Institute of Basic Research in Clinical Medicine, China Academy of Chinese Medical Sciences, Beijing 100700, China.
Law Sau Fai Institute for Advancing Translational Medicine in Bone and Joint Diseases, School of Chinese Medicine, Hong Kong Baptist University, Kowloon Tong, Hong Kong.
Int J Mol Sci. 2018 Jan 26;19(2):376. doi: 10.3390/ijms19020376.
Triptolide (TP), a major extract of the herb Hook F (TWHF), has been shown to exert potent pharmacological effects, especially an immunosuppressive effect in the treatment of rheumatoid arthritis (RA). However, its multiorgan toxicity prevents it from being widely used in clinical practice. Recently, several attempts are being performed to reduce TP toxicity. In this review, recent progress in the use of TP for RA, including its pharmacological effects and toxicity, is summarized. Meanwhile, strategies relying on chemical structural modifications, innovative delivery systems, and drug combinations to alleviate the disadvantages of TP are also reviewed. Furthermore, we also discuss the challenges and perspectives in their clinical translation.
雷公藤红素(TP)是草药 Hook F(TWHF)的主要提取物,已被证明具有很强的药理作用,特别是在治疗类风湿关节炎(RA)方面具有免疫抑制作用。然而,其多器官毒性使其无法在临床实践中广泛应用。最近,人们正在尝试多种方法来降低 TP 的毒性。本综述总结了近年来 TP 在 RA 中的应用进展,包括其药理作用和毒性。同时,还综述了通过化学结构修饰、创新给药系统和药物联合使用等策略来缓解 TP 缺点的方法。此外,我们还讨论了其临床转化面临的挑战和前景。