Minmin Jiang,1,* Yongxia Xie,2,* Ping Wang,1 Mengyu Du,3 Ying Wang,4 Shuxun Yan1 

1Department of Endocrinology, The First Affiliated Hospital of Henan University of Chinese Medicine, Zhengzhou, People’s Republic of China; 2Department of Respiratory Diseases, The First Affiliated Hospital of Henan University of Chinese Medicine, Zhengzhou, People’s Republic of China; 3The First Clinical Medical College, Henan University of Chinese Medicine, Zhengzhou, People’s Republic of China; 4Department of International Medicine, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, People’s Republic of China

*These authors contributed equally to this work

Correspondence: Shuxun Yan; Ying Wang, Email ysx982001@163.com; wangying56994@126.com

Abstract: 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 Tripterygium wilfordii Hook. F (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.

Keywords: triptolide, derivatives, anti-fibrosis, nanoparticles