Objective: To study the effects of baicalein on the proliferation

invasion and migration of A549 cells

and investigate its effects on vascularization of human umbilical vein endothelial cells (HUVEC)

as well as the antitumor effect of baicalein on A549 cell xenografts in vivo

and the antitumor mechanism of baicalein by the method of serum metabnomics. Method: In vitro

the thiazolyl blue terazolium bromide (MTT) assay was used to detect the effect of baicalein on A549 cells proliferation. The effect of baicalein on invasion and migration of A549 cells were detected by transwell assay. The anti-angiogenic effect of baicalein on HUVEC was detected by tubule formation experiment. In vivo:anti-tumor efficacy of baicalein was evaluated in nude mice models of human lung cancer xenograft. The nude mice were divided into model group

cisplatin group

and baicalein groups (50

100 μmol·L-1). The serum samples from nude mice were subjected to metabolomics analysis after baicalein treatment by using gas chromatography/mass spectrometry (GC/MS)

looking for the differential metabolites and related metabolic pathways. Result: The growth of A549 cells was significantly inhibited by different concentrations of baicalein

and the 50% concentration of inhibition(IC50) of baicalein were 43.02

31.11

28.42 μmol·L-1 respectively at 24 h

48 h and 72 h. Different concentrations of baicalein (5

10

20 μmol·L-1) could inhibit the invasion and migration abilities of A549 cells. Baicalein (10

20 μmol·L-1) could inhibit the tubule structure formation of HUVEC (P<0.05). The growth of A549 cell xenograft was inhibited by baicalein (50 mg·kg-1) in vivo. A total of 14 differential metabolites and 7 related metabolic pathways in the serum were found after intervention with baicalein. Conclusion: Baicalein could inhibit the proliferation

invasion and migration of A549 cells and the tubule formation of HUVEC in vitro

with inhibitory effect on the growth of A549 cell xenograft. The changed metabolic pathways in the baicalein group including amino acid metabolism

carbohydrate metabolism and energy metabolism in the serum were found

and the antitumor mechanism of baicalein maybe relevant to these metabolic pathways.