中草药作为我国传统医药的重要组成部分，蕴含丰富的生物活性成分，是新药研发和疾病治疗的宝贵资源。但因其成分多样、活性复杂，使传统筛选鉴定方法面临效率低、通量小及难以识别微量活性成分等局限性。高通量筛选技术（high-throughput screening，HTS）凭借高效性、自动化、大规模处理能力和成本效益等优势，成为快速鉴定潜在活性成分的有效手段，近年来已成为推动中药现代化研究的重要技术支撑。通过系统分析国内外最新研究文献，从分子、细胞及动物3个维度全面阐述高通量筛选技术在中草药活性成分研究中的应用进展。此外，还评估了该技术在中药领域的应用价值与现存挑战，并对未来跨学科融合和技术革新的发展趋势进行了展望，以期为中药活性成分的筛选研究提供理论依据和方法学参考。

Chinese herbal medicine, as an important component of traditional Chinese medicine, contains abundant bioactive compounds and serves as a valuable resource for new drug development and disease treatment. However, due to the diversity and complexity of its components, traditional screening and identification methods suffer from limitations such as low efficiency, limited small throughput, and difficulty in detecting trace active constituents. High-throughput screening (HTS) technology combines high efficiency, automation, large-scale processing capacity, and cost-effectiveness, making it a powerful tool for rapidly identifying potential bioactive compounds. In recent years, it has become an important technological driver in promoting the modernization of traditional Chinese medicine research. This review systematically analyzes recent domestic and international literature to comprehensively elaborate on the application of HTS in the research of bioactive components from Chinese herbal medicine across molecular, cellular, and in vivo dimensions. Furthermore, it assesses the application value and existing challenges of this technology in the field of traditional Chinese medicine, and offers perspectives on future development trends involving interdisciplinary integration and technological innovation. This aims to provide a theoretical foundation and methodological reference for screening bioactive components in traditional Chinese medicine.

R286.2

“十四五”重点研发计划专项(2022YFD130040311);北京市农林科学院创新能力建设专项(KJCX20251005,KJCX20240339);北京市农林科学院国际科技合作平台建设项目(GHPT2025-03)