Baohuoside I is an inhibitor of CXCR4, and downregulates CXCR4 expression at 12-25 μM. Baohuoside I (0-25 μM) suppresses NF-κB activation in a dose-dependent manner, suppresses CXCL12 induced the invasion of cervical cancer cells. Baohuoside I also inhibits invasion of breast cancer cells. Baohuoside I inhibits A549 cell viability, with IC ₅₀ s of 25.1 μM at 24 h, 11.5 μM and 9.6 μM at 48 h and 72 h, respectively. Baohuoside I ((25 μM) suppresses the caspase cascade in A549 cells, elevates ROS levels and activates JNK and p38 ^MAPK signaling cascade. Baohuoside I (3.125, 6.25, 12.5, 25.0 and 50.0 μg/mL) significantly and dose-dependently blocks the growth of esophageal squamous cell carcinoma Eca109 cells, with an IC ₅₀ of 4.8 μg/mL at 48 h.

Baohuoside I (25 mg/kg) decreases β-catenin protein levels, cyclin D1 and survivin expression in nude mice.