Asiaticoside (0, 100, 250, and 500 mg/L) dose-dependently inhibits keloid fibroblasts proliferation. Asiaticoside (100, 250, and 500 mg/L) decreases the expression of collagen protein and mRNA, reduces the expression of TGF-bRI, TGF-bRII protein, and mRNA, increases the expression of Smad7, but does not affect Smad2, Smad3, Smad4, phosphorylated Smad2, and phosphorylated Smad3 in keloid fibroblasts. Asiaticoside (12.5 and 50, and 25 and 50 µg/mL) prevents endothelial cells from hypoxia-induced inhibition of cell viability and NO production. Asiaticoside (50 µg/mL) also protects endothelial cells from hypoxia-induced apoptosis and upregulates and phosphorylation of AKT/eNOS in hypoxia-exposed HPAECs.