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In the present study, we investigated whether tussilagone, a natural product derived from Tussilago farfara, significantly affects the production and gene expression of airway MUC5AC mucin. Confluent NCI-H292 cells were pretreated with tussilagone for 30 min and then stimulated with EGF (epidermal growth factor) or PMA (phorbol 12-myristate 13-acetate) for 24 h or the indicated periods. The MUC5AC mucin gene expression was measured by RT-PCR. Production of MUC5AC mucin protein was measured by ELISA. To elucidate the action mechanism of tussilagone, effect of tussilagone on PMA-induced NF-κB signaling pathway was investigated by western blot analysis. Tussilagone significantly inhibited the production of MUC5AC mucin protein and down-regulated the expression of MUC5AC mucin gene, induced by EGF or PMA. Tussilagone inhibited PMA-induced activation (phosphorylation) of inhibitory kappa B kinase (IKK), and thus phosphorylation and degradation of inhibitory kappa Ba (IκBα). Tussilagone inhibited PMA-induced phosphorylation and nuclear translocation of nuclear factor kappa B (NF-κB) p65. This, in turn, led to the down-regulation of MUC5AC protein production in NCI-H292 cells. These results suggest that tussilagone can regulate the production and gene expression of mucin by acting on airway epithelial cells through regulation of NF-κB signaling pathway.

Tussilagone (TSL) and its allied sesquiterpenoids were considered as the main active principles of the flower buds of Tussilago farfara, which has been widely used in China as an antitussive herbal medicine. Six new bisabolane-type sesquiterpenoids, tussfararins A-F (1-6), along with 12 known sesquiterpenoids, were isolated from the flower buds of T. farfara. Structures of the new compounds were elucidated by extensive spectroscopic analysis. The biological analysis showed that compounds 1, 3, 6, and 7 inhibited nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells with IC50 values of 13.6-24.4 mu M.

The flower bud of Tussilago farfara L., called Farfarae Flos, has traditionally been used in Oriental medicine for the treatment of bronchitis and asthma. To establish a standard for quality control as well as the reliable identification of Farfarae Flos, the contents of five standards, rutin (1), isoquercetin (2), 3,5-dicaffeoylquinic acid (3), tussilagone (4), and tussilagonone (5), were determined by quantitative high-performance liquid chromatography (HPLC)/photodiode array (PDA) analysis. The five standards were separated on a YoungJinBioChrom Aegispak C18-L (250-mm×4.6-mm, 5-µm) column by gradient elution using 0.03% trifluoroacetic acid in water (A), with acetonitrile (B) as the mobile phase. The flow rate was 1.0 mL/min, and the UV detector wavelength was set at 220 nm. The method was successfully used in the analysis of Farfarae Flos from different geographic origins with relatively simple conditions and procedures, and the results demonstrated satisfactory linearity, recovery, precision, accuracy, stability, and robustness. The HPLC analytical method for pattern recognition analysis was validated by repeated analysis of 62 Farfarae Flos samples. This result indicated that the established HPLC/PDA method is suitable for quantitation and pattern recognition analyses for the quality evaluation of Farfarae Flos.

A simple and rapid high-performance liquid chromatographic method was used to study the pharmacokinetics of tussilagone, one of the main bioactive constituents in the flower buds of Tussilago farfara L. of traditional Chinese medicines, in rat plasma. Plasma was deproteinized by ethyl acetate for sample clean-up. The drugs were separated on a Dikma Diamonsil C18 column (4.6 x 250 mm, 5.0 microm), and detected by UV absorption at 220 nm. Methanol-water (75:25, v/v) was used as the mobile phase. It was applied to the pharmacokinetic study of tussilagone in rats after a dose of 5 mg/kg by intravenous administration and a dose of 200 mg/kg by intragastrical administration. A biphasic phenomenon with a rapid distribution followed by a slower elimination phase was observed from the plasma concentration-time curve by intravenous administration, while the plasma concentration-time curve of tussilagone conformed to a one-compartment model by intragastrical administration. The absolute bioavailability of tussilagone is about 1.31%.

1. Traditional Chinese herbal medicine has long used Kuandong Hua (Tussilago farfara L.) in the treatment of various respiratory conditions. 2. Recently, it has been found that an extract of this plant (7R,14R)-14-acetoxy-7-[(2'E)-3'-methylpent-2'-enoyloxy ]-oplopanone, is a potent cardiovascular and respiratory stimulant. 3. This compound has been named Tussilagone (TUS) and when administered intravenously, has been shown to produce an instant and dose dependent pressor effect in anesthetized dogs (0.02-0.3 mg/kg), cats (0.02-0.5 mg/kg), and rats (0.4-4 mg/kg). 4. This pressor effect is similar to that of dopamine; however, no tachyphylaxis has been observed. 5. In addition to its cardiovascular effects TUS produced a significant stimulation of respiration in experimental animals. 6. The acute intravenous LD50 in mice of this compound was 28.9 mg/kg.