Stapleton Paul D, Shah Saroj, Hamilton-Miller Jeremy M T, Hara Yukihiko, Nagaoka Yasuo, Kumagai Ayako, Uesato Shinichi, Taylor Peter W
Microbiology Group, School of Pharmacy, 29-39 Brunswick Square, London WC1N 1AX, UK.
Int J Antimicrob Agents. 2004 Oct;24(4):374-80. doi: 10.1016/j.ijantimicag.2004.03.024.
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.
表没食子儿茶素没食子酸酯（ECg）是绿茶的一种成分，对金黄色葡萄球菌活性较弱，在低于最低抑菌浓度（MIC）的浓度下可降低耐甲氧西林金黄色葡萄球菌对苯唑西林的耐药性。由于儿茶素可与人工脂质双层结合，我们研究了能否通过增强儿茶素与细胞质膜的相互作用能力来提高其抗葡萄球菌活性。用不同长度（C(4)-C(18)）的3-O-酰基链取代ECg的没食子酸酯基团，可增强抗葡萄球菌活性，其中C(8)（辛酰基）和C(10)（癸酰基）链长的效果最佳。3-O-辛酰基儿茶素因膜损伤对耐甲氧西林金黄色葡萄球菌具有杀菌作用。在1/4 MIC浓度下测试的3-O-酰基儿茶素不会使苯唑西林的MIC降低超过两倍。3-O-酰基儿茶素作为抗葡萄球菌药物值得进一步研究。
