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brazilein inhibits neuronal inflammation induced by cerebral ischemia and oxygen-glucose deprivation through targeting NOD2 expression

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Chinese Journal of Natural Medicines 2016年第5期14卷 354-362页

作者： YAN Xiao-Jin CHAI Yu-Shuang YUAN Zhi-Yi WANG Xin-Pei JIANG Jing-Fei LEI Fan XING Dong-Ming DU Li-Jun MOE Key Laboratory of Protein Sciences Laboratory of Molecular Pharmacology and Pharmaceutical Sciences School of Life Sciences and School of Medicine Tsinghua University

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 TNFa （tumor necrosis factor alpha） elicited by cerebral ischemia and reperfusion. This reduction could also be detected in normal mice and C 17.2 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.

关键词： brazilein Neuroinflammation NOD2

Reproductive toxicity of brazilein in ICR mice

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Chinese Journal of Natural Medicines 2016年第6期14卷 441-448页

作者： YUAN Zhi-Yi LEI Fan CHAI Yu-Shuang WU Hao ZHAO Shuang WANG Yu-Gang FENG Tian-Shi LI Hui-Ying LI Hui-Yu ZHAN Hong-Lei XING Dong-Ming DU Li-Jun MOE Key Laboratory of Protein Sciences Laboratory of Molecular Pharmacology and Pharmaceutical Sciences School of Life Sciences and School of Medicine Tsinghua University NGM Biopharmaceuticals Inc.

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.

关键词： brazilein General productive toxicity Mice

Activation of Growth-associated Protein by Intragastric brazilein in Motor Neuron of Spinal Cord Connected with Injured Sciatic Nerve in Mice

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Chemical Research in Chinese Universities 2011年第2期27卷 254-257页

作者： CAO Jian LI Li-sen LIU Biao LIU Hao-yu ZHANG Hui ZHAO Ming-ming YIN Wei-tian China-Japan Union Hospital of Jilin University Changchun 130033 P. R. China

The purpose of this study is to explore the expression of growth-associated protein（GAP-43） in spinal cord segments connected with injured sciatic nerve by the treatment with brazilein in mice. Unilateral sciatic nerve interruption and anastomosis were performed. Physiological saline（blank group）, high dose, middle dose and low dose of brazilein were administrated intragastrically to healthy adult BALB/c mice in separate groups. L4―6 spinal segments connected with the sciatic nerve were harvested. Real-time PCR（Polymerase chain reaction） and Western blot analysis were performed to detect the expression of GAP-43 in spinal segments. Histological staining on myelin and the electrophysiology were performed to examine the sciatic nerve recovery. GAP-43 was activated in spinal cord L4―6 connected with injured sciatic nerve. In the survival time of 12 h, 24 h, 3 d, 5 d, 7 d and 14 d, GAP-43 expression in the motor neurons of spinal cord of the high dose group and that in the middle dose group were significantly higher than those on the low dose and blank groups. Myelin in the high dose group and that in the middle dose group were more mature and the potential amplitude and MNCV（motor nerve conduction velocity） in the high and middle dose groups were obviously higher than those in the low dose group and blank group. brazilein facilitates the expression of GAP-43 in neurons in spinal cord L4―6 segments connected with injured sciatic nerve, which promotes nerve regeneration.

关键词： brazilein Growth-associated protein(GAP-43) Injury of sciatic nerve Regeneration

Antioxidant Activity In Vitro of Three Constituents from Caesalpinia sappan L

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Tsinghua Science and Technology 2008年第4期13卷 474-479页

作者：胡珺闫晓玲王伟吴昊花雷杜力军 Laboratory of Pharmaceutical Sciences Department of Biological Sciences and Biotechnology Tsinghua University Beijing 100084 China

Antioxidant activities of the 95% ethanol extract from Caesalpinia sappan heartwood （ECS）, protosappanin A, protosappanin B, and brazilein were studied in vitro. The inhibition of the formation of malondialdehyde （MDA） and the scavenging of superoxide anions, hydrogen peroxide, and hydroxyl radicals were assayed. The experimental results show that all four substances had antioxidant activity in vitro but their capabilities differed for the different indicators. ECS, protosappanin A, and protosappanin B show more inhibition of MDA and scavenging of hydrogen peroxide, while brazilein shows more scavenging of hydroxyl radicals. All the samples show little scavenging of superoxide anions.

关键词： antioxidant Caesalpinia sappan L protosappanin A protosappanin B brazilein