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This chapter explores the basics of High Throughput Screening (HTS) and its crucial role in functional foods and artificial intelligence (AI). HTS acts as a catalyst for identifying bioactive compounds with various applications, using systematic and automated approaches for swift evaluation. The focus is on molecular and cellular-level assays within HTS, highlighting their importance in uncovering bioactive components in functional foods. Automated instruments, such as liquid handlers, incubators, plate readers, and robotic arms, facilitate the seamless execution of HTS processes. Adapting HTS to assess food-sourced compounds poses challenges due to their complex chemical structures. Addressing these complexities is essential, particularly regarding pan-assay interference compounds (PAINS), exemplified by compounds like resveratrol and curcumin. This chapter also explores HTS applications in screening specific inhibitors for anti-inflammatory, antioxidant, alpha-amylase and alpha-glucosidase inhibition, and pancreatic lipase inhibition activities, demonstrating HTS as an indispensable tool in functional food research. Additionally, a case study on anti-aging studies using a yeast model showcases the versatility and efficiency of HTS in assessing chronological lifespan.

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