Objective To explore the inhibitory effects of Huanggen Tablets on the proliferation, migration, and invasion of glioma U87-MG cells and the possible mechanisms. Methods U87-MG cells were intervened with Huanggen Tablets components solutions at different crude drug concentrations (0.125 mg/mL, 0.25 mg/mL, 0.5 mg/mL, 1 mg/mL, 2 mg/mL, 4 mg/mL, 8 mg/mL, 16 mg/mL, 32 mg/mL, 64 mg/mL). The 50% inhibitory concentration (IC50) of the drug at 24 hours after the intervention was calculated according to the results of the CCK-8 assay, based on which the subsequent experiment was designed to set up a control group, as well as a low-dose Huanggen Tablets group, a medium-dose Huanggen Tablets group, and a high-dose Huanggen Tablets group (with crude Huanggen concentrations of 3.25 mg/mL, 6.5 mg/mL, and 13 mg/mL, respectively). The CCK8 assay and plate colony formation assay were used to detect the cell viability and relative cloning formation rate of U87-MG cells in each group. The Transwell migration and invasion assays were used to detect the relative migration and invasion rates of U87-MG cells in each group. The qRT-PCR method was used to detect the relative expression levels of miRNA-185-5p and cell division cycle 42 (CDC42) mRNA in U87-MG cells of each group. Western blotting was used to detect the relative expression levels of CDC42 and N-myc proteins in U87-MG cells of each group. Results With the increase of the administration concentration of Huanggen Tablets, the survival rate of U87-MG cells gradually decreased, and its IC50 was 13 mg/mL(crude drug) at 24 hours after the intervention. The low-, medium-, and high-dose Huanggen Tablets groups had lower cell viability after 24, 48, 72, and 96 hours of administration, decreased relative cloning formation rate after 7 days of administration, and reduced relative migration and invasion rates after 48 hours of administration, as compared with the control group (all P<0.05). After 24 hours of administration, the relative expression levels of miRNA-185-5p in the cells of the low-, medium-, and high-dose Huanggen Tablets groups were all higher than those in the control group (all P<0.05). After 24 hours of administration, the relative expression levels of CDC42 mRNA in the low- and medium-dose Huanggen Tablets groups were lower than that in the control group (all P<0.05). After 24 hours of administration, the relative expression levels of CDC42 and N-myc proteins in the low-, medium-, and high-dose Huanggen Tablets groups were all lower than those in the control group. Conclusion Huanggen Tablets can inhibit the proliferation, migration, and invasion abilities of human glioma U87-MG cells, thus exerting an anti-glioma effect. Its mechanism may be related to promoting the expression of miRNA-185-5p, which in turn inhibits the expression of CDC42.