Lupeol

Lupeol is a naturally occurring pentacyclic triterpenoid found in many fruits and vegetables, including white cabbage, green pepper, strawberry, olive, mangoes, and grapes[3][5][6]. It has been investigated primarily as an anti-inflammatory agent and for the treatment of acne[1][2]. Lupeol exhibits a broad range of pharmacological activities such as anti-inflammatory, antioxidant, antitumor/anticancer (including chemopreventive), antimicrobial, antiprotozoal, immunomodulatory, anti-angiogenic effects and cholesterol-lowering properties[3][4][5][6]. Mechanistically, lupeol acts as a multi-target agent. Its anti-inflammatory effects are mediated by modulation of key molecular pathways including nuclear factor kappa B (NFκB), cFLIP, Fas receptor signaling pathway (apoptosis), phosphatidylinositol-3-kinase/Akt pathway (PI3K/Akt), Wnt/β-catenin signaling pathway; it also reduces pro-inflammatory cytokines such as IL-4 from T-helper type 2 cells and inhibits production of prostaglandin E2 (PGE2) in macrophages[3][5][7][8]. In cancer models it induces apoptosis via mitochondrial-mediated pathways involving increased reactive oxygen species (ROS) levels and altered Bax/Bcl-2 ratio leading to caspase activation[4]. Lupeol has also shown activity against dipeptidyl peptidase-4 at high concentrations. Additional reported actions include inhibition of cell migration/invasion through suppression of RhoA–ROCK1 signaling in colorectal cancer cells[6], neuroprotection via p38 MAPK modulation[7], wound healing enhancement by docking with GSK3β protein[3], contraceptive effect through inhibition of sperm calcium channel CatSper[5], downregulation of TNF-alpha and VEGFR-2 for its anti-cancer/antiangiogenic effects [5], cytoprotective action against free-radical-induced damage [6] and reduction in hypercholesterolemia [4]. Lupeol is considered investigational; it is not approved for any indication but continues to be studied preclinically for inflammation-related disorders and various cancers.

Other names

lupeol