Liu Zhonghao, Li Dan, Yang Xiongwen, Chen Xisha, Fu Chengxiao
The First Affiliated Hospital, Department of Pharmacy, Hengyang Medical School, University of South China, Hengyang, 421001, Hunan, China.
School of Pharmaceutical Science, Hengyang Medical School, University of South China, Hengyang, 421001, Hunan, China.
Chin Med. 2025 Jul 16;20(1):114. doi: 10.1186/s13020-025-01170-6.
Tripterygium wilfordii Hook F (TWHF) is a traditional Chinese medicine with multifaceted pharmacological properties, has faced clinical application challenges due to its dose-limiting organ toxicity. Through a systematic analysis of current literature, this review deciphers the dual regulatory role of mitochondrial function in mediating both therapeutic efficacy and adverse effects of TWHF-derived active compounds. We elucidate that processes such as mitochondrial biogenesis, mitochondrial fusion and fission, mitophagy and mitochondrial apoptosis pathways influence the therapeutic efficacy and adverse effects of TWHF active ingredients. In addition, we review innovative dosage forms and derivatives of TWHF that exploit mitochondrial targeting to enhance their pharmacological efficacy. This article offers a concise overview pharmacological and toxicological effects of the principal active components of TWHF, in particular triptolide and celastrol, with a particular emphasis on elucidating the critical role of mitochondria in these processes. Further high-quality basic studies are essential to strengthen the link between mitochondrial function and the active compounds of TWHF, offering more diverse options for their clinical development.
雷公藤（Tripterygium wilfordii Hook F，TWHF）是一种具有多种药理特性的传统中药，因其剂量限制性器官毒性而面临临床应用挑战。通过对当前文献的系统分析，本综述解读了线粒体功能在介导TWHF衍生活性化合物的治疗效果和不良反应方面的双重调节作用。我们阐明，线粒体生物发生、线粒体融合与裂变、线粒体自噬和线粒体凋亡途径等过程会影响TWHF活性成分的治疗效果和不良反应。此外，我们还综述了TWHF的创新剂型和衍生物，这些剂型和衍生物利用线粒体靶向作用来增强其药理功效。本文简要概述了TWHF主要活性成分的药理和毒理作用，特别是雷公藤内酯醇和雷公藤红素，并特别强调阐明线粒体在这些过程中的关键作用。进一步开展高质量的基础研究对于加强线粒体功能与TWHF活性化合物之间的联系至关重要，可为其临床开发提供更多样化的选择。
