Histidine-containing dipeptides such as carnosine (β-alanine-L-histidine) and anserine (β-alanine-L-methyl histidine) are not incorporated into proteins; instead, they are stored in peripheral skeletal muscle and other organs, including the kidney, retina, and myocardium. Carnosine has several protective functions in health and disease state. This mini review provides a current overview of the knowledge of the histidine containing dipeptides in disease accompanied by oxidative stress like diabetes and diabetic microvascular complications. It also highlights the performed experimental studies of histidine-containing dipeptides in relation to tissue damage related to (non-invasive) human studies. Finally, it describes future perspectives of the therapeutic use of histidine-containing dipeptides in health and disease.