Emodin(Synonyms: 大黄素; Frangula emodin)

天然产物醌类Quinones

Emodin (Synonyms: 大黄素; Frangula emodin) 纯度: 99.39%

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。

Emodin(Synonyms: 大黄素; Frangula emodin)

Emodin Chemical Structure

CAS No. : 518-82-1

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生物活性

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].

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)

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 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

270.24

Formula

C15H10O5

CAS 号

518-82-1

中文名称

大黄素

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
溶解性数据
In Vitro: 

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

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

Ethanol : < 1 mg/mL (ultrasonic) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 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

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [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.

    [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.

    [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.