Emodin (Frangula emodin) 是一种蒽醌

Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction^[1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects^[2]. Emodin is a potent selective 11β-HSD1 inhibitor with the IC₅₀ of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice^[3].

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)

Emodin (10-400 μM) blocks the binding of S protein to ACE2 in a dose-dependent manner with the IC₅₀ value 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 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^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

270.24

C₁₅H₁₀O₅

518-82-1

大黄素

• Quinones
• Anthraquinones

• Phenols
• Polyphenols

• Plants
• Polygonaceae
• Rheum palmatum L.

Room temperature in continental US; may vary elsewhere.

Ethanol : 10.87 mg/mL (40.22 mM; Need ultrasonic)

DMSO : 5.41 mg/mL (20.02 mM; Need ultrasonic)

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储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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• 1.

  请依序添加每种溶剂： 0.5% MC 0.5% Tween-80

  Solubility: 10 mg/mL (37.00 mM); Suspended solution; Need ultrasonic

• 2.

  请依序添加每种溶剂： 0.5% CMC-Na/saline water

  Solubility: 3.33 mg/mL (12.32 mM); Suspened solution; Need ultrasonic

• [1]. Tin-Yun Ho, et al. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 interaction. Antiviral Res. 2007 May;74(2):92-101. [Content Brief]

  [2]. Stefania Sarno, et al. Toward the rational design of protein kinase casein kinase-2 inhibitors. Pharmacol Ther. Feb-Mar 2002;93(2-3):159-68. [Content Brief]

  [3]. Ying Feng, et al. Emodin, a natural product, selectively inhibits 11beta-hydroxysteroid dehydrogenase type 1 and ameliorates metabolic disorder in diet-induced obese mice. Br J Pharmacol. 2010 Sep;161(1):113-26. [Content Brief]