Abstract Vanadium is the 21st richest element in the Earth’s crust and is an essential trace element for human body. This article describes the discovery, natural distribution, and circulation of vanadium in the human body. It sheds light on the vanadate-phosphate antagonism mechanism by studying the chemical structure. From the angle of biochemical mechanism, the article explains the regulation of vanadium compounds on kinases and phosphatases, and their influence on RNA and DNA function and reactive oxygen species. It also explores the potential pharmacological effects on the treatment of diabetes, cancer, and cardiovascular protection from the perspective of human health.