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Emodin

CAS No. : 518-82-1

MCE 站：Emodin

产品活性：Emodin (Frangula emodin) 是一种蒽醌衍生物，是一种抗 SARS-CoV 化合物。Emodin 阻断 SARS 冠状病毒刺突蛋白和血管紧张素转化酶 2 (ACE2) 的相互作用。Emodin 抑制酪蛋白激酶 2 (CK2)。 具有抗炎和抗癌作用。Emodin 还是一种有效的选择性 11β-HSD1 抑制剂，对人和小鼠 11β-HSD1 的 IC₅₀ 分别为 186 和 86 nM。Emodin 可改善饮食诱导的肥胖小鼠的代谢紊乱。

研究领域：Anti-infection  |  Cell Cycle/DNA Damage  |  Stem Cell/Wnt  |  Autophagy

作用靶点：SARS-CoV  |  Casein Kinase  |  Autophagy

In Vitro: Emodin (10-400 μM) blocks the binding of S protein to ACE2 in a dose-dependent manner with the IC₅₀ value of 200 μM.
Emodin (5-50 μM) inhibits the S protein-pseudotyped retrovirus infectivity in a dose-dependent manner. Emodin blocks the SARS-CoV S protein binding to Vero E6 cells.
Emodin inhibits casein kinase-2 (CK2) with IC₅₀s of 5.9, 30.0, and 7.1 μM for CK2α Wild-type, Ile174Ala mutant, and His160Ala mutant at ATP concentration is 50 μM, respectively. The IC₅₀s are 1.40 and 38.00 μM for CK2α Wild-type, and Val66Ala mutant at ATP concentration is 10 μM.
Emodin exhibits low inhibitory activity against mouse and human 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2), with an IC₅₀ higher than 1 mM, indicating that Emodin is more than 5000-fold selective for the human and mouse 11β-HSD1 enzymes over the type 2 isoenzyme.

In Vivo: Emodin (single oral administration of 100 or 200 mg/kg) inhibits 11β-HSD1 activity in normal C57BL/6J male mice.
Emodin (100 mg/kg; oral administration; b.i.d.) improves insulin sensitivity and lipid metabolism, and lowers blood glucose and hepatic PEPCK, and glucose-6-phosphatase mRNA in diet-induced obese (DIO) mice.

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