A series of traditional Chinese medicine decoction have been proved to inhibit pathological neovascularization in both clinical practice and laboratory experiment. Small molecules of traditional Chinese medicine are the active components of compound decoction of traditional Chinese medicine. Some small molecules of traditional Chinese medicine can inhibit neovascularization by suppressing the expression of vascular endothelial cell growth factors in different ways, which provides new ideas for the treatment of angiogenesis diseases. Neovascularization plays an important role not only in retinal angiogenesis diseases such as diabetic retinopathy, but also in the development and progression of malignant tumors. In this review, the process and the mechanism of neovascularization were briefly described, and the mechanisms of inhibiting neovascularization by flavonoids, saponins, alkaloids and other small molecules of traditional Chinese medicine were reviewed in detail.