| Summary: | The carnivorous pitcher plant <i>Sarracenia purpurea</i> exhibits many ethnobotanical uses, including the treatments of type 2 diabetes and tuberculosis-like symptoms. In this study, we prepared different extracts from the leaves (pitchers), stems, and roots of <i>S. purpurea</i> and investigated their antioxidant and anticancer properties. To evaluate the extraction efficiency, we individually used different solvents, namely methanol, ethanol, acetone, and distilled water, for <i>S. purpurea</i> extract preparations. The root extract of <i>S. purpurea</i>, obtained by 100% acetone (<i>S. purpurea-root-acetone</i>), had the highest anticancer activities, antioxidation capacity (the DPPH activity with IC<sub>50</sub> of 89.3 ± 2.2 μg/mL), antibacterial activities, total phenolic content (33.4 ± 0.7 mg GAE/g), and total flavonoid content (107.9 ± 2.2 mg QUE/g). The most abundant compounds in <i>S. purpurea-root-acetone</i> were identified using gas chromatography–mass spectrometry; 7,8-Dihydro-α-ionone was the major compound present in <i>S. purpurea-root-acetone</i>. In addition, the co-cytotoxicity of <i>S. purpurea-root-acetone</i> (combined with the clinical anticancer drug 5-fluorouracil (5-FU) on the survival, apoptosis, proliferation, and migration of the 4T1 mammary carcinoma) was examined. The combination of 5-FU with <i>S. purpurea-root-acetone</i> could be highly efficient for anti-4T1 cells. We also found that <i>S. purpurea-root-acetone</i> could inhibit the enzymatic activity of human dihydroorotase (huDHOase), an attractive target for potential anticancer chemotherapy. The sic most abundant compounds in <i>S. purpurea-root-acetone</i> were tested using an in silico analysis via MOE-Dock software for their binding affinities. The top-ranked docking conformations were observed for 7,8-dihydro-α-ionone and stigmast-5-en-3-ol, suggesting the inhibition potential against huDHOase. Overall, the collective data in this study may indicate the pharmacological potentials of <i>S. purpurea-root-acetone</i> for possible medical applications.
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