Harpagoside

Harpagoside is a bitter-tasting iridoid glycoside (see iridoids below), a glycosidically linked monoterpene derivative, which can be found as an active drug primarily in the roots of the South African devil's claw (Harpaphagophyti radix). South African devil's claw originates from the arid regions of South Africa, Namibia and Botswana and is traditionally used to treat inflammatory diseases, pain and digestive problems.

Harpagoside belongs to the group of iridoid glycosides, which are known for their anti-inflammatory and pain-relieving properties. The chemical structure consists of an iridoid backbone with a glucose unit.

Harpagoside is an effective, natural anti-inflammatory and painkiller substitute that can be particularly helpful for joint and muscle pain. Harpagoside significantly alters the global chemokine expression profile in IL-1β-stimulated chondrocytes. Furthermore, harpagoside alters the expression of IL-6 in chondrocytes. Harpagoside did not inhibit IL-1-induced activation of the transcription factors NF-κB and C/EBPβ, but suppressed IL-1β-triggered induction, phosphorylation and DNA-binding activity of c-FOS, one of the major components of AP-1 transcription factors. In addition, harpagoside significantly inhibits the expression of MMP-13 in OA chondrocytes under pathological conditions. Harpagoside is considered to be well tolerated and represents a herbal alternative to synthetic painkillers (Haseeb A et al.2017).

Harpagoside has several medically relevant properties that are particularly important in the treatment of rheumatic diseases, osteoarthritis and back pain:

Anti-inflammatory:

• Harpagoside inhibits certain pro-inflammatory enzymes (e.g. COX-2 and lipoxygenase) involved in the production of prostaglandins and reduces the formation of cytokines (e.g. TNF-α, IL-1β), which play a key role in chronic inflammation.

Pain-relieving (analgesic)

• Harpagoside can reduce pain sensitivity, especially in joint and back pain. Prescription. Studies show that it can have a comparable effect to non-steroidal anti-inflammatory drugs (NSAIDs), but with fewer side effects on the gastrointestinal tract.

Cartilage protection (chondroprotective)

• It is assumed that harpagoside slows down the degenerative destruction of cartilage tissue in osteoarthritis. It protects the joints by inhibiting matrix metalloproteinases (MMPs), which break down cartilage.

Improving mobility:

• Studies show that patients with osteoarthritis or back pain experience better mobility and less pain after taking it for several weeks.

Harpagoside is the main active ingredient in devil's claw extracts, which are used for:

• Rheumatoid arthritis
• osteoarthritis
• Back pain & disc problems
• Muscle pain & tendonitis
• gout

Harpagoside is usually supplied in the form of tablets, capsules, tea or ointments and the recommended daily dose is between 50-100 mg harpagoside (equivalent to around 2400 mg devil's claw root extract). The effect does not occur immediately, but after 2-4 weeks of regular use.

Teas: A tea made from 4.5 g of cut or powdered devil's claw root provides an average of 90 mg harpagoside.

Externals (ointments, balms): In addition to harpagoside, many devil's claw ointments contain other herbal ingredients such as juniper, rosemary, horse chestnut, arnica or spruce needle, which can contribute synergistically to pain relief and anti-inflammation. Application: These ointments are typically used to relieve muscle and joint pain and are applied externally to the affected areas.

Well tolerated. Side effects may occur in rare cases:

• Gastrointestinal complaints (nausea, diarrhea, stomach pain)
• Interactions with blood-thinning medication
• Not recommended for stomach ulcers or biliary diseases

Other related ingredients of devil's claw are harpagide and procumbide, which are also pharmacologically active but have a lesser effect.

1. Anauate MC et al. (2010) Effect of isolated fractions of Harpagophytum procumbens D.C. (devil's claw) on COX-1, COX-2 activity and nitric oxide production on whole-blood assay. Phytother Res 24:1365-1369.
2. Brien S et al. (2006) Devil's Claw (Harpagophytum procumbens) as a treatment for osteoarthritis: a review of efficacy and safety. J Altern Complement Med. 12:981-993.
3. Haseeb A et al. (2017) Harpagoside suppresses IL-6 expression in primary human osteoarthritis chondrocytes. J Orthop Res 35:311-320.
4. Mncwangi N et al. (2012) Devil's Claw-a review of the ethnobotany, phytochemistry and biological activity of Harpagophytum procumbens. Journal of ethnopharmacology 143:755-771.