Pathological angiogenesis is recognized as a common denominator underlying a variety of deadly and debilitating human diseases, including cancer, age-related macular degeneration (AMD) and various inflammatory diseases. Currently, angiogenesis inhibitors have become attractive strategy for the treatment of cancer and AMD, leading to a breakthrough in pharmacological research. Discovery of bioactive natural products from Chinese herbal medicine, medical plants and marine organisms is the promising strategy for finding new drug candidates. Natural products also have received a considerable attention as shown by the numerous studies published on their broad-spectrum biological activities. However, the anti-angiogenic property of natural products in current scientific literatures has largely remained a mystery. Therefore, we conducted the anti-angiogenesis study in both in vitro and in vivo models for pursuing novel angiogenesis inhibitors from natural products. Several potential candidate inhibitors have been identified in our lab from nature-based resources. The anti-angiogenic effects and mechanisms of these compounds will be discussed in this presentation.