Chinese Tibetan tea made from the tender leaves of Malus transitoria is a widely consumed health drink, but there are few reports on its chemical composition and biological activity. In this study, we found that a 50% ethanol extract of M. transitoria had good antioxidant and α-glucosidase inhibitory activities in vitro. Guided by in vitro bioassays, chromatographic separation and purification were conducted, and the most active fraction in M. transitoria was determined. UPLC-Orbitrap-MS/MS was used to further quickly and comprehensively characterize the chemical composition. Library searches, MS/MS fragmentation patterns of two isolated reference compounds, and bibliography were used to annotate 81 compounds, of which 2 were new compounds, and 79 were identified from M. transitoria for the first time. This study provides a scientific basis for the development of antioxidant and anti-diabetic functional foods from M. transitoria.