Gerberae Piloselloidis Herba is widely used to treat cough and asthma in China. However, its effects on allergic asthma as related to its chemical compositions have not been fully elucidated, and there is a scarcity of methods to determine multi‐component contents for quality control. In this study, protective effects of Gerberae Piloselloidis Herba on ovalbumin‐induced asthma models were investigated, while qualitative and quantitative analyses of multiple constituents in Gerberae Piloselloidis Herba were conducted by using an ultrahigh‐performance liquid chromatography–Q Exactive hybrid quadrupole‐orbitrap high‐resolution accurate mass spectrometry and an ultrahigh‐performance liquid chromatography–photodiode array detection. The results showed that Gerberae Piloselloidis Herba could significantly mitigate asthma symptoms, reduce eosinophils counts in the bronchoalveolar lavage fluid, as well as decrease IgE, IL‐5, and IL‐13 concentration, and inflammatory cellular infiltration in lung tissues. A total of 51 compounds were tentatively identified, in which the content of 10 representative compounds was determined in 24 batches of Gerberae Piloselloidis Herba by using an ultrahigh‐performance liquid chromatography method with good linearity, precision, repeatability, accuracy, and stability. This research presents a comprehensive strategy combining biological activity evaluation with chemical profiling, providing a useful and comprehensive reference for further application and quality control of Gerberae Piloselloidis Herba.

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Gerberae Piloselloidis Herba, a traditional Chinese medicine, is often employed to treat such lung‐related diseases as coughs, asthma, and pulmonary carbuncles in southwest China. Our previous study demonstrated that its active fraction, prepared from Gerberae Piloselloidis Herba, exerts an obvious beneficial effect on asthma. However, the pharmacokinetics of its major constituents remain unclear. Therefore, an ultra‐performance mass spectrometry‐electrospray ionization‐tandem mass spectrometry method was successfully established to simultaneously perform the pharmacokinetics of the main 11 components of the active fraction between normal and ovalbumin‐induced asthmatic mice. Compared to the normal group, in asthmatic mice the peak concentration of arbutin, marmesin, caffeoylquinic acids, and flavonoid glycosides clearly increased, while for luteolin it significantly declined; the area under the curve for arbutin and luteolin showed an increase, but the values of marmesin, caffeoylquinic acids, and flavonoid glycosides revealed a decline; the peak time for arbutin, caffeoylquinic acids and flavonoid glycosides decreased, while for marmesin and luteolin it significantly augmented; apart from marmesin, the half‐life for all compounds shortened significantly. It is indicated that the pathology of asthma could lead to an alteration in the pharmacokinetic profiles of the 11 components in plasma, providing a reference for further exploration of the pharmacodynamic basis of the anti‐bronchial effect of Gerberae Piloselloidis Herba.

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