【摘要】 雷公藤(Tripterygium wilfordii Hook. f.)作为我国传统中草药，因其提取物具有抗炎、免疫抑制和抗肿瘤等活性而受到广泛关注。然而，雷公藤具有“效-毒同源”特性，限制了其临床应用。研究显示，雷公藤活性成分的多组分协同机制，特别是生物碱和三萜类化合物可通过协同调节NF-κB和JAK/STAT等信号通路发挥药理作用。雷公藤的相关毒性机制分析也已取得突破性进展。通过结构修饰和新型递送系统等科学手段，在保持雷公藤药理活性的同时，可显著降低其毒性。基因编辑和合成生物学等生物技术方法也为实现代谢源的解毒提供了新的方向。对雷公藤提取物的化学成分、药理作用、毒理学机制和衰减策略等方面的研究进展进行梳理，系统综述其创新药物开发策略，以期为研发高效低毒的雷公藤类药物提供理论支撑。更多还原

【Abstract】 As a traditional Chinese medicine, extracts of Tripterygium wilfordii Hook. f. have garnered significant attention for their anti-inflammatory, immunosuppressive, and antitumor activities. However, its undeniable “effect-toxicity homology” characteristic limits clinical application. Recent studies have revealed the multi-component synergistic mechanism of Tripterygium wilfordii’s active constituents, particularly how alkaloids and triterpenoids exert pharmacological effects by synergistically inhibiting signaling pathways such as NF-κB and JAK/STAT. Concurrently, breakthroughs have been achieved in elucidating its toxic mechanisms. Building upon these mechanisms, researchers have employed scientific approaches such as structural modification and novel delivery systems to significantly reduce toxicity while preserving pharmacological activity. Furthermore, biotechnological methods including gene editing and synthetic biology offer novel avenues for toxicity reduction at its metabolic source. Based on recent studies of the chemical composition, pharmacological effects, toxicological mechanisms, and detoxification strategies of Tripterygium wilfordii extracts, this review systematically reviews innovative drug development strategies for this herb, aiming to provide a theoretical basis for developing Tripterygium drugs with higher efficacy and lower toxicity.更多还原