Embelin
(Synonyms: 恩贝酸; Embelic acid; Emberine; NSC 91874) 目录号 : GC13163
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。
Cas No.:550-24-3
Sample solution is provided at 25 µL, 10mM.
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]。
Cell experiment [1]: | |
Cell lines | AML-12 cells |
Preparation Method | AML-12 cells were cultivated for 24h with Embelin (6.25, 12.5µM) for 24h, and then exposure to EtOH (50mM) for 24h. The IL-1β and IL-18 protein levels released from AML-12 cells into culture medium were determined by an ELISA assay. |
Reaction Conditions | 6.25 or 12.5µM; 24h |
Applications | Embelin reversed ethanol-induced inflammatory response in AML-12 cells. |
Animal experiment [2]: | |
Animal models | C57BL/6 female mice |
Preparation Method | Acute liver injury was induced by a single intraperitoneal injection of 4% thioacetamide (TAA, 300µg/g). Embelin was administered via intragastric gavage at 50µg/g starting 2 days before TAA administration and continued throughout the study. The survival of TAA-treated mice was observed 4 days later, and the surviving mice were sacrificed. The acute liver injury protocol was repeated again 1, 2, and 3 days later, and the remaining mice were sacrificed at each time point. To estimate the pathophysiological values, the livers of the sacrificed mice were removed. |
Dosage form | 50µg/g; i.g. |
Applications | Embelin can protect mice from thioacetamide-induced acute liver injury. |
References: |
Cas No. | 550-24-3 | SDF | |
别名 | 恩贝酸; Embelic acid; Emberine; NSC 91874 | ||
化学名 | 2,5-dihydroxy-3-undecylcyclohexa-2,5-diene-1,4-dione | ||
Canonical SMILES | CCCCCCCCCCCC1=C(C(=O)C=C(C1=O)O)O | ||
分子式 | C17H26O4 | 分子量 | 294.39 |
溶解度 | ≥ 9.6mg/mL in DMSO, ≥ 4.23 mg/mL in EtOH with ultrasonic | 储存条件 | 4°C, protect from light |
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1 mg | 5 mg | 10 mg |
1 mM | 3.3969 mL | 16.9843 mL | 33.9685 mL |
5 mM | 0.6794 mL | 3.3969 mL | 6.7937 mL |
10 mM | 0.3397 mL | 1.6984 mL | 3.3969 mL |
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