pristimerin

Pristimerin is a naturally occurring quinone methide triterpenoid isolated from plants of the Celastraceae and Hippocrateaceae families. It has been extensively researched for its broad-spectrum anti-cancer properties and other pharmacological effects including anti-inflammatory, antioxidant, anti-bacterial, anti-malarial and insecticidal activities[1][2][5]. Pristimerin exerts potent antiproliferative effects on a wide range of cancer cell lines by inducing apoptosis (caspase-dependent mitochondrial pathway), autophagy and G0/G1 cell cycle arrest. Its mechanisms involve inhibition of nuclear factor kappa B (NF-kB) signaling via IKKα/IKKβ inhibition; suppression of Akt/protein kinase B; downregulation of cyclins D1/E and CDKs 2/4/6; upregulation of p53/p21/p27; inhibition of Wnt/β-catenin signaling through LRP6 targeting; proteasome inhibition (chymotrypsin-like activity); monoacylglycerol lipase inhibition; modulation of PI3K/Akt/mTOR pathway; suppression of MAPK signaling cascade; interference with sonic hedgehog/Gli1 pathway; downregulation of IGF‑1R signaling[2][3][4][5][8]. Pristimerin also demonstrates in vivo efficacy in animal models for cancer as well as autoimmune arthritis[4].

Other names

celastrol methyl ester(9.beta.,13.alpha.,14.beta.,20.alpha.)-3-hydroxy-9,13-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid 3-hydroxy-9 13-dimethyl-2-oxo-methyl ester (9.beta.,13.alpha.,14.beta.,20.alpha.)