Lactupicrin is a natural product discovered in chicory, exhibiting analgesic, sedative, antimalarial, and anti-atherosclerotic effects. It inhibits NF-κB activation and LDLR1 production, and demonstrates inhibitory activity against yeast alpha-glucosidase (IC50 = 14.71 µM).

acetylcholinesterase (AChE):150.3 μM

Lactupicrin (0.25-1 μM, 24 hours) attenuates cholesterol influx into low-grade inflammatory macrophages by targeting LOX-1 [2].
In inflammatory macrophages, Lactupicrin (0.625-40 μM, 24 hours) inhibits the activity of NF-κB within inflammatory macrophages [3].
In inflammatory macrophages, Lactupicrin (40 μM, 24 hours) suppresses the nuclear translocation process of p65 by downregulating cytoplasmic dynein-mediated transport of p65 [3].
Lactupicrin (50 μg/L, 48 hours) exhibits complete inhibitory effects on parasite growth [4].
Lactupicrin (10-1000 μM, 45 minutes) dose-dependently inhibits AChE activity [4].

Lactupicrin (15-30 mg/kg, intraperitoneal injection) exhibits analgesic activity and sedative properties in mice [1].
In ApoE-/- mice, Lactupicrin (1.2-120 mg/kg, oral administration, once daily for 12 weeks) exerts its anti-atherosclerotic effects by reducing LOX-1 in lipid rafts, thereby inhibiting macrophage foam cell formation [2].
In ApoE-/- mice, Lactupicrin (1.2-120 mg/kg, oral administration, once daily for 12 weeks) can suppress early atherosclerosis formation [3].
In ApoE-/- mice, Lactupicrin (1.2-120 mg/kg, oral administration, once daily for 12 weeks) dose-dependently reduces serum levels of IL-1β and TNF-α, but does not lower IL-6 levels [3].