at the systemic and local levels. The confirmed participation of key iridoids in the regulation of enzymatic and mediator mechanisms allows the pharmacological profile of the plant to be classified as moderately expressed multi-target action.

References:
https://www.ncbi.nlm.nih.gov/p...
https://www.sciencedirect.com/...
https://www.tandfonline.com/do...

Pharmacokinetics — Harpagophytum procumbens

The pharmacokinetics of the active substances of Harpagophytum procumbens has been studied fragmentarily; however, available data allow general patterns to be identified. Upon oral administration, iridoid glycosides undergo partial hydrolysis in the gastrointestinal tract under the action of microflora and enzymes. After hydrolysis, aglycones are formed, which can be absorbed in the small intestine and then enter the systemic circulation. Absorption occurs mainly in the proximal parts of the intestine, and the rate of absorption may vary depending on the dosage form: extracts have a greater rate and completeness of absorption compared to powders.

Distribution in the body occurs with the participation of plasma proteins, while active metabolites of iridoids and phenolic acids can penetrate into connective tissue structures and exert their action in joint capsules and periarticular tissues. Presumably, active components accumulate in the synovial fluid and connective tissue matrices, where they exhibit a prolonged effect.

Metabolism of iridoids occurs mainly in the liver with the participation of phase I and II enzyme systems (oxidation, hydroxylation, conjugation). Some metabolites may undergo glucuronidation and sulfation, facilitating their excretion. It has been established that gut microbiota play an important role in the biotransformation of primary glycosides, which determines the variability of the pharmacokinetic response depending on the state of the intestinal flora.

Excretion is carried out primarily by the kidneys, in the form of metabolites with urine, and to a lesser extent — with bile. Given the moderate lipophilicity of some aglycone metabolites, partial excretion through the skin with prolonged use is possible. External forms (ointment, cream, oil infusion) act locally with minimal systemic absorption, mainly within the epidermal and subcutaneous layers.

Given the high molecular weight and plant origin of the active substances, biotransformation and excretion may depend on the overall metabolic status of the patient, including the functional state of the liver, kidneys, and intestinal microflora.

References:
https://www.ncbi.nlm.nih.gov/p...
https://link.springer.com/arti...
https://pubmed.ncbi.nlm.nih.go...

Mechanisms of Action and Scientific Rationale — Harpagophytum procumbens

The pharmacological activity of Harpagophytum procumbens is primarily due to the content of iridoid glycosides, in particular harpagoside and harpagide. These compounds have a pronounced effect on enzyme systems involved in the regulation of inflammation and pain sensitivity. Harpagoside inhibits the activity of cyclooxygenase-2 (COX-2) and lipoxygenase (LOX), which leads to a decrease in the level of pro-inflammatory prostaglandins and leukotrienes. These mechanisms are confirmed by in vitro and in vivo studies, where a decrease in the production of PGE₂ and LTB₄ in macrophages was observed.

Furthermore, harpagoside has an inhibitory effect on the activation cascade of the nuclear factor NF-κB, thereby modulating the expression of pro-inflammatory cytokines, including TNF-α, IL-1β, and IL-6. The effect on the JNK and p38 MAPK signaling pathways confirms the involvement of iridoids in the modulation of intracellular signaling mechanisms responsible for the proliferation and activation of immune cells. This effect leads to a decrease in the expression of adhesion molecules on the surface of the endothelium and a reduction in the migration of neutrophils and monocytes to the inflammation zone.

Antioxidant properties of iridoids have also been identified, which are realized through an increase in the expression of antioxidant enzymes such as superoxide dismutase (SOD), catalase, and glutathione peroxidase. These effects contribute to the protection of cellular structures from lipid peroxidation, which is especially important under conditions of chronic oxidative stress.

Along with iridoids, flavonoid compounds found in the extract of Harpagophytum procumbens demonstrate additional inhibition of monoamine oxidase and acetylcholinesterase enzymes, which may explain the sedative and spasmolytic component of the plant's action. Interaction with glucocorticoid receptors is also suggested, which mediates the anti-edema and stabilizing effect in tissues.

The targets of action are both cells of innate immunity (macrophages, neutrophils) and signaling proteins that control the inflammatory cascade. The predominant level of action is systemic, with possible localization of the effect in the synovial membrane, connective tissue, and vascular bed. Biomolecular data confirm that modulation of enzymatic and receptor cascades occurs without sharp immunosuppressive effects, but rather with a directed regulatory action.

References:
https://www.ncbi.nlm.nih.gov/p...
https://www.sciencedirect.com/...
https://link.springer.com/arti...
https://www.tandfonline.com/do...

Synergy — Harpagophytum procumbens

Scientific data demonstrate a pronounced pharmacological synergy between the extract of Harpagophytum procumbens and other plant components with anti-inflammatory, antioxidant, and spasmolytic activity. Combined use with curcumin (the active component of Curcuma longa) has shown potentiation of the inhibitory effect on cyclooxygenase-2 and an increase in the suppression of the production of pro-inflammatory cytokines TNF-α and IL-6. This effect has a systemic direction and is realized through cross-action on the NF-κB cascade.

The combination of Harpagophytum procumbens with flavonoid extracts (including Camellia sinensis and Vitis vinifera) enhances the antioxidant effect, due to the synergistic increase in the expression of first-line antioxidant defense enzymes (SOD, GSH, catalase). These interactions are potentiating in nature and manifest both at the systemic and tissue-specific levels, particularly in connective tissue.

Synergy with Boswellia serrata has been noted, manifested in additive inhibition of 5-LOX and a decrease in the expression of caspase-1 in macrophages, which indicates a complex suppression of inflammation mediators both at the level of enzymes and signaling proteins. In this case, the nature of the interaction can be considered as multi-level: including antinociceptive, angiomodulatory, and antioxidant components.

Combined use of Harpagophytum procumbens with magnesium, zinc, and organic forms of selenium has shown protective activity with respect to chondrocytes and endothelial cells. This may indicate cytoprotective synergy at the cellular level, especially under conditions of oxidative and inflammatory stress.

References:
https://www.ncbi.nlm.nih.gov/p...
https://www.tandfonline.com/do...
https://www.sciencedirect.com/...
https://link.springer.com/arti...

Geography of Use and Traditional Medicine — Harpagophytum procumbens

Harpagophytum procumbens, known as devil's claw, is traditionally used in the folk medicine of the peoples of southern Africa, primarily among the Bushmen, Bantu, and Tswana, as well as in the Angolan and Namibian ethnomedical tradition. The main regions of natural distribution and cultural use of the plant are the Kalahari Desert, the savannas of Namibia, Botswana, and the Republic of South Africa. The earliest ethnobotanical evidence of the use of the plant root dates back to the pre-European period, however, the earliest written mentions are recorded in the chronicles of missionaries and naturalists of the 19th century, describing the practices of the Herero and Tswana peoples.

In traditional African healing, both fresh and dried roots of the plant were used. Decoctions and thick extracts were used externally and internally, including as part of multi-component remedies. Wraps and rubbings with heated root powder were used in tribal healing practices in combination with ritual chants and touching totemic symbols. In the culture of the Herero people, the plant was considered "taming the bone" and was used by elderly men as part of health ceremonies.

In some shamanic and semi-magical practices, devil's claw was included in smoking mixtures with other herbs of the Kalahari Desert. Also known are cases of its use as an amulet — the roots of the plant were worn dried on the belt as a protective symbol against "evil winds" and diseases. In oral traditions, the plant was associated with earth spirits and was considered a connecting link between the body and the earth.

In the French and German phytotherapeutic tradition of the 20th century, the plant was adopted from the African heritage and adapted as an official phytoremedy. It was included in the pharmacopoeias of some European countries and became part of phytopharmacy practices. In the modern ethnomedicine of Namibia, the plant continues to be used in the form of infusions, rubs, and also as part of ointments prepared by hand according to traditional recipes.