Celastrol

Celastrol Structure
Celastrol structure
Common Name Celastrol
CAS Number 34157-83-0 Molecular Weight 450.610
Density 1.2±0.1 g/cm3 Boiling Point 645.7±55.0 °C at 760 mmHg
Molecular Formula C29H38O4 Melting Point 185-200ºC
MSDS Chinese USA Flash Point 358.3±28.0 °C
Symbol GHS06
GHS06
Signal Word Danger

Biological activity and safety of Tripterygium extract prepared by sodium carbonate extraction.

Molecules 17(9) , 11113-23, (2012)

The commercial preparation named “Tripterygium glycosides” prepared by column chromatography has been used for the treatment of inflammatory and autoimmune diseases with significant efficacy but concurrent toxicity. The aim of this study was to reduce the tox...

Inhibitory mechanisms of celastrol on human liver cytochrome P450 1A2, 2C19, 2D6, 2E1 and 3A4.

Xenobiotica 45 , 571-7, (2015)

1. The present study was conducted to examine the possibility of herb-drug interaction by celastrol, which is a main compound isolated from Tripterygium wilfordii Hook F. using human liver microsomes with cocktail methods. Focused on its inhibitory manner on ...

[Studies on sustained release solid dispersion of tripterine carried by HPMC-stearic acid].

Zhongguo Zhong Yao Za Zhi 37(20) , 3052-5, (2012)

To prepare the sustained release solid dispersion of tripterine, using HPMC-stearic acid with the intention of improving drug dissolution and controlling drug releases moderate, so that the drug performances lower toxicity.Tripterine sustained release solid d...

Interleukin 34: a new modulator of human and experimental inflammatory bowel disease.

Clin. Sci. (Lond.) 129 , 281-90, (2015)

IBD (inflammatory bowel disease), where CD (Crohn's disease) and UC (ulcerative colitis) represent the two main forms, are chronic inflammatory conditions of the intestine. Macrophages play a central role in IBD pathogenesis and are regulated by major differe...

Celastrol prevents cadmium-induced neuronal cell death via targeting JNK and PTEN-Akt/mTOR network.

J. Neurochem. 128(2) , 256-66, (2014)

Cadmium (Cd), a toxic environmental contaminant, induces neurodegenerative diseases. Celastrol, a plant-derived triterpene, has shown neuroprotective effects in various disease models. However, little is known regarding the effect of celastrol on Cd-induced n...

Hsp70 silencing with siRNA in nanocarriers enhances cancer cell death induced by the inhibitor of Hsp90.

Eur. J. Pharm. Sci. 50(1) , 149-58, (2013)

Inducers of heat shock protein 70 (Hsp70) commonly promote cancer cell viability whereas inhibitors of Hsp90 reduce it. The anticancer agent celastrol, interferes with signal transduction pathways involving these heat shock proteins. The objective of this in ...

Simultaneous NF-κB inhibition and E-cadherin upregulation mediate mutually synergistic anticancer activity of celastrol and SAHA in vitro and in vivo.

Int. J. Cancer 135(7) , 1721-32, (2014)

Suberoylanilide hydroxamic acid (SAHA) is a promising histone deacetylase (HDAC) inhibitor approved by the US Food and Drug Administration (FDA) and whose clinical application for solid tumours is partially limited by decreased susceptibility in cancer cells ...

The yeast Hsp70 Ssa1 is a sensor for activation of the heat shock response by thiol-reactive compounds.

Mol. Biol. Cell 23(17) , 3290-8, (2012)

The heat shock transcription factor HSF1 governs the response to heat shock, oxidative stresses, and xenobiotics through unknown mechanisms. We demonstrate that diverse thiol-reactive molecules potently activate budding yeast Hsf1. Hsf1 activation by thiol-re...

Strong inhibition of celastrol towards UDP-glucuronosyl transferase (UGT) 1A6 and 2B7 indicating potential risk of UGT-based herb-drug interaction.

Molecules 17(6) , 6832-9, (2012)

Celastrol, a quinone methide triterpene isolated from Tripterygium wilfordii Hook F., has various biochemical and pharmacological activities, and is now being developed as a promising anti-tumor agent. Inhibitory activity of compounds towards UDP-glucuronosyl...

Celastrol ameliorates HIV-1 Tat-induced inflammatory responses via NF-kappaB and AP-1 inhibition and heme oxygenase-1 induction in astrocytes.

Toxicol. Appl. Pharmacol. 280(1) , 42-52, (2014)

HIV-1 Tat causes extensive neuroinflammation that may progress to AIDS-related encephalitis and dementia. Celastrol possesses various biological activities such as anti-oxidant, anti-tumor, and anti-inflammatory activities. In this study, we investigated the ...