Modulation of beta-lactam resistance in Staphylococcus aureus by catechins and gallates.

Stapleton, P.D., Shah, S., Anderson, J.C., Hara, Y., Hamilton-Miller, J.M.T. and Taylor, P.W. (2004) Modulation of beta-lactam resistance in Staphylococcus aureus by catechins and gallates. International Journal of Antimicrobial Agents, 23 (5). pp. 462-467. 10.1016/j.ijantimicag.2003.09.027.

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DOI: 10.1016/j.ijantimicag.2003.09.027


Aqueous extracts of Japanese green tea (Camellia sinensis) are able to reverse beta-lactam resistance in methicillin-resistant Staphylococcus aureus (MRSA). We have attributed the capacity to reverse oxacillin resistance in the homogeneous PBP2a producer BB568 and in EMRSA-16 to (-)-epicatechin gallate (ECG) and (-)-catechin gallate (CG). Minimum inhibitory concentration (MIC) values for oxacillin were reduced from 256 and 512 to 1-4 mg/l, respectively, in the presence of these polyphenols. In addition, (-)-epigallocatechin gallate (EGCG) had a moderate capacity to modulate oxacillin activity against S. aureus BB568, but none against EMRSA-16. ECG, CG and EGCG increased the sensitivity of EMRSA-15 to oxacillin. The gallate moiety was essential for the oxacillin-modulating activity of ECG, as both (-)-epicatechin and (-)-epicatechin-3-cyclohexylcarboxylate were unable to reverse resistance to oxacillin. Gallic acid and three alkyl gallates (methyl gallate, propyl gallate, and octyl gallate) did not modulate beta-lactam resistance in MRSA. Octyl gallate exhibited direct antibacterial activity against S. aureus BB568 (16 mg/l). Modulation of beta-lactam resistance by ECG significantly enhanced the activities of flucloxacillin and the carbapenem antibiotics imipenem and meropenem against 40 MRSA isolates, with MIC(90) values for the antibiotics reduced to the susceptibility breakpoint or below. Consequently, EGCG, CG and, particularly, ECG warrant further investigation as agents to combat beta-lactam resistance in S. aureus.

Item Type:Article
Departments, units and centres:Department of Pharmaceutics > Department of Pharmaceutics
ID Code:2636
Journal or Publication Title:International Journal of Antimicrobial Agents
Deposited By:Library Staff
Deposited On:12 Jan 2012 14:58
Last Modified:12 Jan 2012 14:58

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