Reproductive toxicity of brazilein in ICR mice / 中国天然药物

Brazilein is an active small molecular compound extracted from Caesalpinia sappan L. with favorable pharmacological properties on immune system, cardiovascular system, and nervous system. C. sappan has been used as a traditional medicine in China for hundreds of years for various diseases. However, the general reproductive toxicity of brazilein is still unknown. The purpose of the present study was to thoroughly evaluate the general reproductive toxicity of brazilein in ICR mice to support the future drug development and modernization of this potent traditional Chinese medicine. The results showed that, although no apparent toxicity on the reproducibility of the male was observed, brazilein might cause considerable risks to the fetuses and females as indicated by the ratios of dead fetuses and reabsorptions. In conclusion, our results from the present study provided some useful insights about the safety profile of brazilein, suggesting that brazilein should be used with caution in pregnant women.

Brazilein inhibits neuronal inflammation induced by cerebral ischemia and oxygen-glucose deprivation through targeting NOD2 expression / 中国天然药物

Brazilein is reported to have immunosuppressive effect on cardiovascular and cerebral-vascular diseases. The essential roles of innate immunity in cerebral ischemia are increasingly identified, but no studies concerning the influence of brazilein on the innate immunity receptors have been reported. The present study was designed to investigate the regulation of NOD2 (Nucleotide-binding oligomerization domain-containing protein 2) by brazilein for its protection of neuron in cerebral ischemia in vivo and oxygen-glucose deprivation in vitro. The results showed that brazilein could reverse the elevated expression of NOD2 and TNFα (tumor necrosis factor alpha) elicited by cerebral ischemia and reperfusion. This reduction could also be detected in normal mice and C17.2 cells, indicating that this suppressive effect of brazilein was correlated with NOD2. The results from GFP reporter plasmid assay suggested brazilein inhibited NOD2 gene transcription. In conclusion, brazilein could attenuate NOD2 and TNFα expression in cerebral ischemia and NOD2 may be one possible target of brazilein for its immune suppressive effect in neuro-inflammation.

Brazilein induced cells apoptosis in human lung cancer A549 cells and its effects on endoplasmic reticulum stress / 重庆医学

Objective To study the apoptotic effect of brazilein on human lung cancer A549 cells and endoplasmic reticulum stress .Methods The cytotoxic activity was tested by MTT assay in A549 cells .The flow cytometry was used to detect apoptosis . Western blotting was performed to detect GRP78 and cyto c protein expression .Results The IC50 values of brazilein against A549 cells was (5 .36 ± 0 .62)μmol/L .After treatment with 0 ,5 ,10 and 20 μmol/L brazilein for 48 h ,the percent of apoptosis was (1 .15 ± 0 .32)% ,(19 .61 ± 4 .52)% ,(30 .18 ± 6 .35)% and (39 .48 ± 7 .44)% respectively .There was significant difference among the different treatment (P< 0 .05) .Compared with control group ,the protein expression of GRP78 and cytosolic cyto c was in‐creased after 5 ,10 and 20 μmol/L brazilein treated for 48 h .Conclusion Brazilein induced apoptosis in human lung cancer A549 cells though endoplasmic reticulum stress pathway .

Effect of Brazilein on Relaxation of Vascular Smooth Muscle of Rat / 世界科学技术-中医药现代化

Brazilein is one of the active ingredients of a Chinese medicine Caesalpinia sappan L. This study was aimed to test the vasodilator effect of brazilein on vascular smooth muscle cells in vitro from the perspective of molecular biology. The results showed that brazilein mainly acted through the influence of potassium ion channels, reducing membrane depolarization in order to affect the vessel relaxation. This effect can be influenced by blocking 5-HT receptor, and, simultaneously, correlating with the regulation of intracellular calcium ion concentration, affecting calmodulin and downregulating MLCP. In addition, the alterations of cAMP, PKA and PGI2 were involved in the pharmacological process of brazilein.

Study on the plasma binding rate of brazilein / 中国药学杂志

OBJECTIVE: To establish an in vitro equilibrium dialysis method for studying the plasma binding rate of brazilein. METHODS: Equilibrium dialysis was used to determine the binding rates of brazilein to bovine serum albumin and rat plasma, and the compound concentration was determined by HPLC. All the biological samples were handled with acetic ether-extraction. RESULTS: The bovine serum albumin binding rates of brazilein at low, medium and high concentrations ranged from 38.5% to 50.8%, and the rat plasma binding rate of brazilein ranged from 86.2% to 97.3%. CONCLUSION: Brazilein has high binding capacity to plasma, and the phospholipid components may have major contribution to the binding between brazilein and plasma. Copyright 2012 by the Chinese Pharmaceutical Association.