1. Membrane Transporter/Ion Channel Apoptosis Immunology/Inflammation
  2. Na+/K+ ATPase Apoptosis Interleukin Related NO Synthase
  3. Brazilein

Brazilein is a compound with anti-inflammatory and neuroprotective activities, with an IC50 of 500 μM against guinea pig Na+,K+-ATPase. Brazilein reduces iNOS mRNA expression, thereby inhibiting nitric oxide production in immune cells. Brazilein suppresses inflammatory responses by reducing the mRNA expression of TNF-α and IL-6, but has no effect on IL-1β expression. Brazilein reduces the cerebral infarction volume and improves the neurological function scores of rats with cerebral ischemia-reperfusion injury. Brazilein induces apoptosis of splenic lymphocytes in mice. Brazilein inhibits humoral immune responses in mice, and causes thymus and spleen atrophy as well as body weight loss in mice. Brazilein can be used in studies related to the nervous system, cardiovascular system and inflammatory diseases.

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Brazilein

Brazilein Chemical Structure

CAS No. : 600-76-0

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Based on 2 publication(s) in Google Scholar

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Description

Brazilein is a compound with anti-inflammatory and neuroprotective activities, with an IC50 of 500 μM against guinea pig Na+,K+-ATPase. Brazilein reduces iNOS mRNA expression, thereby inhibiting nitric oxide production in immune cells. Brazilein suppresses inflammatory responses by reducing the mRNA expression of TNF-α and IL-6, but has no effect on IL-1β expression. Brazilein reduces the cerebral infarction volume and improves the neurological function scores of rats with cerebral ischemia-reperfusion injury. Brazilein induces apoptosis of splenic lymphocytes in mice. Brazilein inhibits humoral immune responses in mice, and causes thymus and spleen atrophy as well as body weight loss in mice. Brazilein can be used in studies related to the nervous system, cardiovascular system and inflammatory diseases[1][2][3].

IC50 & Target[1]

IL-6

 

iNOS

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
34.08 μM
Compound: 2, CS-2
Cytotoxicity against human A549 cells after 3 days by MTT assay
Cytotoxicity against human A549 cells after 3 days by MTT assay
[PMID: 21800859]
A549 IC50
9.68 μg/mL
Compound: 1, Brazilein
Cytotoxicity against human A549 cells
Cytotoxicity against human A549 cells
[PMID: 20036537]
Ca9-22 IC50
30.39 μM
Compound: 2, CS-2
Cytotoxicity against human Ca9-22 cells after 3 days by MTT assay
Cytotoxicity against human Ca9-22 cells after 3 days by MTT assay
[PMID: 21800859]
Ca9-22 IC50
8.63 μg/mL
Compound: 1, Brazilein
Cytotoxicity against human Ca9-22 cells
Cytotoxicity against human Ca9-22 cells
[PMID: 20036537]
Hep 3B2 IC50
12.04 μM
Compound: 2, CS-2
Cytotoxicity against human Hep3B cells after 3 days by MTT assay
Cytotoxicity against human Hep3B cells after 3 days by MTT assay
[PMID: 21800859]
Hep 3B2 IC50
3.42 μg/mL
Compound: 1, Brazilein
Cytotoxicity against human Hep3B cells
Cytotoxicity against human Hep3B cells
[PMID: 20036537]
HepG2 IC50
11.09 μM
Compound: 2, CS-2
Cytotoxicity against human HepG2 cells after 3 days by MTT assay
Cytotoxicity against human HepG2 cells after 3 days by MTT assay
[PMID: 21800859]
HepG2 IC50
3.15 μg/mL
Compound: 1, Brazilein
Cytotoxicity against human HepG2 cells
Cytotoxicity against human HepG2 cells
[PMID: 20036537]
MCF7 IC50
13.94 μM
Compound: 2, CS-2
Cytotoxicity against human MCF7 cells after 3 days by MTT assay
Cytotoxicity against human MCF7 cells after 3 days by MTT assay
[PMID: 21800859]
MCF7 IC50
3.96 μg/mL
Compound: 1, Brazilein
Cytotoxicity against human MCF7 cells
Cytotoxicity against human MCF7 cells
[PMID: 20036537]
MDA-MB-231 IC50
2.36 μg/mL
Compound: 1, Brazilein
Cytotoxicity against human MDA-MB-231 cells
Cytotoxicity against human MDA-MB-231 cells
[PMID: 20036537]
MDA-MB-231 IC50
8.31 μM
Compound: 2, CS-2
Cytotoxicity against human MDA-MB-231 cells after 3 days by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 3 days by MTT assay
[PMID: 21800859]
Neutrophil IC50
14.2 μM
Compound: 1, Brazilein
Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/cytochalasin B-induced elastase release
Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/cytochalasin B-induced elastase release
[PMID: 20036537]
Neutrophil IC50
4 μM
Compound: 1, Brazilein
Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/cytochalasin B-induced superoxide anion generation
Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/cytochalasin B-induced superoxide anion generation
[PMID: 20036537]
In Vitro

Brazilein (3.5-28 μM; 16 h) inhibits LPS (HY-D1056)-induced NO production in BV2 and RAW 264.7 cells, with IC50 values of 18.77 μM and 264.18 μM[1].
Brazilein (10-50 μM; 4 h) dose-dependently inhibits LPS-induced mRNA expression of iNOS, TNF-α and IL-6 in BV2 mouse microglia, but exerts no effect on the mRNA expression of IL-1β[1].
Brazilein (1-10 μg/mL; 72 h) dose-dependently inhibits Concanavalin A (HY-P2149)-induced proliferation of mouse splenic T lymphocytes, with an inhibition rate of 56.18% at 10 μg/mL (72 h), 27.25% at 5 μg/mL (72 h), and 10.67% at 1 μg/mL (72 h)[3].
Brazilein (1-10 μg/mL; 72 h) dose-dependently inhibits LPS-induced proliferation of mouse splenic B lymphocytes in vitro, with an inhibition rate of 68.38% at 10 μg/mL (72 h), 54.41% at 5 μg/mL (72 h), 46.69% at 2.5 μg/mL (72 h), and 26.11% at 1 μg/mL (72 h)[3].
Brazilein (1-10 μg/mL; 72 h) induces apoptosis of mitogen-stimulated mouse splenic lymphocytes in a dose-dependent manner in vitro[3].

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

RT-PCR[1]

Cell Line: LPS-stimulated BV2 mouse microglial cells
Concentration: 10 μM, 20 μM, 30 μM, 40 μM, 50 μM
Incubation Time: 4 h (co-incubated with LPS)
Result: Inhibited LPS-induced iNOS, TNF-α and IL-6 mRNA expression in a dose-dependent manner.
Showed no significant effect on LPS-induced IL-1β mRNA expression at any tested concentration relative to LPS-only controls.
In Vivo

Brazilein (2.5-10 mg/kg; single intravenous injection) significantly reduces cerebral infarction volume, improves neurological deficits, and inhibits the expression of pro-inflammatory cytokines in rats with transient focal cerebral ischemia/reperfusion[1].
Brazilein (1-48 mg/kg; intravenous injection; continuous infusion at 0.4 mL/kg/min) dose-dependently alters the electrocardiographic parameters of anesthetized guinea pigs, but does not induce ventricular arrhythmias even at the lethal dose of 48 mg/kg, which causes death via dyspnea[2].
Brazilein (12.5-50 mg/kg/day; intraperitoneal injection; 7 days) exhibits dose-dependent in vivo immunosuppressive activity in healthy mice[3].

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

Animal Model: Wistar rats (male, 260-280 g, transient focal cerebral ischemia/reperfusion model)[1]
Dosage: 2.5 mg/kg; 5 mg/kg; 10 mg/kg
Administration: i.v.; single dose at reperfusion onset
Result: Reduced brain infarct volume.
Improved neurological scores.
Significantly decreased ischemia-induced TNF-α and IL-6 mRNA expression in ipsilateral cerebral cortex (5 mg/kg), with no significant effect on IL-1β mRNA expression.
Maintained physiological variables (rectal temperature, mean arterial blood pressure, blood gases, pH) within normal limits, with no significant difference from vehicle controls.
Animal Model: CD-1 (ICR) (male, adult, 25-30 g)[3]
Dosage: 12.5-50 mg/kg/day
Administration: i.p.; daily; 7 consecutive days
Result: Decreased thymus weight/body weight ratio.
Decreased spleen weight/body weight ratio.
Reduced splenic PFC count.
Caused significant atrophy and weight loss of thymus and spleen at 25 and 50 mg/kg/day relative to untreated controls.
Significantly reduced splenic PFC counts at 25 and 50 mg/kg/day relative to untreated controls.
Molecular Weight

284.26

Formula

C16H12O5

CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

O=C1C=C2C(C=C1O)=C3C4=C(OCC3(C2)O)C=C(O)C=C4

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMF : 11 mg/mL (38.70 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5179 mL 17.5895 mL 35.1791 mL
5 mM 0.7036 mL 3.5179 mL 7.0358 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.9%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMF 1 mM 3.5179 mL 17.5895 mL 35.1791 mL 87.9477 mL
5 mM 0.7036 mL 3.5179 mL 7.0358 mL 17.5895 mL
10 mM 0.3518 mL 1.7590 mL 3.5179 mL 8.7948 mL
15 mM 0.2345 mL 1.1726 mL 2.3453 mL 5.8632 mL
20 mM 0.1759 mL 0.8795 mL 1.7590 mL 4.3974 mL
25 mM 0.1407 mL 0.7036 mL 1.4072 mL 3.5179 mL
30 mM 0.1173 mL 0.5863 mL 1.1726 mL 2.9316 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Brazilein
Cat. No.:
HY-N10424
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