Abstract
<jats:p>Traditional Chinese medicine (TCM) has played a great role in treating various diseases in China’s 5000-year history, from common infectious illnesses to chronic metabolic disorders. Their therapeutic efficacy mainly derives from abundant bioactive constituents within medicinal herbs and compound formulas, such as alkaloids, flavonoids, terpenoids and polysaccharides, which exert pharmacological activities through synergistic interactions. Given such extreme chemical complexity of TCM matrixes, it is infeasible to evaluate their overall quality based only on an individual marker component. High-performance liquid chromatography (HPLC) has long been a classic quantitative analysis method in such complex TCM systems, capable of precisely separating and determining the contents of certain chemical components. Nevertheless, relying merely on the content level of contained compounds as an indicator is insufficient to determine whether these ingredients actually possess biological activity. Therefore, how to effectively combine quantitative chemical analysis with activity evaluation methods has become an essential and urgent issue for comprehensive quality assessment of TCM. Due to the superiority of high sensitivity, fast response, easy accessibility, low cost, high selectivity, and simple operation, fluorescent sensors have generated great attraction in the fields of detection, diagnosis, and imaging. Integrating the separation power of HPLC with the real-time monitoring capability of fluorescent sensors enables the exploration of pharmacodynamic substances from complex TCM matrices. This hyphenated approach not only facilitates rapid identification of bioactive components but also provides a general and efficient strategy for detecting and screening natural inhibitors against other disease-related enzymes, thereby accelerating drug discovery from natural products.</jats:p>