Objective: To investigate the effects of Temozolomide (TMZ) on the growth and angiogenesis of human glioma U87 cells in vitro and in vivo. Methods: Flow cytometry was used to determine the cell cycle progression of U87 cells induced by TMZ, EdU method was used to detect the effect of TMZ on the proliferation activity of U87 cells, CCK-8 method was used to determine the effect of TMZ on the survival of U87 cells, nude mice tumorigenesis experiment was used to detect the effect of TMZ on the growth of U87 xenografts in vivo, and immunohistochemical method was used to detect the expressions of Ki-67, BDNF and CD31 in tumors. Angiogenesis was detected by chicken chorioallantoic membrane (CAM) model. The effect of TMZ on the secretion of angiogenesis-related proteins VEGF, TGF-βand FGF in U87 cells were detected by ELISA. Results: TMZ increased the proportion of G0/G1 and G2 phase cells in U87 cells, decreased the proportion of S phase cells and inhibited the survival and proliferation of U87 cells in vitro. TMZ therapy inhibited the growth of transplanted tumors and the expression of vascular endothelial markers in nude mice, and rEdUced the level of angiogenesis-related proteins in U87 cells. Conclusion: TMZ inhibits the angiogenesis of glioma U87 cells in vitro and in vivo. This inhibitory effect may be associated with decreased the protein expressions of Ki-67, BDNF, VEGF, TGF-β and FGF.