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Int. J. Mol. Sci. 2013, 14(1), 1802-1821; doi:10.3390/ijms14011802
Article

The Combination of Catechin and Epicatechin Gallate from Fructus Crataegi Potentiates β-Lactam Antibiotics Against Methicillin-Resistant Staphylococcus aureus (MRSA) in Vitro and in Vivo

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Received: 8 October 2012; in revised form: 29 November 2012 / Accepted: 8 January 2013 / Published: 16 January 2013
(This article belongs to the Special Issue Plant-Derived Pharmaceuticals by Molecular Farming 2012)
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Abstract: Fructus crataegi (hawthorn) is the common name of all plant species in the genus Crataegus of the Rosaceae family. In the present study, three monomers of (+)-catechin (C), (−)-epicatechin gallate (ECg) and (−)-epigallocatechin (EGC) were isolated from the hawthorn under the guide of antibacterial sensitization activity. The bioactivity of the composite fraction in enhancing the antibacterial effect of oxacillin against methicillin-resistant Staphylococcus aureus (MRSA) was greater than that of the individual monomer of the hawthorn extract in vitro. Two-fold dilution and checkerboard methods were used to analyze antibacterial activity and screen for the combination and proportion of monomers with the best bioactivity. The result showed that C (128 mg/L) combined with ECg (16 mg/L) had the greatest effect and the combination also reduced the bacterial load in blood of septic mice challenged with a sublethal dose of MRSA, increased daunomycin accumulation within MRSA and down-regulated the mRNA expression of norA, norC and abcA, three important efflux pumps of MRSA. In summary, C and ECg enhanced the antibacterial effect of β-lactam antibiotics against MRSA in vitro and in vivo, which might be related to the increased accumulation of antibiotics within MRSA via suppression of important efflux pumps’ gene expression.
Keywords: fructus crataegi; (+)-catechin; (−)-epicatechin gallate; synergistic effect; MRSA; drug accumulation fructus crataegi; (+)-catechin; (−)-epicatechin gallate; synergistic effect; MRSA; drug accumulation
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Qin, R.; Xiao, K.; Li, B.; Jiang, W.; Peng, W.; Zheng, J.; Zhou, H. The Combination of Catechin and Epicatechin Gallate from Fructus Crataegi Potentiates β-Lactam Antibiotics Against Methicillin-Resistant Staphylococcus aureus (MRSA) in Vitro and in Vivo. Int. J. Mol. Sci. 2013, 14, 1802-1821.

AMA Style

Qin R, Xiao K, Li B, Jiang W, Peng W, Zheng J, Zhou H. The Combination of Catechin and Epicatechin Gallate from Fructus Crataegi Potentiates β-Lactam Antibiotics Against Methicillin-Resistant Staphylococcus aureus (MRSA) in Vitro and in Vivo. International Journal of Molecular Sciences. 2013; 14(1):1802-1821.

Chicago/Turabian Style

Qin, Rongxin; Xiao, Kangkang; Li, Bin; Jiang, Weiwei; Peng, Wei; Zheng, Jiang; Zhou, Hong. 2013. "The Combination of Catechin and Epicatechin Gallate from Fructus Crataegi Potentiates β-Lactam Antibiotics Against Methicillin-Resistant Staphylococcus aureus (MRSA) in Vitro and in Vivo." Int. J. Mol. Sci. 14, no. 1: 1802-1821.


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