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Open Access Research article

Role of berberine in anti-bacterial as a high-affinity LPS antagonist binding to TLR4/MD-2 receptor

Ming Chu1*, Ran Ding2, Zheng-yun Chu2, Ming-bo Zhang2, Xiao-yan Liu1, Shao-hua Xie1, Yan-jun Zhai2 and Yue-dan Wang1*

Author Affiliations

1 Department of Immunology, School of Basic Medical Sciences, Peking University, No.38, Xueyuan Road, Haidian District, Beijing 100191, China

2 Pharmacy Departments, Liao Ning University of Traditional Chinese Medicine, Liao Ning 116600, China

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BMC Complementary and Alternative Medicine 2014, 14:89  doi:10.1186/1472-6882-14-89

Published: 6 March 2014

Abstract

Background

Berberine is an isoquinoline alkaloid mainly extracted from Rhizoma Coptidis and has been shown to possess a potent inhibitory activity against bacterial. However, the role of berberine in anti-bacterial action has not been extensively studied.

Methods

The animal model was established to investigate the effects of berberine on bacterial and LPS infection. Docking analysis, Molecular dynamics simulations and Real-time RT-PCR analysis was adopted to investigate the molecular mechanism.

Results

Treatment with 40 mg/kg berberine significantly increased the survival rate of mice challenged with Salmonella typhimurium (LT2), but berberine show no effects in bacteriostasis. Further study indicated that treatment with 0.20 g/kg berberine markedly increased the survival rate of mice challenged with 2 EU/ml bacterial endotoxin (LPS) and postpone the death time of the dead mice. Moreover, pretreatment with 0.05 g/kg berberine significantly lower the increasing temperature of rabbits challenged with LPS. The studies of molecular mechanism demonstrated that Berberine was able to bind to the TLR4/MD-2 receptor, and presented higher affinity in comparison with LPS. Furthermore, berberine could significantly suppressed the increasing expression of NF-κB, IL-6, TNFα, and IFNβ in the RAW264.7 challenged with LPS.

Conclusion

Berberine can act as a LPS antagonist and block the LPS/TLR4 signaling from the sourse, resulting in the anti-bacterial action.