Drug-derived carbon dots (CDs) not only have excellent photoluminescence properties of CDs, but also maintain pharmacological effects of original drugs, so as to realize extended applications for both bioimaging and chemotherapy. In this work, metformin (Met)-derived CDs (Met-CDs) as multifunctional nanocarriers with tumor cell imaging and cancer therapy are synthesized using Met and citric acid as precursors. The created Met-CDs exhibit obvious resistance to photobleaching, significant pH sensitivity in acidic environments, good pH stability in alkaline environments, and high temperature sensitivity. In addition, we further investigate the biological activity of Met-CDs using diabetic cell models, which demonstrate the ability of Met-CDs to treat diabetes and reduce the production of reactive oxygen species in diseased cells. Subsequently, human alveolar adenocarcinoma basal epithelial cells (A549) are cultured in both normal glucose and low glucose media, and different concentrations of Met and Met-CDs are added to investigate the effect of Met-CDs on A549 cells. Finally, we successfully utilize the prepared Met-CDs to image live A549 cells in vitro in normal glucose medium. The Met-CDs prepared in this work reveal high potential to be used as both fluorescent probes and drug agents for tumor therapy, realizing controllable integrated diagnosis and treatment of diseases.