Celastrol: Molecular targets of Thunder God Vine

作者：Salminen Antero^*; Lehtonen Marko; Paimela Tuomas; Kaarniranta Kai

来源：Biochemical and Biophysical Research Communications, 2010, 394(3): 439-442.

DOI：10.1016/j.bbrc.2010.03.050

• Celastrol
• IKK beta
• NF-kappa B
• Heat shock response
• Traditional medicine

Celastrol, a quinone methide triterpene, is a pharmacologically active compound present in Thunder God Vine root extracts used as a remedy of inflammatory and autoimmune diseases, e g. rheumatoid arthritis Celastrol is one of the most promising medicinal molecules isolated from the plant extracts of traditional medicines. Molecular studies have identified several molecular targets which are mostly centered on the inhibition of IKK-NF-kappa B signaling Celastrol (i) inhibits directly the IKK alpha and beta kinases, (II) inactivates the Cdc37 and p23 proteins which are co-chaperones of HSP90, (III) inhibits the function of proteasomes, and (IV) activates the HSF1 and subsequently triggers the heat shock response. It seems that the quinone methide structure present in celastrol can react with the thiol groups of cysteine residues, forming covalent protein adducts In laboratory experiments, celastrol has proved to be a potent inhibitor of inflammatory responses and cancer formation as well as alleviating diseases of proteostasis deficiency.

• 出版日期2010-4-9