Anti-Staphylococcus aureus activity and oxacillin resistance modulating capacity of 3-O-acyl-catechins
Anti-Staphylococcus aureus activity and oxacillin resistance modulating capacity of 3-O-acyl-catechins
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DOI：
10.1016/j.ijantimicag.2004.03.024
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发表时间：
2004-10-01
影响因子：
10.8
通讯作者：
Taylor, PW
中科院分区：
文献类型：
--
作者：
Stapleton, PD;Shah, S;Taylor, PW
表儿茶素没食子酸酯（ECg）是绿茶中对金黄色葡萄球菌活性较弱的一种成分，当浓度低于MIC时，可降低耐甲氧西林金黄色葡萄球菌对奥西林的耐药性。由于儿茶素与人工脂质双分子层结合，我们研究了儿茶素是否可以通过增加其与细胞质膜相互作用的能力来提高其抗葡萄球菌活性。ECg的没食子酸酯基团被不同长度的3- o -酰基链（C-4-C-18）取代，导致抗葡萄球菌活性增强，链长为C-8（辛烷基）和C-10（癸烷基）。3- o -辛烷基儿茶素对MRSA具有杀菌作用。3- o-酰基儿茶素在1/4 MIC下测试，并没有使奥西林MIC降低2倍以上。3- o -酰基儿茶素作为抗葡萄球菌药物值得进一步研究。(C) 2004 Elsevier B.V.与International Society of Chemotherapy。版权所有。
Epicatechin gallate (ECg), a component of green tea with weak activity against Staphylococcus aureus, reduces oxacillin resistance in methicillin-resistant S. aureus at concentrations below the MIC. Because catechins bind to artificial lipid bilayers, we investigated whether the anti-staphylococcal activity of catechins could be improved by increasing their capacity to interact with the cytoplasmic membrane. Substitution of the gallate group of ECg with 3-O-acyl chains of varying lengths (C-4-C-18) led to enhanced anti-staphylococcal activity with chain lengths of C-8 (octanoyl) and C-10 (decanoyl). 3-O-octanoyl catechin was bactericidal against MRSA as the result of membrane damage. 3-O-acyl catechins tested at a 1/4 MIC did not reduce the oxacillin MIC greater than two-fold. 3-O-acyl catechins warrant further investigation as anti-staphylococcal agents. (C) 2004 Elsevier B.V. and the International Society of Chemotherapy. All rights reserved.