Background: Dai antidotes are the most distinctive medicine and treatment in traditional Dai medicine. Clerodendrum chinense var. simplex, Marsdenia tenacissima (Roxb.) Moon and Arundina graminifolia (D. Don) Hochr are three Dai antidotes widely used for their “detoxifying effects”, and their use is rooted in a theoretical system significantly different and much less understood than Western or traditional Chinese medicines. This study aims to provide the mechanistic insights into the detoxifying effects of Dai antidotes, providing a modern scientific basis for understanding and developing Dai medicine as well as encouraging its use in other regions.Methods: We successively extracted the three Dai antidotes using petroleum ether, ethyl acetate, n-butanol, or water, and prepared their decoctions. Their contents of total flavonoids and polyphenols were determined by colorimetric method. Their antioxidant activity were tested by 1,1-diphenyl-2-picrylhydrazyl(DPPH), hydroxyl radical (·OH) and 2,2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals scavenging assays. Anti-bacterial activity were evaluated in terms of minimum inhibitory concentrations (MICs), minimum bactericidal concentrations (MBCs) and zones of inhibition (ZOI) against Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus. Their anti-inflammatory activity were studied in macrophages stimulated with lipopolysaccharide (LPS) through measuring the production of nitric oxide, tumor necrosis factor-α, interleukin-1β, and interleukin-6.Results: The content of total flavonoids in three Dai antidotes ranged from 22.41 to 586.39 mg/g, which is higher than the content of total polyphenols (2.76 to 28.66 mg/g). The various extracts were found to scavenge radicals of DPPH, ·OH and ABTS. They scavenged ABTS radicals much more efficiently (IC50 9.54 μg/mL) than other radicals (IC50 > 380 μg/mL). They weakly inhibited the growth of E. coli, P. aeruginosa and S. aureus. Notably, even at low concentration 60 μg/mL, the extracts can significantly down-regulate nitric oxide production, tumor necrosis factor-α, interleukin-1β, and interleukin-6 by macrophages stimulated with lipopolysaccharide. Conclusion: In conclusion, our results provide the first mechanistic insights into the detoxifying effects of three Dai antidotes, providing a basis for their optimization and for future research to strengthen Dai medicine through modern scientific practices.