Fermented tea (Cha-miang in Thai) is a local product made by traditional food preservation processes in Northern Thailand that involve steaming fresh tea leaves followed by fermenting in the dark. Information on changes in nutritive values, bioactive compounds, antioxidant activities, and health properties that occur during the steaming and fermenting processes of tea leaves is, however, limited. Changes in nutritive values, phenolics, antioxidant activities, and in vitro health properties through inhibition of key enzymes that control obesity (lipase), diabetes (α-amylase and α-glucosidase), hypertension (angiotensin-converting enzyme (ACE)), and Alzheimer’s disease (cholinesterases (ChEs) and β-secretase (BACE-1)) of fermented tea were compared to the corresponding fresh and steamed tea leaves. Results showed that energy, carbohydrate, and vitamin B1 increased after steaming, while most nutrients including protein, dietary fiber, vitamins (B2, B3, and C), and minerals (Na, K, Ca, Mg, Fe, and Zn) decreased after the steaming process. After fermentation, energy, fat, sodium, potassium, and iron contents increased, while calcium and vitamins (B1, B2, B3, and C) decreased compared to steamed tea leaves. However, the contents of vitamin B1 and iron were insignificantly different between fresh and fermented tea leaves. Five flavonoids (quercetin, kaempferol, cyanidin, myricetin, and apigenin) and three phenolic acids (gallic acid, caffeic acid, and p-coumaric acid) were identified in the tea samples. Total phenolic content (TPC) and antioxidant activities increased significantly after steaming and fermentation, suggesting structural changes in bioactive compounds during these processes. Steamed tea exhibited high inhibition against lipase, α-amylase, and α-glucosidase, while fermented tea possessed high anti-ChE and anti-ACE activities. Fresh tea exhibited high BACE-1 inhibitory activity. Results suggest that tea preparations (steaming and fermentation) play a significant role in the amounts of nutrients and bioactive compounds, which, in turn, affect the in vitro health properties. Knowledge gained from this research will support future investigations on in vivo health properties of fermented tea, as well as promote future food development of fermented tea as a healthy food.