Emerging evidences suggest that gut microbiota-derived substances play a pivotal role in the regulation of host homeostasis including vascular function. Actually, these substances and/or their metabolites can be presented in circulation and local tissue and their levels are often abnormal in the pathophysiological states. Therefore, to determine the role of them in physiological function is important in human health. On the other hand, vascular dysfunction is a key event in the initiation and progression of systematic complications of cardiovascular, kidney and metabolic diseases including hypertension, dyslipidemia, diabetes, and atherosclerosis. Although abnormalities in endothelial and vascular smooth muscle cells play an important role on vascular dysfunction, emerging evidences has suggested that gut microbiota-derived substances can directly or indirectly affect these cellular functions. The present review will focus on the relationship between vascular function and indoxyl sulfate or trimethylamine-N-oxide (TMAO).