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Dendrobium, a genus of orchids celebrated for their ornamental, medicinal, and culinary uses, is the focus of this study, which examines the metabolite profiles and bioactivity of five species: Dendrobium officinale, Dendrobium nobile, Dendrobium crepidatum, Dendrobium chrysotoxum, and Dendrobium denneanum. Utilizing UPLC-Q-TOF-MSE analysis, we have identified 88 compounds from the stems and leaves of these species. Notably, extracts from D. denneanum and D. chrysotoxum exhibited the highest antioxidant activities as demonstrated by DPPH, ABTS radical scavenging, and FRAP assays. Additionally, D. officinale showed significant anti-hepatoma activity with an IC50 value of 104 μg/mL. Multivariate analysis, hierarchical cluster analysis, and metabolites correlation analysis further elucidated the bioactive potential of these species. This comprehensive approach revealed distinct metabolite profiles that correlate with the observed bioactivities. The antioxidant activities of D. denneanum and D. chrysotoxum were particularly noteworthy, suggesting their potential as natural sources of antioxidants for pharmaceutical and nutraceutical applications. The anti-hepatoma activity of D. officinale, with its notable IC50 value, indicates its promise as a therapeutic agent against liver cancer. The findings underscore the richness of bioactive compounds in Dendrobium species, highlighting their antioxidant and anti-hepatoma properties. These insights pave the way for further research into the medicinal utilization of Dendrobium leaves and contribute to the development of novel applications in healthcare and wellness industries. The potential health benefits identified in this research emphasize the importance of preserving and studying these valuable plant species for their diverse bioactivities.

P-glycoprotein (P-gp) highly expressed in cancer cells can lead to multidrug resistance (MDR) and the combination of anti-cancer drugs with P-gp inhibitor has been a promising strategy to reverse MDR in cancer treatment. In this study, we established a label-free and detergent-free system combining surface plasmon resonance (SPR) biosensor with styrene maleic acid (SMA) polymer membrane proteins (MPs) stabilization technology to screen potential P-gp inhibitors. First, P-gp was extracted from MCF-7/ADR cells using SMA polymer to form SMA liposomes (SMALPs). Following that, SMALPs were immobilized on an SPR biosensor chip to establish a P-gp inhibitor screening system, and the affinity between P-gp and small molecule ligand was determined. The methodological investigation proved that the screening system had good specificity and stability. Nine P-gp ligands were screened out from 50 natural products, and their affinity constants with P-gp were also determined. The in vitro cell verification experiments demonstrated that tetrandrine, fangchinoline, praeruptorin B, neobaicalein, and icariin could significantly increase the sensitivity of MCF-7/ADR cells to Adriamycin (Adr). Moreover, tetrandrine, praeruptorin B, and neobaicalein could reverse MDR in MCF-7/ADR cells by inhibiting the function of P-gp. This is the first time that SMALPs-based stabilization strategy was applied to SPR analysis system. SMA polymer can retain P-gp in the environment of natural lipid bilayer and thus maintain the correct conformation and physiological functions of P-gp. The developed system can quickly and accurately screen small molecule ligands of complex MPs and obtain affinity between complex MPs and small molecule ligands without protein purification.