CFTR chloride channel is the molecular drug target for the treatment of secretory diarrhea. Screening CFTR inhibitors is the most important and basic part of anti-diarrheal drug development. The natural products are diversified both in the structure and the biological activity. In the discovery of drugs and leading compounds, natural products play a key role and become the main source of drug development. Natural products from foods and herbal plants are usually safe for low or no toxicity and side-effect in clinic. CFTR inhibitors which source of foods and traditional Chinese medicines are important of study and treatment of CFTR related diseases, as well as providing a basis for the modern drug discovery in the natural product resources.