Department of Endocrinology, The First Affiliated Hospital of Henan University of Chinese Medicine, Zhengzhou, People's Republic of China.
Department of Respiratory Diseases, The First Affiliated Hospital of Henan University of Chinese Medicine, Zhengzhou, People's Republic of China.
Drug Des Devel Ther. 2024 Jul 25;18:3255-3266. doi: 10.2147/DDDT.S467929. eCollection 2024.
Fibrosis leads to organ failure and death, which is the final stage of many chronic diseases. Triptolide (TPL) is a terpenoid extracted from the traditional Chinese medicine (TwHF). Triptolide and its derivatives (Omtriptolide, Minnelide, (5R)-5-hydroxytriptolide) have been proven to have a variety of pharmacological effects. This study comprehensively reviewed the antifibrotic mechanism of TPL and its derivatives, and discussed the application of advanced nanoparticles (NPs) drug delivery system in the treatment of fibrotic diseases by TPL. The results show that TPL can inhibit immune inflammatory response, relieve oxidative stress and endoplasmic reticulum stress (ERS), regulate collagen deposition and inhibit myofibroblast production to play an anti-fibrosis effect and reduce organ injury. A low dose of TPL has no obvious toxicity. Under pathological conditions, a toxic dose of TPL has a protective effect on organs. The emergence of TPL derivatives (especially Minnelide) and NPs drug delivery systems promotes the anti-fibrosis effect of TPL and reduces its toxicity, which may be the main direction of anti-fibrosis research in the future.
纤维化导致器官衰竭和死亡，是许多慢性疾病的终末阶段。雷公藤红素（TPL）是从中药（雷公藤）中提取的一种萜类化合物。雷公藤红素及其衍生物（奥曲肽、米内莱特、（5R）-5-羟基雷公藤红素）已被证明具有多种药理作用。本研究全面综述了 TPL 及其衍生物的抗纤维化机制，并讨论了 TPL 通过先进的纳米颗粒（NPs）药物递送系统在治疗纤维化疾病中的应用。结果表明，TPL 可抑制免疫炎症反应，缓解氧化应激和内质网应激（ERS），调节胶原沉积并抑制肌成纤维细胞生成，发挥抗纤维化作用，减少器官损伤。低剂量 TPL 无明显毒性。在病理条件下，TPL 的毒性剂量对器官具有保护作用。TPL 衍生物（尤其是米内莱特）和 NPs 药物递送系统的出现促进了 TPL 的抗纤维化作用，降低了其毒性，这可能是未来抗纤维化研究的主要方向。
