Traditional Chinese Medicine (TCM) has demonstrated significant therapeutic potential in the treatment of various diseases through its multi-component and multi-target mechanisms. The renin-angiotensin system (RAS) is a critical regulatory system involved in the maintenance of cardiovascular homeostasis and fluid-electrolyte balance. Angiotensin-converting enzyme 2 (ACE2), a receptor protein widely expressed in multiple human tissues, is particularly abundant in the lungs, cardiovascular system, kidneys, and gastrointestinal tract. Angiotensin(1-7)[Ang(1-7)], the primary metabolite of ACE2, is distributed across organs such as the heart, lungs, brain, and kidneys. It functions as a bioactive peptide with cardioprotective and renoprotective properties, exerting its effects by binding to the Mas receptor (MasR) and mediating beneficial physiological responses. The ACE2/Ang(1-7)/MasR axis, as an essential branch of the RAS, plays a pivotal role in tissue protection and homeostasis.This review summarizes recent advancements in the application of TCM in regulating the ACE2/Ang(1-7)/MasR axis for the treatment of diseases, including COVID-19, acute lung injury, myocardial infarction/acute heart failure, hypertension, and acute kidney injury. With the continuous progress in TCM research and a deeper understanding of the ACE2/Ang(1-7) pathway, this axis represents a promising target for developing novel therapeutic strategies and improving clinical outcomes.