Petasin health benefit, use for migraine, allergy, vessel dilation
February 1 2017

Petasin is a substance found in plants, particularly in butterbur, that has a number of physiological activities.

Petasin and blood pressure
Eremophilanlactones isolated from roots of Petasites hybridus and S-petasin have blood vessel dilation effects.

Petasin in Butterbur
Quantitative analysis of petasin and pyrrolizidine alkaloids in leaves and rhizomes of in situ grown Petasites hybridus plants.
Planta Med. 1998. Universität Basel, Institut für Pharmazie--Pharmazeutische Biologie, Witterswil, Switzerland.
Various locations in Switzerland were screened for Petasites hybridus plants with high petasin and low pyrrolizidine alkaloid content. The mean petasin content of the various populations ranged from 7.4 to 15 mg/g dry weight in rhizomes and from 3.3 to 11 mg/g dry weight in leaves. Mean pyrrolizidine alkaloid content in rhizomes ranged from 5 to 90 ppm whereas leaves contained between 0.02 to 1.50 ppm. These results suggest that leaves might be a preferable source for harvesting compared to the underground organ due to the finding of high petasin contents and consistently lower amounts of toxic pyrrolizidine alkaloids.

Physiological effects of petasin
Effects of S-petasin on cyclic AMP production and enzyme activity of P450scc in rat zona fasciculata-reticularis cells.
Eur J Pharmacol. 2004. Department of Chemical Engineering, Chinese Culture University, Shih-Lin, Taipei, Taiwan, ROC.
Petasites hybridus is used in Chinese herbal medicine. S petasin is a bioactive compound isolated from leaves or roots of P. hybridus, which has been used to relieve gastrointestinal pain, lung disease, and spasms of urogenital tract. We have demonstrated that petasin inhibited corticosterone release from rat zona fasiculata-reticularis cells. This study explored the effects of petasin on cellular adenosine 3':5'-cyclic monophosphate (cAMP) production, the functions of steroidogenic enzymes including cytochrome P450 side-chain cleavage enzyme (P450scc), 11beta-hydroxylase, and the expression levels of steroidogenic acute regulatory protein or P450scc. In summary, the actions of petasin mediate the inhibition of cAMP formation, decrease the activities of key enzymes P450scc and 11beta-hydroxylase, and reduce mRNA of steroidogenic acute regulatory protein and expression of steroidogenic acute regulatory protein.

S-petasin and butterbur lactones dilate vessels through blockage of voltage gated calcium channels and block DNA synthesis.
Eur J Pharmacol. 2008. Department of Pharmacology and Pharmacotherapy, Faculty of Pharmaceutical Sciences, University of Copenhagen, Copenhagen, Denmark.
Eremophilanlactones isolated from roots of Petasites hybridus and S-petasin have vasodilatory effects.

Petasin and allergy
The butterbur extract petasin has no effect on skin test reactivity induced by different stimuli: a randomized, double-blind crossover study using histamine, codeine, methacholine, and aeroallergen solutions.
J Investig Allergol Clin Immunol. 2006. Division of Allergology, Department of Rheumatology and Clinical Immunology/Allergology, Inselspital, Bern, Switzerland.
Petasin was recently introduced on the market as a potent herbal anti-allergic drug for treatment of respiratory allergies such as hay fever. Few clinical studies have been performed so far addressing the clinical effectiveness of Ze 339. We evaluated the anti-allergic properties of petasin using skin prick tests with different stimuli, such as codeine, histamine, methacholine, and a relevant inhalant allergen. A randomized, double-blind, placebo-controlled study was performed in which petasin was compared to acrivastine, a short-acting antihistamine, in 8 patients with respiratory allergy and in 10 nonatopic, healthy volunteers. In this study we found no antiallergic, particularly antihistaminic, effect of petasin in skin tests using a variety of stimuli often used to evaluate immediate skin test reactivity. The mechanism by which petasin is effective in the treatment of seasonal allergic rhinitis still needs to be elucidated.