Purpose: To investigate the phytochemical analysis and bioactivity screening of some Asteraceae medicinal plants. Methods: The chemical constituents were isolated by column chromatography and elucidated using chemical and extensive spectroscopic methodologies including gas chromatoraphy-mass spectrometry (GC-MS), Fourier transform infrared spectroscopy (FTIR), as well as 1D and 2D nuclear magnetic resonance (NMR). The plant extracts were obtained by solvent extraction method while hydrodistillation was used to isolate plant essential oils. Furthermore, cup-plate agar diffusion was applied for antimicrobial activity evaluation while minimum inhibitory concentration (MIC) was assessed by microdilution technique. Results: Centaurea pseudosinaica, Tripleurospermum auriculatum, and Koelpinia linearis afforded previously undescribed three coumarins (xanthotoxin, cirsimaritin, salvigenins) from C. pseudosinaica, one steroid (estradiol) and a pentacyclic triterpene (β-amyrin) from T. auriculatum and a coumarin (santin) from K. linearis in good yields. In addition, the plant extracts and oils exhibited remarkable bioactivities including antifungal, antibacterial and antipyretic etc. Conclusion: The results reveal the presence of bioactive phytomolecules from Asteraceae plant extracts and volatile oils from three Asteraceae plants. Keywords: C. pseudosinaica, T. auriculatum, K. linearis, Xanthotoxin, Salvigenin, Cirsimaritin, Santin, Estradiol, β-amyrin, Antimicrobial activity
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