Insulin resistance (IR) is known to be a critical factor, which can lead to the onset of type 2 diabetes. Traditional Chinese medicine (TCM) has special advantages in treating IR, but the active components and action mechanisms of most TCM remain unclear. Therefore, the elucidation of the potential mechanisms is a major challenge in TCM research. In the study, we tried to elucidate the potential pharmacological efficacy and mechanism of breviacapine for improving IR through network analysis and validate the possible biological target for its quality evaluation. We computationally recognized the active components, potential targets, and the targets closely related to IR by using integrative analysis based on network pharmacology approach. We also established the active components-targets network, protein interactions network and analyzing the biological functions and pathways of targets to evaluate the links between components and pharmacological actions to help explain the action mechanisms of breviscapine. Based on the network analysis, our experimental data preliminarily confirmed that breviscapine could improve IR in HepG2 cells, which may be associated with the dynamic regulation of the PTP1B. This study combined network pharmacology with partial experiment validation to clarify the underlying mechanism of breviscapine in improving IR and thus laid the experimental foundation for the depth exploration of its functional mechanism.