Arglabin

Arglabin is a sesquiterpene γ-lactone originally isolated from A. glabella that has anticancer and anti-inflammatory activities.¹ It inhibits the growth of LS-180, SSC-4, HeLa, MCF-7, and HL-60 cancer cells (IC₅₀s = 20, 10, 20, 20, and 50 µM, respectively).² Arglabin reduces tumor growth in an SCC-4 mouse xenograft model when administered at a dose of 40 µg/g. It is a selective inhibitor of the NLRP3 inflammasome over the NLRP1, AIM2, and NLRC4 inflammasomes when used at a concentration of 50 nM.¹ Arglabin (50 nM) reduces increases in protein levels of NLRP3, caspase-1, IL-1β, and IL-18 induced by cholesterol crystals in LPS-primed mouse peritoneal macrophages. It decreases plasma levels of IL-1β, oxidized LDL autoantibodies, total cholesterol, and triglycerides, and reduces the size of atherosclerotic lesions in the aorta of mice fed a high-fat diet when administered at a dose of 2.5 ng/g.

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1. Abderrazak, A., Couchie, D., Mahmood, D.F.D., et al. Anti-inflammatory and antiatherogenic effects of the NLRP3 inflammasome inhibitor arglabin in ApoE2.K_i mice fed a high-fat diet. Circulation 131(12), 1061-1070 (2015).

2. He, W., Lai, R., Lin, Q., et al. Arglabin is a plant sesquiterpene lactone that exerts potent anticancer effects on human oral squamous cancer cells via mitochondrial apoptosis and downregulation of the mTOR/PI3K/Akt signaling pathway to inhibit tumor growth in vivo. J. BUON 23(6), 1679-1685 (2018).