Traditional Chinese medicine (TCM) has been widely applied for the prevention and cure of various diseases for centuries. Ingredient with pharmacological activity is the key to the application of TCM. Hence, it is of significance to separate and detect active ingredients in TCM effectively. Micro/nanomaterial is the promising candidate for adsorption and sensing due to its unique physical and chemical properties. For years, many efforts have been made to develop functional micro/nanomaterials to realize the effective adsorption or sensing of bioactive compounds in TCM. In this review, we discussed recent progresses in the application of various functional micro/nanomaterials for adsorption or detection (electrochemical detection, fluorescent detection, and colorimetric detection) of active ingredients. Based on the kind of matrix materials, micro/nano-adsorbents or sensors can be classified into following categories: metal-based micro/nanomaterials, porous materials, carbon-based materials, graphene/graphite-liked micro/nanomaterials and hybrid micro/nanomaterials.