The flowering process has been reported to play crucial roles in improving the flavor and efficacy of fermented tea. leaves containing many beneficial ingredients are a suitable plant source for tea processing. In this study, we isolated a β-glucosidase-producing fungus BSX001 from the fermented tea and used leaves (HRL) as a substrate to explore the detailed process of bioconversion of some important functional factors. The results show that the contents of total phenolic compounds and flavonoids increased significantly after seven days, especially flavonoid aglycones (e.g., quercetin, kaempferol, and isorhamnetin). Such compounds greatly enhance the antioxidative activity of fermented products. Metabolic analysis of the standard compounds (rutin, quercetin-3-glucoside, kaempferol-3-glucoside, quercetin, isorhamnetin-3-glucoside, isorhamnetin, and kaempferol) further confirmed the effective biotransformation by . Mechanisms of the bioconversion could be involved in deglycosylation, dihydroxylation, and O-methylation. Our findings expand the understanding of tea fermentation process and provide further guidance for the fermented tea industry.