Objective: To explore the effects of the containing serum of Xiaoai Jiedu decoction with different concentrations on proliferation and glycolysis of human colon cancer cells and investigate its action mechanism. Method: Eight new zealand rabbits were randomized into the serum containing medicine[40 g · (kg · d)-1 of Xiaoai Jiedu decoction]group and the blank serum group (equivoluminal normal saline).Both groups received intragastric administration for 3 days to prepare serum containing Xiaoai Jiedu decoction and blank serum.Human colon cancer HT-29 and HCT-116 cells were cultured with pharmacological serum of Xiaoai Jiedu decoction (5%

10% and 15%)

and then their effects on the human colon cancer cells' proliferation was examined by methyl thiazolyl tetrazolium assay.The amount of lactic acid produced by HT-29 and HCT-116 cells was measured by lactic acid test kit

and the amount of glucose produced by HT-29 and HCT-116 cells was measured by glucose test kit.The expression levels of hexokinase 2 (HK2)

pyruvate dehydrogenase kinase 1 (PDK1)

lactate dehydrogenase (LDHA)

and Hypoxia inducible factor-1α (HIF-1α) were detected by using Western blot. Result: Serum containing Xiaoai Jiedu decoction exhibited suppressive effects on HT-29 and HCT-116 proliferation.The effect of 15% serum containing Xiaoai Jiedu decoction was the best

with inhibition rate of 42.7% and 50.2% respectively for HT-29 and HCT-116 cells.Western blot analysis indicated that as compared with blank control group

the serum containing Xiaoai Jiedu decoction reduced the expression of HK2

PDK1

LDHA and HIF-1α (P<0.05)

and with the increase of concentration

the expression was decreased.The results of lactic acid and glucose test kit showed that as compared with the blank control group

the serum containing Xiaoai Jiedu decoction can reduce the levels of lactic acid and glucose (P<0.05) and with the increasing of concentration

the levels of lactic acid and glucose were decreased. Conclusion: The serum containing Xiaoai Jiedu decoction can inhibit the proliferation of human colon cancer HT-29 and HCT-116 cells by inhibiting the process of the glycolysis.Inhibitory mechanisms of glycolysis might be associated with reducing the expression of HIF-1α

thereby reducing the expression of glycolytic enzymes HK2

PDK1

and LDHA.