Liu L X, Durham D G, Richards R M
School of Pharmacy, Faculty of Health and Social Care, The Robert Gordon University, Aberdeen, UK.
J Pharm Pharmacol. 2001 Jan;53(1):129-32. doi: 10.1211/0022357011775118.
The development of clinical vancomycin-resistant strains of enterococci (VRE) is a major cause for concern. Here we show that a combination of galangin or 3,7-dihydroxyflavone with vancomycin may be used to sensitize resistant strains of Enterococcus faecalis and Enterococcus faecium to the level of vancomycin-sensitive strains. Minimum inhibitory concentrations (MICs) and viable counts were determined in Iso-sensitest broth using a microtitre method. MICs of vancomycin against 67% of resistant clinical isolates and a type strain of enterococci were lowered from > 250 microg mL(-1) to < 4 microg mL(-1) in the presence of galangin (12.5 microg mL(-1)) or 3,7-dihydroxyflavone (6.25 microg mL(-1)). Viable counts for type culture E. faecalis ATCC 51299 showed the flavonoids alone significantly lowered numbers of colony forming units (CFUs). CFUs were maintained at low levels (< 10(3) CFU mL(-1)) for 24 h by vancomycin/flavone combinations. This combinational action in reversing vancomycin resistance of enterococci highlights novel drug targets and has importance in the design of new therapeutic regimes against resistant pathogens.
肠球菌临床耐万古霉素菌株（VRE）的出现是一个主要的担忧原因。在此我们表明，高良姜素或3,7 - 二羟基黄酮与万古霉素联合使用，可使粪肠球菌和屎肠球菌的耐药菌株对万古霉素敏感菌株的水平敏感。使用微量滴定法在异感测肉汤中测定最低抑菌浓度（MIC）和活菌数。在存在高良姜素（12.5μg mL⁻¹）或3,7 - 二羟基黄酮（6.25μg mL⁻¹）的情况下，万古霉素对67%的耐药临床分离株和一株肠球菌标准菌株的MIC从>250μg mL⁻¹降至<4μg mL⁻¹。粪肠球菌ATCC 51299标准培养物的活菌数表明，单独的黄酮类化合物显著降低了菌落形成单位（CFU）的数量。万古霉素/黄酮联合用药可使CFU在24小时内维持在低水平（<10³ CFU mL⁻¹）。这种逆转肠球菌对万古霉素耐药性的联合作用突出了新的药物靶点，并且在设计针对耐药病原体的新治疗方案方面具有重要意义。
