Osthole benefit and research, osthol, review of health benefits and side effects
April 20 2018 by
Ray Sahelian, M.D.

Osthole - also spelled osthol - is a type of coumarin. It is found in cnidium monnieri and several other plants. Osthol may increase androgen, gonadotropin and nitric oxide synthase (NOS) activity. One mouse study indicates osthol had androgen like effect and gonadotropin like effect. Little research has been done with osthole, however it appears that this substance may have a role to play in liver health, brain function, and vasodilation (dilation of blood vessels).

Plants, herbs that contain osthole
A number of herbs contain it, including cnidium and angelica pubescens root.

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Q. We have been trying to buy A Chinese herb Osthole A derivative of (angelica pubescence maxim). Could you show us how to find a source?
   A. As of 2018, I do not believe it is sold over the counter as a supplement to the public.


Osthole benefit for fatty liver
Osthole improves fat milk-induced fatty liver in rats: modulation of hepatic PPAR-alpha/gamma-mediated lipogenic gene expression.
Planta Med. 2007.
The objectives of this study were to determine the therapeutic effect of osthole, an active constituent isolated from Cnidium monnieri, in hyperlipidemic fatty liver rats and investigate the possible mechanism of the osthole treatment. Osthole exerts therapeutic effects on fat milk-induced fatty liver in rats, by regulating mRNA expression of the target genes of CYP7A, DGAT, L-FABP and FATP4 via increasing the PPARalpha/gamma mRNA expression.

Liver cancer
Chemical aspects of coumarin compounds for the prevention of hepatocellular carcinomas.
Curr Med Chem Anti-Cancer Agents. 2005.
The normalization of plasma alanine aminotransferase (ALT) has been proved to be a strategy for preventing the development of hepatocellular carcinoma in hepatitis C virus (HCV)-infection. Glycyrrhizin, a plant medicine, normalizes plasma ALT and prevents HCC. However, glycyrrhizin is administered intravenously and thereby chemical which is effective on oral administration is required. Coumarin compounds are active components of herbs used for the treatment of various diseases. The ability of coumarin compounds to lower plasma ALT were examined using mice concanavalin A-induced hepatitis and mice anti-Fas antibody-induced hepatitis. We conclude that osthole will become a leading chemical for synthesizing a compound which prevents liver cancer on oral administration.

PLoS One. May 2012. Growth inhibition and apoptosis induced by osthole, a natural coumarin, in hepatocellular carcinoma.

Mental effects
Osthole improves aspects of spatial performance in ovariectomized rats.
Am J Chin Med. 2004.
The present study was designed to investigate the ameliorating effects of Cnidiuim monnieri and osthole, a constituent of cnidium, on the spatial performance deficit in scopolamine (SCOP)-treated or ovariectomized rats. Osthole improved the performance deficit in ovariectomized rats. The action mechanism of the effects of osthole on performance deficits was related to the estrogen-like properties and activating the central cholinergic neuronal system.

Biol Pharm Bulletin. 2015. The Coumarin Derivative Osthole Stimulates Adult Neural Stem Cells, Promotes Neurogenesis in the Hippocampus, and Ameliorates Cognitive Impairment in APP/PS1 Transgenic Mice.

Pulmonary hypertension
Eur Journal Pharmacology. 2013. Osthole relaxes pulmonary arteries through endothelial phosphatidylinositol 3-kinase/Akt-eNOS-NO signaling pathway in rats. Pulmonary arterial hypertension is a life-threatening disease lacking effective therapies. Osthole is a natural coumarin compound isolated from Angelica pubescens Maxim., which possesses hypotensive effect.

Osthole relaxes trachea
The relaxant action of osthole isolated from Angelica pubescens in guinea-pig trachea.
Naunyn Schmiedebergs Archives Pharmacolology. 1994.
Osthole, theophylline and higher concentrations of nifedipine suppressed the contraction response curves of tracheal smooth muscle caused by carbachol, prostaglandin F2 alpha (PGF2 alpha), U46619 (thromboxane A2 analogue) and leukotriene C4 (LTC4) in a concentration-dependent manner. It is concluded that osthole exerts a non-specific relaxant effect on the trachealis by inhibiting the cAMP and cGMP phosphodiesterases.