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[Biological and chemical synthesis of high-value active ingredients in traditional Chinese medicine]. Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica Traditional Chinese medicine(TCM) contains many high-value active ingredients, such as artemisinin, paclitaxel, vinblastine, and vincristine. However, these ingredients are present in low concentrations in the original plants, and their complex structures make extraction and separation challenging. To protect the limited resources of TCM, researchers have employed total chemical synthesis strategies to prepare structurally complex high-value active ingredients in TCM. However, harsh reaction conditions, lengthy routes, and low yields pose challenges to total chemical synthesis. With the development of synthetic biology, many high-value active ingredients can now be prepared through bio-cell engineering, complementing total chemical synthesis and offering new strategies for the preparation of high-value active ingredients in TCM. This article briefly reviewed the research progress in the biological and chemical synthesis of representative high-value active ingredients in TCM, including β-elemene, artemisinin, tanshinone, vincristine, and homoharringtonine. This article proposed a research paradigm that combined biological and chemical synthesis, including chemical enzyme-mediated structural modification of high-value active ingredients in TCM, semi-synthetic production of high-value active ingredients in TCM using biological synthesis, and biomimetic synthesis to facilitate the biological synthesis pathway of high-value active ingredients in TCM. It provided an important reference for the synthesis of high-value active ingredients in TCM. 10.19540/j.cnki.cjcmm.20240517.102