BACKGROUND: Chinese herbal medicine (CHM) is a fundamental component of traditional Chinese medical practice, offering a rich source of natural remedies with significant therapeutic potential. However, the scarcity of active ingredients and complex extraction procedures present substantial challenges to their widespread clinical application. This review aims to address this gap by exploring the potential of modern biotechnological advancements in enhancing the biosynthesis of these valuable compounds. METHODOLOGY: The study takes a comprehensive approach, delving into the chemical composition of CHM's active ingredients and elucidating their biosynthetic pathways and molecular regulatory mechanisms. Additionally, it surveys recent progress in extraction methodologies and evaluates engineering strategies aimed at synthetic production. This multifaceted analysis forms the foundation for examining the role of synthetic biology in augmenting CHM's active ingredient synthesis. RESULTS: Our examination provides insights into the intricate biosynthetic pathways governing the formation of CHM's active ingredients, as well as the complex molecular regulatory networks that underlie these processes. Furthermore, the review highlights advancements in extraction techniques, demonstrating their ability to streamline and enhance the isolation of these compounds. Engineering approaches for synthetic production, including metabolic engineering and synthetic biology tools, are assessed for their potential to overcome natural limitations and scale up production. CONCLUSIONS: By integrating insights from biosynthesis, molecular regulation, extraction methodologies, and synthetic biology, this review establishes a robust theoretical framework for enhancing the production of CHM's active ingredients. The proposed strategies and practical guidance aim to facilitate their broader utilization in modern medicine while promoting sustainability and accessibility within this invaluable medicinal heritage.