Hermetica Superfood Encyclopedia
The Short Answer
Osthole (7-methoxy-8-(3-methyl-2-butenyl)coumarin) is a natural coumarin compound isolated primarily from Cnidium monnieri and Angelica pubescens that exerts anti-inflammatory, anti-cancer, and neuroprotective effects. Its primary mechanisms involve inhibition of NF-κB signaling, modulation of Th2 cytokine cascades, and induction of mitochondria-mediated apoptosis in tumor cells.
CategoryNamed Bioactive Compounds
GroupCompound
Evidence LevelModerate
Primary Keywordosthole (7-methoxy-8-(3-methyl-2-butenyl)coumarin) benefits
Synergy Pairings3
Osthole (7-methoxy-8-(3-methyl-2-butenyl)coumarin) — botanical close-up
Health Benefits
Origin & History
Natural habitat
Osthole (7-methoxy-8-(3-methyl-2-butenyl)coumarin) is a coumarin derivative primarily found in medicinal plants Cnidium monnieri and Angelica pubescens. It is one of the major bioactive components isolated from these traditional medicinal species.
“The research provides no information on historical traditional medicine applications of osthole. While identified as a component of Cnidium monnieri and Angelica pubescens used in traditional Chinese medicine, specific traditional indications or historical uses are not documented.”Traditional Medicine
Scientific Research
No human clinical trials, randomized controlled trials, or meta-analyses of osthole were found in the provided research. All available evidence derives exclusively from preclinical in vitro and animal studies, with no PMIDs provided for human trials.
Preparation & Dosage
Traditional preparation
No standardized human dosages have been established. Animal studies used 25-50 mg/kg orally in mice. In vitro studies used 6.25-25 μM concentrations. No human safety data or clinical dosing recommendations are available. Consult a healthcare provider before starting any new supplement.
Nutritional Profile
Osthole (7-methoxy-8-(3-methyl-2-butenyl)coumarin) is a pure isolated bioactive compound, not a whole food ingredient, and therefore has no macronutrient, micronutrient, fiber, or protein content. Molecular formula: C15H16O3; molecular weight: 244.29 g/mol. It is a prenylated coumarin derivative classified as a secondary plant metabolite. Naturally occurring concentrations in source plants: found in Cnidium monnieri seeds at approximately 0.5–2.0% dry weight, in Angelica pubescens root at 0.1–0.8% dry weight, and in smaller quantities in other Apiaceae/Umbelliferae family plants including Peucedanum ostruthium and Notopterygium incisum. As a pure compound used in research, it is typically evaluated at defined doses (25–50 mg/kg in animal studies). Bioavailability: Osthole is lipophilic (logP approximately 3.5), with limited water solubility (~0.03 mg/mL), which restricts oral bioavailability. Studies in rodents indicate rapid absorption after oral administration with peak plasma concentrations within 0.5–1 hour, though first-pass hepatic metabolism is significant. It undergoes cytochrome P450-mediated hydroxylation and glucuronidation. The prenyl side chain contributes to membrane permeability. No established dietary reference intake or recommended human dose exists; all quantified efficacy data derives from in vitro or animal models.
How It Works
Mechanism of Action
Osthole suppresses NF-κB nuclear translocation and downregulates pro-inflammatory cytokines including IL-4, IL-5, and IL-13, reducing Th2-driven airway inflammation in allergic asthma models. In cancer cells, it triggers intrinsic apoptosis by disrupting mitochondrial membrane potential, upregulating Bax, and downregulating Bcl-2, while also inhibiting PI3K/Akt and MAPK/ERK signaling pathways. Additionally, osthole acts as a PDE5 inhibitor and activates the Wnt/β-catenin pathway, which may contribute to its reported bone anabolic and neuroprotective effects.
Clinical Evidence
The majority of osthole research consists of in vitro cell studies and rodent models, with no large-scale randomized controlled trials in humans published to date. Animal studies using 25–50 mg/kg doses in murine asthma models demonstrated significant reductions in bronchoalveolar lavage eosinophils and Th2 cytokines (IL-4, IL-5). In vitro studies confirmed cytotoxic activity against HeLa, SiHa, and C-33A cervical cancer cell lines through apoptosis induction, though these findings cannot be extrapolated to clinical efficacy. The overall evidence is preliminary and hypothesis-generating; human pharmacokinetic and safety data are largely absent.
Safety & Interactions
Osthole has demonstrated hepatotoxic potential at high doses in rodent studies, raising concerns about liver safety with prolonged or high-dose supplementation in humans. As a coumarin derivative, osthole may potentiate the anticoagulant effects of warfarin and other blood thinners, increasing bleeding risk, and should be avoided alongside anticoagulant or antiplatelet therapy. Its inhibition of cytochrome P450 enzymes (notably CYP3A4 and CYP2C9) suggests potential for drug-drug interactions affecting the metabolism of numerous pharmaceuticals. Osthole is contraindicated during pregnancy due to its historically documented abortifacient properties in traditional medicine and lack of safety data.
Synergy Stack
Hermetica Formulation Heuristic
Also Known As
7-methoxy-8-(3-methyl-2-butenyl)coumarin8-prenyl-7-methoxycoumarinCnidium monnieri extract compoundAngelica pubescens compoundShe Chuang Zi compoundDu Huo compoundOsthol
Frequently Asked Questions
What is osthole and where does it come from?
Osthole (7-methoxy-8-(3-methyl-2-butenyl)coumarin) is a coumarin derivative compound primarily extracted from the medicinal plants Cnidium monnieri and Angelica pubescens. It serves as one of the major bioactive components in these traditional Chinese medicine herbs and belongs to the coumarin family of natural compounds.
Can osthole help with asthma symptoms?
Animal studies suggest osthole may reduce airway inflammation and hyperresponsiveness associated with allergic asthma. Research in mice showed that doses of 25-50 mg/kg effectively reduced Th2 cytokines, which are inflammatory markers involved in asthmatic responses, though human studies are still needed.
Does osthole have anti-cancer properties?
Laboratory studies indicate osthole shows potential anti-cancer effects specifically against cervical cancer cells. In vitro research demonstrated that osthole induced apoptosis (programmed cell death) in multiple cervical cancer cell lines including HeLa, SiHa, and C-33A, though clinical trials in humans have not been conducted.
How does osthole affect skin inflammation?
In vitro studies show osthole may reduce key skin inflammation markers by decreasing levels of pro-inflammatory cytokines including IL-1β, TNF-α, CCL2, and CCL5 in cell cultures. These findings suggest potential anti-inflammatory benefits for skin conditions, though topical applications in humans require further research.
What is the chemical structure of osthole?
Osthole has the chemical name 7-methoxy-8-(3-methyl-2-butenyl)coumarin, indicating it contains a methoxy group at position 7 and a prenyl side chain at position 8 of the coumarin backbone. This specific structural arrangement is responsible for its bioactive properties and distinguishes it from other coumarin compounds.
What does the current research evidence show about osthole's effectiveness in humans?
Most osthole research to date has been conducted in laboratory cell cultures and animal models, with very limited human clinical trials. While animal studies show promising effects on airway inflammation and immune markers at doses of 25-50 mg/kg, these results have not yet been replicated in controlled human studies. Any claims about osthole's effectiveness in people remain preliminary and require further clinical investigation.
Are there known drug interactions with osthole?
Limited research exists on osthole's potential interactions with medications in humans. As a coumarin derivative, osthole may theoretically interact with blood-thinning medications or drugs metabolized through cytochrome P450 pathways, though this has not been formally studied. Anyone taking prescription medications should consult a healthcare provider before adding osthole supplements to avoid potential interactions.
Who should avoid taking osthole supplements?
Osthole should be avoided by pregnant and nursing women due to lack of safety data in these populations. Individuals with bleeding disorders, those taking anticoagulant medications, or people with known coumarin sensitivity should exercise caution and seek medical guidance before use. People planning surgery should inform their healthcare provider about osthole use due to potential effects on clotting.
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