Osthole

Osthole at a Glance

Osthole is a prenylated methoxylated coumarin and the signature active of Cnidium monnieri seed (she chuang zi), also present in angelica and other Apiaceae.

Its marquee preclinical signals are bone formation — osteoblast stimulation, unusual among plant coumarins — and neuroprotection, alongside broad anti-inflammatory activity.

Osthole Is Not a Furanocoumarin

Osthole travels in company that shapes how it gets described, and the company is chemically different from it. Cnidium fruit and Angelica root both carry osthole alongside a set of linear furanocoumarins — imperatorin, bergapten, xanthotoxin, isopimpinellin — and it is those molecules, not osthole, that carry the two hazards the coumarin class is known for.

Structurally osthole is a simple coumarin with a prenyl group at C-8 and a methoxy at C-7. It has no fused furan ring, and the furan ring is the whole mechanism: it is what lets a psoralen intercalate into DNA and form cyclobutane adducts with thymine under UVA light. That photochemistry is what makes imperatorin, bergapten and xanthotoxin photo-cytotoxic and photo-genotoxic in a modelled furanocoumarin mixture ^{25Reference 25Raquet N · 2014In vitroApplication of the equivalency factor concept to the phototoxicity and -genotoxicity of furocoumarin mixtures — in vitroView study →}, and what turns Angelica sap into a documented cause of phytophotodermatitis ^{17Reference 17Knapp CF 3rd · 2009ReviewBotanical briefs: garden Angelica (Angelica archangelica) — reviewView study →}. Osthole cannot do it.

The second attribution worth separating is the drug-interaction one. “Furanocoumarins inhibit CYP3A4” is a real finding attached to specific molecules — the grapefruit-type, mechanism-based inactivation of intestinal CYP3A4 is best characterised for bergamottin, a citrus-peel furanocoumarin, and modelled quantitatively as such ^{24Reference 24Fuhr LM et al. · 2023Physiologically Based Pharmacokinetic Modeling of Bergamottin and 6,7-Dihydroxybergamottin to Describe CYP3A4 Mediated Grapefruit-Drug InteractionsView study →}, while imperatorin is a mechanism-based inactivator of CYP2B6 ^{26Reference 26Zheng L et al. · 2015In vitroImperatorin is a mechanism-based inactivator of CYP2B6 — in vitroView study →}. Neither result belongs to osthole, which has no comparable human interaction dataset of its own.

The practical consequence runs the other way from what the caution list would suggest. A photosensitivity warning on a Cnidium seed product is a whole-extract warning earned by the furanocoumarins that ride along with osthole — real, but not a property of osthole itself. And the absence of an osthole interaction signal is an absence of data, not a clearance.

What It's Used For

Osthole (7-methoxy-8-isopentenyloxycoumarin) is a simple prenylated coumarin — the dominant active molecule in the seed of Cnidium monnieri (she chuang zi), and a minor constituent of Angelica and other members of the carrot family. It has one of the broadest preclinical literatures of any single coumarin: isolated osthole shows osteogenic, neuroprotective, anti-inflammatory/anti-asthmatic, hepatoprotective, anticancer, and glucose-lowering activity across cell and rodent models ^{1Reference 1Lin H et al. · 2024ReviewOsthole, a Coumarin from Cnidium monnieri: A Review on Its Pharmacology, Pharmacokinetics, Safety, and Innovative Drug Delivery Platforms — reviewView study →2Reference 2Zhang ZR et al. · 2015ReviewOsthole: A Review on Its Bioactivities, Pharmacological Properties, and Potential as Alternative Medicine — reviewView study →}.

The catch runs through all of it: osthole is highly lipophilic and poorly water-soluble, its oral bioavailability is low and its half-life short ^{12Reference 12Sun C et al. · 2018AnimalPreparation and Pharmacokinetics Evaluation of Solid Self-Microemulsifying Drug Delivery System (S-SMEDDS) of Osthole — rat pharmacokinetic animal modelView study →14Reference 14Luo DD et al. · 2017AnimalDifferent effects of (+)-borneol and (−)-borneol on the pharmacokinetics of osthole in rats following oral administration — rat pharmacokinetic animal modelView study →}, and not a single one of these effects has been tested as the isolated molecule in a human trial. The whole-seed Cnidium extract is used traditionally, but a whole-plant result is not a molecule result.

Evidence by IndicationStrength of support · Beta

01Bone / osteoporosisPromising50%Isolated osthole; mechanistic in vitro + ovariectomized-rat in vivo; no human data

02NeuroprotectionShaky40%Isolated osthole; cell + APP/PS1 mouse models; BBB penetration modest

03Asthma / airway inflammationShaky38%Isolated osthole; resolved PDE4D structure + ovalbumin mouse model

04Fatty liver / metabolicShaky32%Isolated osthole; rat steatohepatitis + hyperlipidemia + cell glucose uptake

05AnticancerShaky22%Isolated osthole; in-vitro cell lines, high doses; sparse in vivo

06AnticonvulsantShaky28%Isolated osthole; mouse electroshock model with a measured protective index

Mechanisms

A Unifying Interpretation

Read one application at a time, osthole looks like a molecule that does everything — bone, brain, airway, liver, tumour — which is usually the signature of a weak, non-specific compound. Read across them, a single thread shows up in most: osthole raises cyclic nucleotides.

It inhibits cAMP and cGMP phosphodiesterases fairly broadly, and the elevation that follows is what the individual tissue results have in common — cAMP/PKA signalling relaxing airway smooth muscle, cGMP-linked relaxation in vascular smooth muscle and ileum, cGMP/PKG involvement in hippocampal glutamate release, and cGMP elevation behind the suppression of inflammatory mediators in the carrageenan model ^{2Reference 2Zhang ZR et al. · 2015ReviewOsthole: A Review on Its Bioactivities, Pharmacological Properties, and Potential as Alternative Medicine — reviewView study →}. The airway work is where the thread was pinned down structurally: a co-crystal placed osthole in the PDE4D catalytic site, blocking cAMP hydrolysis ^{5Reference 5Wang S et al. · 2020In vitroAirway relaxation mechanisms and structural basis of osthole for improving lung function in asthma — in vitro, structural, and mouse modelView study →}.

This is an interpretation, not a proven single mechanism, and it does not cover everything on the page — the Wnt/β-catenin–BMP osteoblast axis and the PPARα/γ lipid work sit outside it, and the ketohexokinase inhibition is a straightforward enzyme block ^{3,7,22Reference 3Tang DZ et al. · 2010In vitroOsthole stimulates osteoblast differentiation and bone formation by activation of β-catenin–BMP signaling — in vitro and ovariectomised-rat in vivo animal modelView study →Reference 7Zhao X et al. · 2018AnimalPPARα/γ antagonists reverse the ameliorative effects of osthole on hepatic lipid metabolism and inflammatory response in steatohepatitic rats — rat in vivo animal modelView study →Reference 22Le MT et al. · 2016In vitroBioactivity-Guided Identification of Botanical Inhibitors of Ketohexokinase — in vitroView study →}. But it explains why one small lipophilic coumarin keeps producing smooth-muscle relaxation and anti-inflammatory readouts in unrelated tissues, and it predicts where the molecule is most likely to be genuinely useful: somewhere a phosphodiesterase inhibitor would be useful.

Pharmacokinetics

Bioavailability is the load-bearing caveat for the entire osthole literature. Osthole is highly lipophilic and poorly water-soluble, so its oral bioavailability as the pure compound is low and variable, and it undergoes rapid, extensive metabolism (over a dozen phase-I and phase-II metabolites identified in rat urine) with a short plasma half-life ^{1Reference 1Lin H et al. · 2024ReviewOsthole, a Coumarin from Cnidium monnieri: A Review on Its Pharmacology, Pharmacokinetics, Safety, and Innovative Drug Delivery Platforms — reviewView study →12Reference 12Sun C et al. · 2018AnimalPreparation and Pharmacokinetics Evaluation of Solid Self-Microemulsifying Drug Delivery System (S-SMEDDS) of Osthole — rat pharmacokinetic animal modelView study →}. This is why so much of the applied work leans on formulation tricks: a solid self-microemulsifying delivery system (S-SMEDDS) raised osthole exposure by roughly 200% over an aqueous suspension in rats ^{12Reference 12Sun C et al. · 2018AnimalPreparation and Pharmacokinetics Evaluation of Solid Self-Microemulsifying Drug Delivery System (S-SMEDDS) of Osthole — rat pharmacokinetic animal modelView study →}, borneol co-administration markedly increased AUC and Cmax by inhibiting metabolism and aiding absorption ^{14Reference 14Luo DD et al. · 2017AnimalDifferent effects of (+)-borneol and (−)-borneol on the pharmacokinetics of osthole in rats following oral administration — rat pharmacokinetic animal modelView study →}, and brain-targeting studies use intranasal nanoemulsions to bypass poor systemic delivery ^{14Reference 14Luo DD et al. · 2017AnimalDifferent effects of (+)-borneol and (−)-borneol on the pharmacokinetics of osthole in rats following oral administration — rat pharmacokinetic animal modelView study →}. Comparative rat studies also show tissue distribution and absorption differ between pure osthole and plant-extract matrices ^{13Reference 13Shi J et al. · 2013AnimalComparative study of pharmacokinetics and tissue distribution of osthole in rats after oral administration of pure osthole and Libanotis buchtormensis supercritical extract — rat pharmacokinetic animal modelView study →}. The practical upshot: potent in-vitro concentrations are not trivially reachable from an oral dose, which tempers every downstream claim.

Clinical Trials

There are essentially no registered trials of isolated osthole; the human evidence is limited to traditional whole-seed Cnidium monnieri use, which is a plant-extract exposure and cannot be read as a molecule result. The osthole evidence base is entirely preclinical.

Last checked: July 2026.

Isolate vs. Plant Studies

Almost all of the osthole literature is isolate work, and that is unusually clean for a plant coumarin — the osteoblast, PDE4D, PPAR and ketohexokinase results were all obtained with purified osthole at stated concentrations, not with an extract ^{3,5,7,22Reference 3Tang DZ et al. · 2010In vitroOsthole stimulates osteoblast differentiation and bone formation by activation of β-catenin–BMP signaling — in vitro and ovariectomised-rat in vivo animal modelView study →Reference 5Wang S et al. · 2020In vitroAirway relaxation mechanisms and structural basis of osthole for improving lung function in asthma — in vitro, structural, and mouse modelView study →Reference 7Zhao X et al. · 2018AnimalPPARα/γ antagonists reverse the ameliorative effects of osthole on hepatic lipid metabolism and inflammatory response in steatohepatitic rats — rat in vivo animal modelView study →Reference 22Le MT et al. · 2016In vitroBioactivity-Guided Identification of Botanical Inhibitors of Ketohexokinase — in vitroView study →}. The other half is missing: there is no human trial of the isolate at all, so the strength of the preclinical attribution never converts into a human result.

The plant-side evidence points the other way, and the two rarely meet. Cnidium monnieri fruit is used whole in traditional practice for the indications osthole is least studied for — the aphrodisiac/androgenic reputation rests on whole-seed extract in rodent sexual-behaviour work, not on isolated osthole, and cannot be read as a molecule result. Where the two have been run side by side, they mostly agree: in the ketohexokinase screen, purified osthole (IC50 0.7 µM) and whole Angelica archangelica extract (IC50 22.6–57.3 µg/mL) were both among the top hits in the same assay, and the extract also blocked fructose-induced ATP depletion and triglyceride rise in hepatocytes — the isolate accounting for at least part of what the plant did ^{22Reference 22Le MT et al. · 2016In vitroBioactivity-Guided Identification of Botanical Inhibitors of Ketohexokinase — in vitroView study →}.

Pharmacokinetics is where the isolate/plant distinction stops being academic. Rats given pure osthole and rats given a Libanotis supercritical extract containing it show different absorption and tissue distribution ^{13Reference 13Shi J et al. · 2013AnimalComparative study of pharmacokinetics and tissue distribution of osthole in rats after oral administration of pure osthole and Libanotis buchtormensis supercritical extract — rat pharmacokinetic animal modelView study →}, so a dose of the molecule and a dose of the plant that contains it are not interchangeable exposures.

Its Role in Plants

Osthole is built on the general phenylpropanoid route to coumarins: p-coumaroyl-CoA is ortho-hydroxylated and cyclised — with coumarin synthase performing a step long assumed to be spontaneous — to give umbelliferone, which is then prenylated at C-8 and methylated at the C-7 hydroxyl. That sequence was proved by rebuilding it: introducing the umbelliferone pathway plus the downstream prenyltransferase and methyltransferase into brewer’s yeast produced osthole from sugar ^{19Reference 19Wang P et al. · 2023Biosynthesis of the Plant Coumarin Osthole by Engineered Saccharomyces cerevisiaeView study →}.

Its function in the plant is defensive, and the modern evidence is unusually direct. Against two-spotted spider mite and green peach aphid, isolated osthole was the most acutely toxic of the five coumarins tested from Cnidium fruit, killing nymphs and adults dose-dependently, cutting fecundity, lengthening development, and acting as a feeding deterrent in leaf-choice assays ^{18Reference 18Dong F et al. · 2023Contact Toxicity, Antifeedant Activity, and Oviposition Preference of Osthole against Agricultural Pests — laboratory bioassayView study →}. It is not uniformly repellent, though: oriental fruit fly females preferred to lay eggs in juice dosed at 0.02 mg/mL, so at low concentration the same molecule reads as an attractant to a different insect ^{18Reference 18Dong F et al. · 2023Contact Toxicity, Antifeedant Activity, and Oviposition Preference of Osthole against Agricultural Pests — laboratory bioassayView study →}. That dual role — toxin to the herbivores that chew the plant, signal to something else — is a better description of what a defensive coumarin does than “insecticide” alone.

The pharmacology and the ecology were never separate. The 1930s chemistry that established osthole’s structure was published in a series titled Über pflanzliche Fischgifte — “on plant fish poisons” — because masterwort was being worked up as a fish and insect poison in the first place ^{15,27Reference 15Späth E · 1933Späth E, Pesta O (1933). Über pflanzliche Fischgifte, III. Mitteil.: Konstitution des Osthols (aus Imperatoria Ostruthium). Berichte der deutschen chemischen Gesellschaft. https://doi.org/10.1002/cber.19330660527View study →Reference 27Butenandt A · 1932Untersuchungen über pflanzliche Fisch- und InsektengifteView study →}.

Prevalence in Nature

Osthole is an Apiaceae molecule first, with a scattering of occurrences in the Rutaceae. It is concentrated in fruits, seeds and rhizomes rather than leaves, and it is one component of a coumarin mixture in every plant that makes it — never the sole coumarin present.

The richest documented source is the ripe fruit of Cnidium monnieri (Fructus Cnidii, she chuang zi), measured at 11.4 mg/g — about 1.1% of dry weight ^{18Reference 18Dong F et al. · 2023Contact Toxicity, Antifeedant Activity, and Oviposition Preference of Osthole against Agricultural Pests — laboratory bioassayView study →}, where it sits alongside imperatorin, isopimpinellin, bergapten and several angelicin-type coumarins ^{2Reference 2Zhang ZR et al. · 2015ReviewOsthole: A Review on Its Bioactivities, Pharmacological Properties, and Potential as Alternative Medicine — reviewView study →}. Masterwort (Peucedanum ostruthium) rhizome carries it as one of seven quantified main coumarins together with oxypeucedanin, ostruthol, imperatorin, isoimperatorin and ostruthin — and, because masterwort rhizome is an ingredient of alpine bitters and liqueurs, that is a real if small route of human dietary exposure ^{23Reference 23Vogl S et al. · 2011Identification and Quantification of Coumarins in Peucedanum ostruthium (L.) Koch by HPLC-DAD and HPLC-DAD-MSView study →}. Angelica (A. archangelica) root and Angelica pubescens (du huo) both carry it, and reviews also record it in Citrus and Clausena species ^{2,22Reference 2Zhang ZR et al. · 2015ReviewOsthole: A Review on Its Bioactivities, Pharmacological Properties, and Potential as Alternative Medicine — reviewView study →Reference 22Le MT et al. · 2016In vitroBioactivity-Guided Identification of Botanical Inhibitors of Ketohexokinase — in vitroView study →}.

Quantified figures outside Cnidium are scarce — most reports establish presence rather than concentration — so the comparison below is honest about which sources have a number attached.

Major Natural Sources

Source	Part	Osthole content	Notes
Cnidium monnieri (she chuang zi)	Ripe fruit	~11.4 mg/g (~1.1% dry wt) 18Reference 18Dong F et al. · 2023Contact Toxicity, Antifeedant Activity, and Oviposition Preference of Osthole against Agricultural Pests — laboratory bioassayView study →	The reference source; dominant coumarin of the drug
Peucedanum ostruthium (masterwort)	Rhizome	Quantified, one of seven main coumarins 23Reference 23Vogl S et al. · 2011Identification and Quantification of Coumarins in Peucedanum ostruthium (L.) Koch by HPLC-DAD and HPLC-DAD-MSView study →	Alpine bitters and liqueurs; the plant osthole is named after
Angelica archangelica	Root	Present; not quantified here 22Reference 22Le MT et al. · 2016In vitroBioactivity-Guided Identification of Botanical Inhibitors of Ketohexokinase — in vitroView study →	Extract active in the same assay as the isolate
Angelica pubescens (du huo)	Root	Present; not quantified here 2Reference 2Zhang ZR et al. · 2015ReviewOsthole: A Review on Its Bioactivities, Pharmacological Properties, and Potential as Alternative Medicine — reviewView study →	Second major TCM source
Citrus, Clausena spp.	Fruit / leaf	Reported occurrence 2Reference 2Zhang ZR et al. · 2015ReviewOsthole: A Review on Its Bioactivities, Pharmacological Properties, and Potential as Alternative Medicine — reviewView study →	Rutaceae outliers

Discovery & Synthesis

Osthole is named for the plant it came out of: masterwort, Imperatoria ostruthium (now Peucedanum ostruthium), an alpine Apiaceae long used in bitters and in veterinary practice. The molecule was pulled out of that plant as part of a systematic 1930s effort to identify what made it a fish and insect poison — Butenandt and Marten worked through the masterwort constituents in 1932 ^{27Reference 27Butenandt A · 1932Untersuchungen über pflanzliche Fisch- und InsektengifteView study →}, and the following year Ernst Späth and Otto Pesta established osthole’s structure as 7-methoxy-8-prenylcoumarin ^{15Reference 15Späth E · 1933Späth E, Pesta O (1933). Über pflanzliche Fischgifte, III. Mitteil.: Konstitution des Osthols (aus Imperatoria Ostruthium). Berichte der deutschen chemischen Gesellschaft. https://doi.org/10.1002/cber.19330660527View study →}. Späth’s group settled the neighbouring molecules from the same rhizome in the same run, imperatorin among them, which is why osthole and imperatorin share a discovery record. The first total synthesis followed quickly: Späth and Holzen, 1934 ^{16Reference 16Späth E · 1934Synthese des Osthols (XView study →}.

Manufacture today is extraction, not synthesis. Commercial osthole is obtained from Cnidium monnieri fruit, which at over 1% dry weight makes extraction straightforward and cheap ^{18Reference 18Dong F et al. · 2023Contact Toxicity, Antifeedant Activity, and Oviposition Preference of Osthole against Agricultural Pests — laboratory bioassayView study →}, and the molecule’s poor aqueous solubility means the applied engineering effort has gone into delivery rather than supply — self-microemulsifying systems, nanoemulsions and absorption enhancers ^{12,14Reference 12Sun C et al. · 2018AnimalPreparation and Pharmacokinetics Evaluation of Solid Self-Microemulsifying Drug Delivery System (S-SMEDDS) of Osthole — rat pharmacokinetic animal modelView study →Reference 14Luo DD et al. · 2017AnimalDifferent effects of (+)-borneol and (−)-borneol on the pharmacokinetics of osthole in rats following oral administration — rat pharmacokinetic animal modelView study →}. A third route now exists in the laboratory: the complete pathway has been reconstructed in engineered Saccharomyces cerevisiae, reaching 255.1 mg/L in fed-batch fermentation — a fermentation supply independent of the crop, though not yet at extraction’s cost ^{19Reference 19Wang P et al. · 2023Biosynthesis of the Plant Coumarin Osthole by Engineered Saccharomyces cerevisiaeView study →}.

Patents: not yet researched.

Toxicity & Safety

Osthole carries a low toxicity flag: reviews describe it as generally well tolerated in animal studies with no signature acute organ toxicity at the doses used ^{1,2Reference 1Lin H et al. · 2024ReviewOsthole, a Coumarin from Cnidium monnieri: A Review on Its Pharmacology, Pharmacokinetics, Safety, and Innovative Drug Delivery Platforms — reviewView study →Reference 2Zhang ZR et al. · 2015ReviewOsthole: A Review on Its Bioactivities, Pharmacological Properties, and Potential as Alternative Medicine — reviewView study →}, and in a mouse xenograft study at an effective anticancer dose neither renal nor hepatic toxicity appeared ^{1Reference 1Lin H et al. · 2024ReviewOsthole, a Coumarin from Cnidium monnieri: A Review on Its Pharmacology, Pharmacokinetics, Safety, and Innovative Drug Delivery Platforms — reviewView study →}. There is no formal human safety database, because the isolated molecule has never been trialled in people.

The liver is the organ to watch. A 2024 review notes reports of osthole-associated liver injury and cautions specifically about combination use ^{1Reference 1Lin H et al. · 2024ReviewOsthole, a Coumarin from Cnidium monnieri: A Review on Its Pharmacology, Pharmacokinetics, Safety, and Innovative Drug Delivery Platforms — reviewView study →}, and in cultured human liver cells (L02) osthole reduced viability and triggered apoptosis through endoplasmic-reticulum stress — GRP78/CHOP, IRE1α, PERK and caspase-4 — with G2/M arrest ^{20Reference 20Shen Z et al. · 2019In vitroOsthole induced apoptosis in human normal liver cells by regulating cell proliferation and endoplasmic reticulum stress — in vitroView study →}. That is a cell-line finding at concentrations chosen to produce an effect, not a demonstrated human hazard, and it sits awkwardly beside the several rodent studies in which osthole protected the liver from steatosis and CCl₄ injury ^{7,8Reference 7Zhao X et al. · 2018AnimalPPARα/γ antagonists reverse the ameliorative effects of osthole on hepatic lipid metabolism and inflammatory response in steatohepatitic rats — rat in vivo animal modelView study →Reference 8Zhang Y et al. · 2007AnimalTherapeutic effect of osthole on hyperlipidemic fatty liver in rats — rat in vivo animal modelView study →}. Both results can be true at different exposures; what they jointly argue is that the liver is where an osthole dose would first show itself.

Phototoxicity is not an osthole property. The photosensitivity risk attached to Cnidium seed and Angelica preparations belongs to the furanocoumarins that accompany it ^{17,25Reference 17Knapp CF 3rd · 2009ReviewBotanical briefs: garden Angelica (Angelica archangelica) — reviewView study →Reference 25Raquet N · 2014In vitroApplication of the equivalency factor concept to the phototoxicity and -genotoxicity of furocoumarin mixtures — in vitroView study →}. Equally, no human drug-interaction data exist for osthole itself; the CYP results commonly quoted for “coumarins” were obtained with other molecules ^{24,26Reference 24Fuhr LM et al. · 2023Physiologically Based Pharmacokinetic Modeling of Bergamottin and 6,7-Dihydroxybergamottin to Describe CYP3A4 Mediated Grapefruit-Drug InteractionsView study →Reference 26Zheng L et al. · 2015In vitroImperatorin is a mechanism-based inactivator of CYP2B6 — in vitroView study →}, and an absence of an interaction signal here is an absence of study.

Osthole and its source seed carry an androgen-like reputation from rodent sexual-behaviour work with whole Cnidium extract, so hormone-sensitive contexts warrant caution. No dedicated reproductive- or developmental-toxicity package for the isolated molecule was located.

Dosage

There is no established human dose for isolated osthole, and no human study to derive one from. The figures below are the exposures used in the research described above.

Two things make the gap between these and a human dose wider than usual. The rodent doses are milligrams per kilogram given by injection or by gavage, and osthole’s low oral bioavailability and rapid metabolism mean an equivalent oral human exposure is not a simple weight scaling ^{1,12Reference 1Lin H et al. · 2024ReviewOsthole, a Coumarin from Cnidium monnieri: A Review on Its Pharmacology, Pharmacokinetics, Safety, and Innovative Drug Delivery Platforms — reviewView study →Reference 12Sun C et al. · 2018AnimalPreparation and Pharmacokinetics Evaluation of Solid Self-Microemulsifying Drug Delivery System (S-SMEDDS) of Osthole — rat pharmacokinetic animal modelView study →}. And much of the applied literature reaches its effective concentrations only with a delivery vehicle — a microemulsion, a nanoemulsion, or borneol co-dosing to slow metabolism ^{12,14Reference 12Sun C et al. · 2018AnimalPreparation and Pharmacokinetics Evaluation of Solid Self-Microemulsifying Drug Delivery System (S-SMEDDS) of Osthole — rat pharmacokinetic animal modelView study →Reference 14Luo DD et al. · 2017AnimalDifferent effects of (+)-borneol and (−)-borneol on the pharmacokinetics of osthole in rats following oral administration — rat pharmacokinetic animal modelView study →} — so the plain compound taken by mouth is not the exposure most of these results were obtained at.

These are doses studied in research and are not a personal recommendation.

References

1. Lin H, et al. (2024). Osthole, a Coumarin from Cnidium monnieri: A Review on Its Pharmacology, Pharmacokinetics, Safety, and Innovative Drug Delivery Platforms — review. The American Journal of Chinese Medicine. https://pubmed.ncbi.nlm.nih.gov/39327653/
2. Zhang ZR, et al. (2015). Osthole: A Review on Its Bioactivities, Pharmacological Properties, and Potential as Alternative Medicine — review. Evidence-Based Complementary and Alternative Medicine. https://pubmed.ncbi.nlm.nih.gov/26246843/
3. Tang DZ, et al. (2010). Osthole stimulates osteoblast differentiation and bone formation by activation of β-catenin–BMP signaling — in vitro and ovariectomised-rat in vivo animal model. Journal of Bone and Mineral Research. https://pubmed.ncbi.nlm.nih.gov/20200936/
4. Li SH, et al. (2017). Osthole Stimulated Neural Stem Cells Differentiation into Neurons in an Alzheimer’s Disease Cell Model via Upregulation of MicroRNA-9 and Rescued Hippocampal Neurons in APP/PS1 Transgenic Mice — in vitro and mouse model. Frontiers in Neuroscience. https://pubmed.ncbi.nlm.nih.gov/28659755/
5. Wang S, et al. (2020). Airway relaxation mechanisms and structural basis of osthole for improving lung function in asthma — in vitro, structural, and mouse model. Science Signaling. https://pubmed.ncbi.nlm.nih.gov/33234690/
6. Yang Q, et al. (2020). Osthole attenuates ovalbumin-induced lung inflammation via the inhibition of IL-33/ST2 signaling in asthmatic mice — mouse model. International Journal of Molecular Medicine. https://pubmed.ncbi.nlm.nih.gov/32700747/
7. Zhao X, et al. (2018). PPARα/γ antagonists reverse the ameliorative effects of osthole on hepatic lipid metabolism and inflammatory response in steatohepatitic rats — rat in vivo animal model. Inflammopharmacology. https://pubmed.ncbi.nlm.nih.gov/28236037/
8. Zhang Y, et al. (2007). Therapeutic effect of osthole on hyperlipidemic fatty liver in rats — rat in vivo animal model. Acta Pharmacologica Sinica. https://pubmed.ncbi.nlm.nih.gov/17303003/
9. Che Y, et al. (2018). Osthole enhances antitumor activity and irradiation sensitivity of cervical cancer cells by suppressing ATM/NF-κB signaling — in vitro. Oncology Reports. https://pubmed.ncbi.nlm.nih.gov/29989651/
10. Jiang G, et al. (2016). Anti-tumor effects of osthole on ovarian cancer cells in vitro — in vitro. Journal of Ethnopharmacology. https://pubmed.ncbi.nlm.nih.gov/27566206/
11. Lee WH, et al. (2011). Osthole enhances glucose uptake through activation of AMP-activated protein kinase in skeletal muscle cells — in vitro. Journal of Agricultural and Food Chemistry. https://pubmed.ncbi.nlm.nih.gov/22098542/
12. Sun C, et al. (2018). Preparation and Pharmacokinetics Evaluation of Solid Self-Microemulsifying Drug Delivery System (S-SMEDDS) of Osthole — rat pharmacokinetic animal model. AAPS PharmSciTech. https://pubmed.ncbi.nlm.nih.gov/29845504/
13. Shi J, et al. (2013). Comparative study of pharmacokinetics and tissue distribution of osthole in rats after oral administration of pure osthole and Libanotis buchtormensis supercritical extract — rat pharmacokinetic animal model. Journal of Ethnopharmacology. https://pubmed.ncbi.nlm.nih.gov/23142197/
14. Luo DD, et al. (2017). Different effects of (+)-borneol and (−)-borneol on the pharmacokinetics of osthole in rats following oral administration — rat pharmacokinetic animal model. Molecular Medicine Reports. https://pubmed.ncbi.nlm.nih.gov/28440419/
15. Späth E, Pesta O (1933). Über pflanzliche Fischgifte, III. Mitteil.: Konstitution des Osthols (aus Imperatoria Ostruthium). Berichte der deutschen chemischen Gesellschaft. https://doi.org/10.1002/cber.19330660527
16. Späth E, Holzen H (1934). Synthese des Osthols (X. Mitteil. über natürliche Cumarine). Berichte der deutschen chemischen Gesellschaft. https://doi.org/10.1002/cber.19340670221
17. Knapp CF 3rd, Elston DM (2009). Botanical briefs: garden Angelica (Angelica archangelica) — review. Cutis. https://pubmed.ncbi.nlm.nih.gov/19911672/
18. Dong F, Chen X, Men X, et al. (2023). Contact Toxicity, Antifeedant Activity, and Oviposition Preference of Osthole against Agricultural Pests — laboratory bioassay. Insects. https://pubmed.ncbi.nlm.nih.gov/37754693/
19. Wang P, Fan Z, Wei W, et al. (2023). Biosynthesis of the Plant Coumarin Osthole by Engineered Saccharomyces cerevisiae. ACS Synthetic Biology. https://doi.org/10.1021/acssynbio.3c00321
20. Shen Z, Chen J, Lu H (2019). Osthole induced apoptosis in human normal liver cells by regulating cell proliferation and endoplasmic reticulum stress — in vitro. Environmental Toxicology. https://pubmed.ncbi.nlm.nih.gov/30848542/
21. Luszczki JJ, Wojda E, Andres-Mach M, et al. (2009). Anticonvulsant and acute neurotoxic effects of imperatorin, osthole and valproate in the maximal electroshock seizure and chimney tests in mice: a comparative study. Epilepsy Research. https://pubmed.ncbi.nlm.nih.gov/19406619/
22. Le MT, Lanaspa MA, Cicerchi CM, et al. (2016). Bioactivity-Guided Identification of Botanical Inhibitors of Ketohexokinase — in vitro. PLoS One. https://pubmed.ncbi.nlm.nih.gov/27322374/
23. Vogl S, Zehl M, Picker P, et al. (2011). Identification and Quantification of Coumarins in Peucedanum ostruthium (L.) Koch by HPLC-DAD and HPLC-DAD-MS. Journal of Agricultural and Food Chemistry. https://doi.org/10.1021/jf104772x
24. Fuhr LM, Marok FZ, Fuhr U, et al. (2023). Physiologically Based Pharmacokinetic Modeling of Bergamottin and 6,7-Dihydroxybergamottin to Describe CYP3A4 Mediated Grapefruit-Drug Interactions. Clinical Pharmacology & Therapeutics. https://pubmed.ncbi.nlm.nih.gov/37307228/
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