Catestatin, a multifunctional neuroendocrine peptide derived from chromogranin A, is widely expressed in the nervous, endocrine, immune, and cardiovascular systems. Catestatin can bind to nicotinic acetylcholine receptors, activating the phosphatidylinositol 3-kinase/protein kinase B (PI3K/Akt),mitogen-activated protein kinase/extracellular signal-regulated kinase(MAPK/ERK), toll-like receptor 4/p38 mitogen-activated protein kinase (TLR4/p38 MAPK), and Notch1 signaling pathways, exerting various biological effects such as antioxidation, promotion of angiogenesis, regulation of immune homeostasis, and modulation of glucose and lipid metabolism. Recent studies have shown that catestatin is involved in the pathophysiological processes of several diseases, including hypertension, atherosclerosis, inflammatory bowel disease, diabetes, and preeclampsia. This review focuses on recent research progress on the origin, structure, receptors, associated signaling pathways, biological effects, and pathophysiological significance of catestatin, with the aim of providing a theoretical basis for further mechanistic research and potential clinical applications of catestatin.