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.
Highlights
Triptolide and CelastrolThe chloroform/methanol extract of Tripterygium wilfordii Hook F (TWHF) attenuates inflammation in patients with Crohn’s disease by inducing the differentiation of Foxp3+ T regulatory (Treg) cells and suppressing the serum levels of pro-inflammation cytokines, such as interleukin-10 and transforming growth factor (TGF)-β (Li et al, 2014)
On the basis of the pharmacological activities of compounds isolated from THWF, especially triptolide and celastrol, we conclude that the systemic evaluation of the in vivo activities of these compounds is still needed
Structure modifications, and the mechanisms of action of these compounds are essential in the design of novel derivatives with reduced cytotoxicity, improved efficacy, and increased therapeutic index
Summary
The chloroform/methanol extract of TWHF attenuates inflammation in patients with Crohn’s disease by inducing the differentiation of Foxp3+ T regulatory (Treg) cells and suppressing the serum levels of pro-inflammation cytokines, such as interleukin-10 and TGF-β (Li et al, 2014). Several classes of bioactive substances have been isolated and characterized from TWHF, including sesquiterpenes, diterpenes (triptolide, tripdiolide, and triptonide), triterpenes (celastrol, pristimerin, and wilforlide A), lignans, glycosides, and alkaloids (Bao and Dai, 2011; Li et al, 2012b; Wang et al, 2013). Triptolide and celastrol are considered as the most active and promising components of TWHF. Their pharmacological activities and mechanisms of action have been extensively investigated in many disease models (Table 1)
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