Embelin is a non-peptidic, cell-permeable small inhibitor of the X-linked inhibitor of apoptosis protein (XIAP) with an IC₅₀ value of 4.1µM[1].
In vitro, Embelin (6.25 or 12.5µM; 24h) reversed ethanol-induced inflammatory response in AML-12 cells[2]. Embelin (20µM; 2h) protects against apoptosis and inflammation by regulating PI3K/Akt signaling in IL-1β-stimulated human nucleus pulposus cells[3].
In vivo, Embelin (50 or 100mg/kg; 10 days; i.g.) ameliorates alcoholic steatohepatitis (ASH) by modulating the ATF6-P2×7r/NLRP3 signaling pathway in mice with alcoholic liver disease (ALD)[2]. Embelin (50μg/g; i.g.) can protect mice from thioacetamide-induced acute liver injury[4].
References:
[1] Sheng Z, Ge S, Gao M, et al. Synthesis and Biological Activity of Embelin and its Derivatives: An Overview. Mini Rev Med Chem. 2020;20(5):396-407.
[2] Zhang JJ, Zhong JT, Wang WL, et al. Embelin improves alcoholic steatohepatitis in alcohol-associated liver disease via ATF6-mediated P2X7r-NLRP3 signaling pathway. Phytomedicine. 2025 May;140:156638.
[3] Bai X, Wang J, Ding S, et al. Embelin protects against apoptosis and inflammation by regulating PI3K/Akt signaling in IL-1β-stimulated human nucleus pulposus cells. Tissue Cell. 2023 Jun;82:102089.
[4] Wang H, Zhang H, Wang Y, et al. Embelin can protect mice from thioacetamide-induced acute liver injury. Biomed Pharmacother. 2019 Oct;118:109360.
Embelin是一种非肽类、可穿透细胞的小分子X连锁凋亡抑制蛋白（XIAP）抑制剂，其IC₅₀值为4.1µM[1]。
在体外实验中，Embelin（6.25或12.5µM; 24小时）可逆转乙醇诱导的AML-12细胞的炎症反应[2]。Embelin（20µM; 2小时）通过调节PI3K/Akt信号通路，保护白细胞介素-1β（IL-1β）刺激的人髓核细胞免受凋亡和炎症的侵害[3]。
在体内实验中，Embelin（50或100mg/kg; 10天; 灌胃）通过调节酒精性肝病（ALD）小鼠的ATF6-P2×7r/NLRP3信号通路，改善酒精性脂肪性肝炎（ASH）[2]。Embelin（50μg/g; 灌胃）可保护小鼠免受硫代乙酰胺诱导的急性肝损伤[4]。