Objective: To explore the effects of the decoction and active ingredients of Epimedii Folium combined with Ligustri Lucidi Fructus on transforming growth factor-β1 (TGF-β1)/Smads pathway in glucocorticoid-induced osteoporosis (GIOP) rats. Method: The 49 male SD rats were randomly divided into 7 groups:the normal group

the model group

the extract of Epimedii Folium combined with Ligustri Lucidi Fructus groups (200

100 mg·kg-1)

the decoction groups (7

3.5 g·kg-1) and Caltrate calcium D3 group (0.277 3 g·kg-1)

with 7 rats in each group. All of the rats were given dexamethasone (1 mg·kg-1) through intramuscular injection twice a week to establish osteoporosis model. After eight weeks

the rats were put to death

and left femurs were collected to measure weight

calculate the ratio of wet weight

dry weight and ash weight to bone volume. The protein expressions of TGF-β1

p-Smad2/3

Smad4

Smad7 were observed by immunofluorescence staining. Result: Body weight

bone mass and the expressions of TGF-β1

p-Smad2/3 and Smad4 in model group were lower than those in normal group (P<0.01)

the protein levels of TGF-β1

p-Smad2/3 and Smad4 significantly decreased (P<0.01)

while Smad7 protein expression were higher in femurs (P<0.01). Compared with the model group

the body weight and bone mass increased significantly in each administration group

the protein levels of TGF-β1

p-Smad2/3 and Smad4 were increased (P < 0.05

P < 0.01)

and Smad7 protein expression was decreased in all Epimedii Folium and Ligustri Lucidi Fructus treatment groups (P<0.01). Conclusion: The mechanism of the combination of Epimedii Folium and Fructus Ligustri Lucidi in treating GIOP may be related to the up-regulation on the expressions of TGF-β1

p-Smad2/3 and Smad4

down-regulation on the expression of Smad7

and strengthening of the function of osteoblasts

and reduction of bone loss in GIOP rats.