With the constant development of the drug screening technology, new screening methods and techniques have came to the fore, driving drug screening to grow rapidly and efficiently with a high throughput. Characterized by micro-scale analysis, high throughput, inheritability and good biocompatibility, the micro-fluidic analytical technology provides a new method and technical platform for screening active ingredients from natural products. This essay introduces multiple methods used for screening active ingredients from natural products and focuses on the micro-fluidic chip screening technology combined with cell culture and its characteristics, the composition of the platform of the micro-fluidic chip screening technology and its application in screening active ingredients from natural products.