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Review
. 2018 Feb 14:9:104.
doi: 10.3389/fphar.2018.00104. eCollection 2018.

A Mechanistic Overview of Triptolide and Celastrol, Natural Products from Tripterygium wilfordii Hook F

Shao-Ru Chen  1 , Yan Dai  1 , Jing Zhao  1 , Ligen Lin  1 , Yitao Wang  1 , Ying Wang  1
Affiliations
Review

A Mechanistic Overview of Triptolide and Celastrol, Natural Products from Tripterygium wilfordii Hook F

Shao-Ru Chen et al. Front Pharmacol. .

Abstract

Triptolide and celastrol are predominantly active natural products isolated from the medicinal plant Tripterygium wilfordii Hook F. These compounds exhibit similar pharmacological activities, including anti-cancer, anti-inflammation, anti-obesity, and anti-diabetic activities. Triptolide and celastrol also provide neuroprotection and prevent cardiovascular and metabolic diseases. However, toxicity restricts the further development of triptolide and celastrol. In this review, we comprehensively review therapeutic targets and mechanisms of action, and translational study of triptolide and celastrol. We systemically discuss the structure-activity-relationship of triptolide, celastrol, and their derivatives. Furthermore, we propose the use of structural derivatives, targeted therapy, and combination treatment as possible solutions to reduce toxicity and increase therapeutic window of these potent natural products from T. wilfordii Hook F.

Keywords: Tripterygium wilfordii Hook F; celastrol; mechanisms of action; structure-activity-relationship; triptolide.

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Figures

FIGURE 1
FIGURE 1
Chemical structures of compounds isolated from Tripterygium wilfordii Hook F. Red color labeled moieties essential to maintain biological activities.
See this image and copyright information in PMC

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