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.