Common name: Celastrol
Synonyms: Tripterin, Tripterine
CAS NO.: 34157-83-0
Molecular Formula: C29H38O4
Molecular Weight: 450.6
Specification: 80%, 98%( Red Powder)
Test method: HPLC
Product Main Quality Items：
Contents(Calculated on dry basis by HPLC)
Packing: 50g/bag, 100g/bag, 1kg/bag
Storage: Store in cool and dry place and keep away from strong direct light and heat
Shelf Life: Two years when properly stored
Applications and Health Benefits:
What is Celastrol?
Celastrol (tripterine) is a chemical compound isolated from the root extracts of Celastrus regelii and Tripterygium wilfordii (Thunder god vine) . Celastrol is a pentacyclic triterpenoid and belongs to the family of quinone methides.
Health Benefits of Celastrol:
Celastrol is known to possess anti-inflammatory and antioxidant, anti-tumors activities and has been shown to have various pharmacological properties
1. Anti-Tumour/Anti-Cancer Effects of Celastrol
Celastrol is a triterpene with promising anticancer activity in several cancer models, including prostate cancer, pancreatic cancer, leukemia and melanoma.19–23 A recent study using a rat mammary carcinosarcoma model (W256 cells) reported that Celastrol not only suppressed tumor cell growth but also inhibited cell migration in vitro; in vivo, Celastrol suppressed trabecular bone loss and reduced osteolytic lesions in tumor-bearing rats.24 The additional ability of Celastrol to inhibit bone metastasis,24 as opposed to a potential pro-metastatic effect of 17-AAG,17 suggests a therapeutic advantage for Celastrol over 17-AAG as an HSP90 inhibitor.
2. Anti-inflammation Activities of Celastrol Independent of HSP90
Treatment with celastrol reduces inflammation in several disease models independent of HSP90. Celastrol significantly suppresses inflammation by reducing the secretion of IL-1β and IL-18, and inactivating the NLRP3 inflammasomes and caspase-1 in LPS/ATP-primed macrophage cells (Xin et al., 2017; Yu X. et al., 2017). Celastrol ameliorates colitis in IL-10-deficient mice by reducing colon myeloperoxidase concentration and inhibiting colonic pro-inflammatory cytokines via PI3K/Akt/mTOR signaling pathway (Zhao J. et al., 2015). It also ameliorates dextran sulfate sodium-induced colitis in caspase-1-/- mice by inhibiting the activation of NLRP3 inflammasomes and the subsequent secretion of IL-1β (Yu X. et al., 2017). Celastrol potentiates mitochondrial damage and inflammation in palmitate-induced insulin resistance in C3A hepatocytes (Abu Bakar et al., 2017). Treatment with celastrol also inhibits acute liver inflammation through the Nur77-dependent pathway and activation of autophagy in LPS and d-galactosamine-induced inflammation in mice (Greenhill, 2015). Although it inhibits the differentiation of Th17 cells, celastrol enhances the production of Treg cells by restricting the activation of STAT3 and its downstream target genes. In adjuvant arthritis rats, these processes suppress joint inflammation (Astry et al., 2015).
3. Preventing neuronal degeneration in Alzheimer's disease (AD).
In the brains of patients with Alzheimer's disease (AD) signs of neuronal degeneration are accompanied by markers of microglial activation, inflammation, and oxidant damage. The presence of nitrotyrosine in the cell bodies of neurons in AD suggests that peroxynitrite contributes to the pathogenesis of the disease. A drug with antioxidant and anti-inflammatory activity may prevent neuronal degeneration in AD. Celastrol, a plant-derived triterpene, has these effects. In low nanomolar concentrations celastrol was found to suppress the production by human monocytes and macrophages of the pro-inflammatory cytokines TNF-alpha and IL-1beta. Celastrol also decreased the induced expression of class II MHC molecules by microglia. In macrophage lineage cells and endothelial cells celastrol decreased induced but not constitutive NO production. Celastrol suppressed adjuvant arthritis in the rat, demonstrating in vivo anti-inflammatory activity. Low doses of celastrol administered to rats significantly improved their performance in memory, learning and psychomotor activity tests. The potent antioxidant and anti-inflammatory activities of celastrol, and its effects on cognitive functions, suggest that the drug may be useful to treat neurodegenerative diseases accompanied by inflammation, such as AD.
celastrol was identified from a panel of 1040 existing drugs as a neuroprotective agent through a collaborative drug screen that targeted the identification of small molecules for the treatment of neurodegenerative diseases. In contrast to Hsp90 N- and C-terminal inhibitors, Sun and coworkers demonstrated that celastrol disrupts the interaction between Hsp90 and the cochaperone, Cdc 37. The celastrol binding site appears to be located in the N-terminal region of Hsp90 and does not prevent ATP from binding.
Celastrol increases the brain’s sensitivity to leptin, the hormone that signals we’ve had enough to eat, but until now, no one knew how this was activated.
Celastrol curbed food intake in obese mice by almost 80%, producing up to a 45% weight loss. Celastrol increases the brain’s sensitivity to leptin, the hormone that signals we’ve had enough to eat, and now published in Nature Medicine, a study led by Umut Ozcan at Boston Children’s Hospital, USA, the mystery of how it curbs hunger and obesity may finally be solved.