Antioxidant and anti-inflammatory agent. Potently inhibits lipid peroxidation in mitochondria and inhibits TNF-α-induced NFκB activation. Also shown to inhibit topoisomerase II activity in vitro (IC₅₀ = 7.41 μM)

Sassa et al (1990) The triterpene celastrol as a very potent inhibitor of lipid peroxidation in mitochondria. Biochem.Biophys.Res.Comms. 172 890. Nagase et al (2003) Apoptosis induction in HL-60 cells and inhibition of topoisomerase II by triterpene celastrol. Biosci. Biotechnol.Biochem. 67 1883. Sethi et al (2007) Celastrol, a novel triterpene, potentiates TNF-induced apoptosis and suppresses invasion of tumor cells by inhibiting NF-kB-regulated gene products and TAK1-mediated NF-kB activation. Blood 109 2727