Emodin (Frangula emodin) 是一种蒽醌衍生物，是一种抗COVID-19化合物。Emodin 阻断 SARS 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。
| 生物活性 | Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoVcompound. Emodin blocks the SARS coronavirus spike protein andangiotensin-converting enzyme 2 (ACE2)interaction[1]. Emodin inhibitscasein kinase-2(CK2). Anti-inflammatory and anticancer effects[2]. Emodin is a potent selective11β-HSD1inhibitor with theIC50of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice[3]. |
| IC50& Target[1][2][3] | SARS-CoV | CK2α Wild-type 1.4 μM (IC50, at ATP concentration is 10 μM) | CK2α Wild-type 5.9 μM (IC50, at ATP concentration is 50 μM) | mouse 11β-HSD1 86 nM (IC50) | human 11β-HSD1 186 nM (IC50) |
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体外研究
(In Vitro) | Emodin (10-400 μM) blocks the binding of S protein to ACE2 in a dose-dependent manner with the IC50value of 200 μM[1].
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[1].
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[2].
Emodin exhibits low inhibitory activity against mouse and human 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2), with an IC50higher 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[3].
Cell Viability Assay[1] | Cell Line: | Vero E6 cells transfected with the plasmid encoding ACE2 | | Concentration: | 0, 5, 25, 50 μM | | Incubation Time: | 24 hours | | Result: | Vero cells treated with 50 μM remained 82.4±3.8% viability, the anti-SARS-CoV activity was not due to toxicity. |
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体内研究
(In Vivo) | Emodin (single oral administration of 100 or 200 mg/kg) inhibits 11β-HSD1 activity in normal C57BL/6J male mice[3].
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[3].
| Animal Model: | C57BL/6J male mice[3] | | Dosage: | 100 or 200 mg/kg | | Administration: | Acute administered p.o. ; Two hours later, the mice were killed by cervical dislocation, | | Result: | Significantly inhibited liver 11β-HSD1 enzymatic activity by 17.6 and 31.3% and mesenteric fat 11β-HSD1 enzymatic activity by 21.5 and 46.7% at 100 or 200 mg/kg, respectively. |
| Animal Model: | DIO mice (C57BL/6J male mice were fed a formulated research diet)[3] | | Dosage: | 100 mg/kg | | Administration: | Oral gavage; twice per day; for 35 days | | Result: | Reduced fasting glucose concentrations to 77.2% of the vehicle control mice after 7 days of treatment, and these remained significantly lower throughout the treatment period.
Exhibited a significant reduction in blood glucose levels at all time-points following oral glucose challenge after 24 days of treatment.
Evoked a significantly greater reduction in blood glucose values 40 and 90 min after insulin injection after 28 days of treatment.
The serum insulin level was also significantly reduced, to 66.2% of control mice, after 35 days of treatment.
Improved the lipid profiles. The serum triglyceride and total cholesterol levels were significantly reduced by 19.3 and 12.5% after 35 days of treatment, respectively.
Caused a 22.7% reduction of non-esterified free fatty acid (NEFA) level.
Lowered body weight and appetite from day 18 of the treatment; their body weights were reduced by 13.9% at the end of treatment.
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| 来源 | - Plants
- Polygonaceae
- Rheum palmatumL.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: Acetone : 10.87 mg/mL(40.22 mM;Need ultrasonic) Ethanol : 10.87 mg/mL(40.22 mM;Need ultrasonic) DMSO : 5.41 mg/mL(20.02 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.7004 mL | 18.5021 mL | 37.0041 mL | | 5 mM | 0.7401 mL | 3.7004 mL | 7.4008 mL | | 10 mM | 0.3700 mL | 1.8502 mL | 3.7004 mL |
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以下溶剂前显示的百
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