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Tri-Yannarose is a Thai traditional herbal medicine formula composed of <i>Areca catechu</i>, <i>Azadirachta indica</i>, and <i>Tinospora crispa</i>. It possesses antipyretic, diuretic, expectorant, and appetite-stimulating effects. This study aimed to evaluate the antioxidant activities, cytotoxicity, and chemical constituents of an aqueous extract following a Tri-Yannarose recipe and its plant ingredients. The phytochemical analysis was performed using LC-QTOF-MS. Antioxidant activities were determined using DPPH, ABTS, TPC, TFC, FRAP, NBT, MCA, and ORAC assays. Cytotoxicity was investigated using a methyl thiazol tetrazolium (MTT) assay. In addition, the relationship between the chemical composition of Tri-Yannarose and antioxidant activities was investigated by examining the structure–activity relationship (SAR). The results of the LC-QTOF-MS analysis revealed trigonelline, succinic acid, citric acid, and other chemical constituents. The aqueous extract of the recipe showed significant scavenging effects against ABTS and DPPH radicals, with IC₅₀ values of 1054.843 ± 151.330 and 747.210 ± 44.173 µg/mL, respectively. The TPC of the recipe was 92.685 mg of gallic acid equivalent/g of extract and the TFC was 14.160 mg of catechin equivalent/g of extract. All extracts demonstrated lower toxicity in the Vero cell line according to the MTT assay. In addition, the SAR analysis indicated that prenyl arabinosyl-(1–6)-glucoside and quinic acid were the primary antioxidant compounds in the Tri-Yannarose extract. In conclusion, this study demonstrates that Tri-Yannarose and its plant ingredients have potent antioxidant activities with low toxicity. These results support the application of the Tri-Yannarose recipe for the management of a range of disorders related to oxidative stress.