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S -Petasin is the main sesquiterpene of  Petasites formosanus , a traditional folk medicine used to treat hypertension, tumors and asthma in Taiwan. The aim of the present study was to investigate its inhibitory effects on phosphodiesterase (PDE) 1–5, and on ovalbumin (OVA)-induced airway hyperresponsiveness (AHR) in a murine model of allergic asthma.  S -Petasin concentration-dependently inhibited PDE3 and PDE4 activities with 50% inhibitory concentrations (IC 50 ) of 25.5, and 17.5  μ M, respectively. According to the Lineweaver-Burk analysis,  S -petasin competitively inhibited PDE3 and PDE4 activities with respective dissociation constants for inhibitor binding ( K   i ) of 25.3 and 18.1  μ M, respectively. Both IC 50  and  K   i  values for PDE3 were significantly greater than those for PDE4.  S -Petasin (10–30  μ mol/kg, administered subcutaneously (s.c.)) dose-dependently and significantly attenuated the enhanced pause ( P   enh ) value induced by methacholine (MCh) in sensitized and challenged mice. It also significantly suppressed the increases in total inflammatory cells, lymphocytes, neutrophils, eosinophils and levels of cytokines, including interleukin (IL)-2, IL-4 and IL-5, tumor necrosis factor (TNF)- α  and interferon (IFN)- γ  in bronchoalveolar lavage fluid (BALF) of these mice. In addition,  S -petasin (10–30  μ mol/kg, s.c.) dose-dependently and significantly attenuated total and OVA-specific immunoglobulin E (IgE) levels in the serum and BALF, and enhanced the IgG 2a  level in serum of these mice. The PDE4 H  value of  S -petasin was >300  μ M; therefore, its PDE4 H /PDE4 L  value was calculated to be >17. In conclusion, the present results for  S -petasin at least partially explain why  Petasites formosanus  is used as a folk medicine to treat asthma in Taiwan.

evidence-based complementary and alternative medicine

<i>S</i>-Petasin, the Main Sesquiterpene of<i>Petasites formosanus</i>, Inhibits Phosphodiesterase Activity and Suppresses Ovalbumin-Induced Airway Hyperresponsiveness

S-Petasin, the Main Sesquiterpene ofPetasites formosanus, Inhibits Phosphodiesterase Activity and Suppresses Ovalbumin-Induced Airway Hyperresponsiveness