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

1 Department of Pharmacology, College of Pharmacy, The Third Military Medical University, Chongqing 400038, China 2 Medical Research Center, Southwestern Hospital, The Third Military Medical University, Chongqing 400038, China These authors contributed equally to this work.
* Authors to whom correspondence should be addressed.
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

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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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