Triptolide: reflections on two decades of research and prospects for the future

Lu Tong; Qunfei Zhao; Emmanuel Datan; Guo-Qiang Lin; Il Minn; Martin G. Pomper; Biao Yu; Daniel Romo; Qing-Li He; Jun O. Liu

doi:10.1039/D0NP00054J

Triptolide: reflections on two decades of research and prospects for the future

Lu Tong,†^a Qunfei Zhao,†^a Emmanuel Datan,^b Guo-Qiang Lin,^ac Il Minn,^d Martin G. Pomper,^d Biao Yu,^e Daniel Romo,

^f Qing-Li He*^a and Jun O. Liu

*^b

Author affiliations

* Corresponding authors

^a The Research Center of Chiral Drugs, Innovation Research Institute of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai 201203, China
E-mail: qinglihe@shutcm.edu.cn

^b Department of Pharmacology, Johns Hopkins School of Medicine, 725 North Wolfe Street, Hunterian Building, Room 516, Baltimore, MD 21205, USA
E-mail: joliu@jhu.edu

^c CAS Key Laboratory of Synthetic Chemistry of Natural Substances, Center for Excellence in Molecular Synthesis, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032, China

^d Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins School of Medicine, Baltimore, MD 21205, USA

^e State Key Laboratory of Bio-organic and Natural Products Chemistry, Center for Excellence in Molecular Synthesis, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 200032, China

^f Department of Chemistry and Biochemistry, The CPRIT Synthesis and Drug Lead Discovery Laboratory, Baylor University, Waco, Texas 76710, USA

Abstract

Covering: 2000 to 2020

Triptolide is a bioactive diterpene triepoxide isolated from Tripterygium wilfordii Hook F, a traditional Chinese medicinal plant whose extracts have been used as anti-inflammatory and immunosuppressive remedies for centuries. Although triptolide and its analogs exhibit potent bioactivities against various cancers, and inflammatory and autoimmune diseases, none of them has been approved to be used in the clinic. This review highlights advances in material sourcing, molecular mechanisms, clinical progress and new drug design strategies for triptolide over the past two decades, along with some prospects for the future course of development of triptolide.

Graphical abstract: Triptolide: reflections on two decades of research and prospects for the future

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Triptolide: reflections on two decades of research and prospects for the future

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