Dark tea has long been recognized for its health-promoting benefits, attributed to its complex phytochemical composition. However, the specific bioactive compounds responsible for these beneficial effects remain inadequately characterized. This study aimed to explore the impact of dark tea water extract (DTE) on digestive enzyme activity, antioxidant capacity, and glucose-lipid balance. DTE was fractioned into four fractions using gel separation, followed by analysis with high-performance liquid chromatography and quasi-targeted metabolomics. The 30 % ethanol elution (EEA) and 50 % ethanol elution (EEB) fractions showed stronger antioxidant and enzyme inhibition effects compared to the whole DTE. The EEA fraction was rich in 5 catechins and 26 additional phytochemicals, while the EEB fraction contained high levels of caffeine, ECG, and 29 other phytochemicals. Notably, significant correlations were observed between quercetin-3,4'-O-di-β-glucopyranoside and 3-(2-Naphthyl)-L-alanine with digestive enzyme inhibition. Cellular studies revealed the ability of EEA and EEB to reduce lipid accumulation, improve glycolipid metabolism, and alleviate oxidative stress by increasing SOD, CAT, and GSH levels while decreasing MDA and ROS in HepG2 cells. Furthermore, 34 flavonoids, 2 alkaloids, 2 terpenes, 2 alcohols and polyols, 2 phenylpropanoids and polyketides, 1 organoheterocyclic compound were directly linked to the antioxidant activity and the modulation of glucose and lipid levels. These findings offer valuable insights into the phytochemical profiles of dark tea and its potential health benefits.