Diabetes mellitus (DM) is a global health issue in the twenty-first century, and there are numerous challenges in preventing and alleviating its chronic complications. The herb Epimedium has beneficial
therapeutic effects on various human diseases, including DM. Its major
flavonoid component,
icariin, has significant anti-DM activity and may help improve pancreatic β-cell dysfunction and
insulin resistance. Furthermore, preclinical evidence has shown that
icariin and its in vivo bioactive form,
icariside II, have preventive and
therapeutic effects on several
diabetic complications, including
diabetic cardiomyopathy, diabetic vascular endothelial disorder,
diabetic nephropathy, and diabetic
erectile dysfunction. In this review, we present the general and toxicological information concerning
icariin and
icariside II and review the anti-DM effects of
icariin from a molecular perspective. Additionally, we discuss the potential benefits of
icariin and
icariside II on the important pathological mechanisms of various
diabetic complications. Despite positive preclinical evidence, additional investigations are needed before relevant clinical studies can be conducted. Therefore, we conclude with suggestions for future research. Hopefully, this review will provide a comprehensive molecular perspective for future research and product development related to
icariin and
icariside II in treating DM and
diabetic complications.