Background Ophiopogon D is an important natural organic compound in Ophiopogon japonicus , which often has significant biological activity. Purpose The purpose of this review is to systemically summarize and discuss the pharmacological activity and underlying mechanisms of OP-D in recent years. Method PubMed and Web of Science were searched with the keywords:“ Ophiopogon japonicus ”, “Ophiopogon D” “pharmacology”, and “pharmacokinetics”. There was no restriction on the publication year, and the last search was conducted on 1 Jan 2024. Results Emerging evidence suggests that OP-D possess numerous pharmacological activities, including bone protection, cardiovascular protection, immune regulation, anti-cancer, anti-atherosclerosis, anti-inflammatory and anti-NAFLD. Conclusion OP-D has a potential value in the prevention and treatment of many diseases. We hope that this review will contribute to therapeutic development and future studies of OP-D.