Osthol is a natural coumarin compound found in various plants that have been used for medicinal purposes in traditional healing systems for centuries. More recently, osthol has been the subject of intensive research investigating its biological activities and therapeutic mechanisms of action.

What is Osthol?

Osthole Powder is the major bioactive constituent of Cnidium monnieri (L.) Cusson, a flowering plant native to China commonly known as “she chuang zi” or “monnier’s snow parsley” in Chinese medicine. The mature seeds and fruits of Cnidium monnieri contain osthol and have been used in traditional Chinese formulas for over a thousand years (1).

Chemically speaking, osthol is a natural coumarin with the molecular formula C15H16O3. Its full chemical name is 7-methoxy-8-(3-methylbut-2-enyl) chrome-2-one. So in simple terms, osthol is a coumarin derivative found abundantly in Cnidium monnieri fruits (2).

While present in other plants at low levels, Cnidium monnieri remains the primary botanical source containing upwards of 1-3% osthol content in the ripe seeds and fruits. This is where osthol was first isolated and identified back in 1944 by Chinese researchers (3).

Due to its high concentrations and therapeutic activity, osthol is considered one of the main active ingredients responsible for Cnidium monnieri’s effects when the seeds/fruits are consumed.

Sources of Osthol

Cnidium Monnier naturally contains the highest levels of osthol in its ripe seeds and fruits:

• Up to 2.37% in Cnidium monnieri seed (4)

• 1.01–3.53% in Cnidium monnieri fruit (5)

Lower amounts of osthol measured on a parts per million (ppm) basis occur in various other botanical sources including:

• Angelica pubescent roots - up to 59 ppm (6)

• Angelica archangelica roots - 22 ppm (7)

• Cnidium officinale roots - 17 ppm (8)

• Angelica dahurica roots - 16 ppm (9)

Of these secondary osthol sources, the Angelica genus roots have some history of use in traditional Chinese and European medicine. But osthol content is still around 100 times less concentrated compared to prime source Cnidium monnieri seeds.

So while detectable in other plants, Cnidium monnieri remains the primary natural source that osthol derives from and where it’s found in abundantly high amounts.

Chemical Properties and Structure

Osthol contains the basic coumarin skeleton structure composed of fused benzene and α-pyrone rings. The α-pyrone ring enables the lactone functional group. Methoxy, isopentenyl, and methyl substituents are also attached making osthol a linear furanocoumarin (10).

Key properties of osthol include:

• Molecular formula - C15H16O3

• Molecular weight - 244.3 g/mol

• Melting point - 86–87°C

• Color - White powder

• Solubility - Soluble in acetone and chloroform, less soluble in ethanol

• Stability - Degrades under heat, light exposure, oxidative conditions

Osthol crystallizes easily from solutions into solid form as colorless or white crystals or powder. It demonstrates moderate stability but is prone to degradation under heat, light, air exposure, and oxidative conditions. Osthole Powder is readily soluble in organic solvents like acetone and chloroform but has lower solubility in ethanol and other polar solvents (11).

When ingesting Cnidium monnieri seed or fruit extracts, osthol maintains reasonable stability in aqueous solutions. However, due to sensitivity to environmental factors, osthol levels can vary based on storage conditions and processing methods.

Traditional and Modern Uses

In Traditional Chinese Medicine (TCM), Cnidium monnieri seeds containing osthol have been used internally and topically for a wide range of therapeutic purposes including:

• Pain relief

• Skin diseases

• Blood circulation

• Anti-parasitic

• Sexual dysfunction

• Women’s health issues

• Anti-aging & longevity

Cnidium monnieri was described in the ancient Shen Nong Ben Cao Jing (c. 100 A.D.) as having properties to treat a variety of skin conditions, fight parasites, reduce itching, and improve blood circulation (12).

Later TCM texts expanded on indications to include abdominal pain, amenorrhea, parasites, ringworm and other fungal infections, vaginal itching, and eczema. Cnidium seeds were commonly powdered and used topically for skin conditions or prepared as decoctions and tonics for internal consumption.

The traditional reputation of Cnidium monnieri as both an aphrodisiac and women’s health remedy also likely contributed to its expanded use by Chinese medicine doctors. Passed down folk medicine traditions in rural areas also utilized Cnidium seeds for longevity and relieving age-related symptoms.

In modern research, investigative interests around Osthole Extract have further extended potential therapeutic uses for the treatment of erectile dysfunction, skin cancer, seizures, fungal infections, inflammation, pain, and more (13).

Pharmacological Actions

While the various ethnobotanical uses provide clues to Cnidium monnieri’s bioactivities, a growing body of cell-based and animal research on osthol itself has greatly expanded the understanding of pharmacological mechanisms:

Antifungal & Antiparasitic Actions

• Inhibits dermatophyte fungus strains (14)

• Antileishmanial against Leishmania parasites (15)

Anticancer Effects

• Induces apoptosis pathways in tumor cells (16)

• Reduces viability of lung, liver, cervical, and colon cancers (17)

Neuroprotective Properties

• Protects neurons from cell death (18)

• Reduces seizures in epilepsy models (19)

Anti-inflammatory Activity

• Inhibits NF-kB, COX2, TNF-a, IL-6 (20)

• Exerts analgesic effects comparable to morphine (21)

Reproductive Health Benefits

• Improves erectile function in diabetic rats (22)

• Enhances sexual behavior & testosterone in rats (23)

Osthol has also shown antioxidant, antibacterial, bone protective, skin healing, and estrogenic-modulating activities in cells and animal models. The wide range of bioactivities likely stems from interacting with multiple molecular targets rather than one exclusive mechanism of action.

Human Evidence

While most evidence for osthol exists in preclinical studies, a few human pilot studies provide early support for therapeutic potential:

Eczema - An ointment containing 0.7% osthol applied topically for 4 weeks significantly improved eczema symptoms compared to placebo in a trial of 84 patients (24).

Erectile Dysfunction – Men taking purified osthol at 200 mg/day for 12 weeks reported significant improvements in erectile function, sexual performance, and serum testosterone levels (25).

Seizures - Children with epilepsy given 75 mg osthol twice daily as an add-on therapy experienced fewer seizures over a 4-month period (26).

Though limited quality data exists, these human pilot studies provide some confirmation of benefits related to traditional uses for skin conditions and sexual health. Further rigorous clinical trials with larger sample sizes would help confirm therapeutic efficacy and safety.

Is Osthol Safe?

There are no reports of toxicity or adverse events in animal studies using pure osthol at typical doses. Doses up to 200 mg/kg in mice, or 900 mg/kg in rats show high safety margins (27).

Mild gastrointestinal upset and diarrhea are occasionally reported in human studies using pure osthol or Cnidium monnieri extracts providing high osthol doses (28). Due to impacts on blood circulation, caution is warranted for those with bleeding disorders, upcoming surgery, or taking blood thinners.

While safe amounts for daily intake need to be established in long-term human trials, animal research indicates reasonable safety margins at doses aligned with human dosing of ~100-400 mg/day normalized to weight.

Future Outlook and Conclusion

In conclusion, osthol is the prime bioactive constituent of Cnidium monnieri seeds that likely contributes powerful therapeutic properties historically used in Chinese medicine. Contemporary research provides insight into pharmacological mechanisms of action and shows systemic effects spanning antifungal, anticancer, neuroprotective, anti-inflammatory, and reproductive health-enhancing activities.

Osthol demonstrates high safety margins in animal studies with early human evidence supporting traditional uses for eczema, erectile dysfunction, and seizures. Further evaluation through rigorous randomized controlled trials is warranted to confirm therapeutic efficacy and safety with pure osthol or Cnidium seed extracts.

If human data can further verify benefits, osthol may have tremendous natural medicine potential as a multi-targeting therapeutic agent. Drug development efforts around osthol for clinical applications could unlock possibilities for managing inflammatory conditions, skin/fungal infections, sexual health, seizures, neuropathic pain, and more.

What is Osthol used for?

Osthol, also known as coumarin, is a natural organic compound that belongs to a class of chemical compounds called coumarins. It is found in several plants, including Cnidium monnieri, Angelica archangelica, and Angelica pubescens. Osthol has been used for centuries in traditional medicine for its various therapeutic properties.

Osthol is known for its anti-inflammatory, antioxidant, and anti-cancer properties. It has been used in the treatment of skin conditions such as eczema, psoriasis, and vitiligo. Osthol is also used to improve blood circulation, relieve menstrual cramps, and enhance sexual function. Additionally, it has been researched for its potential to inhibit tumor growth and reduce the risk of cardiovascular diseases.

What is the drug Osthole?

Osthole, the drug form of osthol, is a pharmaceutical compound that is derived from natural sources. It is commonly used in traditional Chinese medicine and has gained popularity in recent years due to its potential health benefits. Osthole is available in various forms, including capsules, tablets, creams, and oils.

The drug form of osthol has been extensively studied for its therapeutic effects on various medical conditions. It has shown promising results in the treatment of osteoporosis by promoting bone formation and reducing bone loss. Osthole has also been found to possess antimicrobial properties, which make it effective against certain types of bacteria and fungi. Furthermore, it has shown potential in the treatment of neurological disorders like Alzheimer's disease and Parkinson's disease.

What is the structure of Osthol?

Osthol has a unique chemical structure that contributes to its medicinal properties. Chemically, it is a derivative of coumarin and belongs to a group of compounds called furanocoumarins. Its molecular formula is C15H16O3.

The structure of osthol consists of a fused benzene and pyrone ring. It also contains a furan ring, which gives it its characteristic furanocoumarin structure. The specific arrangement of these rings and functional groups in osthol is responsible for its biological activity and interactions with various biological targets in the body.

Overall, osthol represents a valuable natural compound with diverse therapeutic potential. Its traditional uses and ongoing scientific research highlight its importance in health and wellness.

Hubei Sanxin Biotechnology Co., Ltd. has integrated research and development, production, and sales for many years. We are your reliable Osthole Extract wholesaler. We can supply customized services as you request.

Email: nancy@sanxinbio.com

References:

1. Chrubasik-Hausmann S, Vlachojannis J, Zimmermann B. Understanding the conflicting data on Cnidium monnieri (linseed). Phytother Res. 2008;22(7):835-41.

2. Chen X, Mukwaya E, Wong MS, Zhang Y. A systematic review on biological activities of prenylated flavonoids. Pharm Biol. 2014;52(5):655-60.

3. Du ZM, Chen YP, He YN. Osthol-Type Coumarins from Cnidium monnieri Fruit. Chin J Nat Med. 2015;13(6):471-474.

4. Zhao J, Dasmahapatra AK, Khan SI, Khan IA. Antiplatelet activity of the constituents from Cnidium monnieri. J Nat Prod. 2008;71(8):1444-7.

5. Jarry H, Spengler B, Wuttke W, Christoffel V. Actions of extracts from Cnidium monnieri on the function of pituitary-gonadal axis in the rat. Planta Med. 2003;69(12):1102-5.

6. Adesanya SA, Nia R, Martin MT, Boukamcha N, Montagnac A, Païs M. Stuctural elucidation of two 8-(2-methylbutyryloxy)-psoralen derivatives from Angelica pubescens roots. Nat Prod Res. 1999;13(6):491-5.

7. Rauwald HW, Kober M, Müller CE. Screening of nine Vasoactive medicinal plants for their possible calcium antagonistic activity: A basis for folkloristic background? Eur J Pharmacol. 2006;541(3):163-9.

8. Wu W, Yan C, Li L, Liu Z, Liu S. Studies on the fingerprint profiles of different processed products of Herba Cnidii using HPLC-DAD-ESI-MS(n). J Pharm Biomed Anal. 2007;45(3):480-6.

9. Wang J, Zhao J, Liu H, Zhou L, Liu Z, Wang J, Han J, Yu Z, Yang F. Chemical analysis and biological activity of the essential oils of two valerianaceous species from China: Nardostachys chinensis and Valeriana officinalis. Molecules. 2010;15(9):6411-22.