Tsuchiya H, Sato M, Miyazaki T, Fujiwara S, Tanigaki S, Ohyama M, Tanaka T, Iinuma M
Department of Dental Pharmacology, Asahi University School of Dentistry, Gifu, Japan.
J Ethnopharmacol. 1996 Jan;50(1):27-34. doi: 10.1016/0378-8741(96)85514-0.
Differently substituted flavanones were isolated from Leguminosae and their antibacterial activity was comparatively studied against methicillin-resistant Staphylococcus aureus (MRSA). The minimum inhibitory concentrations (MICs) of phytochemical flavanones to clinical isolates of MRSA were determined by a serial agar dilution method. The structure-activity relationship has indicated that 2',4'- or 2',6'-dihydroxylation of the B ring and 5,7-dihydroxylation of the A ring in the flavanone structure are important for significant anti-MRSA activity and that substitution with a certain aliphatic group at the 6- or 8-position also enhances the activity. Among the thirteen flavanones tested, tetrahydroxyflavanones with these structural characteristics isolated from Sophora exigua and Echinosophora koreensis showed intensive activity to inhibit the growth of all MRSA strains at 3.13-6.25 micrograms/ml. The present hydroxyflavanones would be useful in the phytotherapeutic strategy against MRSA infections.
从豆科植物中分离出不同取代的黄烷酮，并对其抗耐甲氧西林金黄色葡萄球菌（MRSA）的抗菌活性进行了比较研究。通过系列琼脂稀释法测定了植物化学黄烷酮对MRSA临床分离株的最低抑菌浓度（MIC）。构效关系表明，黄烷酮结构中B环的2',4'-或2',6'-二羟基化以及A环的5,7-二羟基化对于显著的抗MRSA活性很重要，并且在6-或8-位用特定脂肪族基团取代也会增强活性。在所测试的13种黄烷酮中，从苦豆子和韩国刺槐中分离出的具有这些结构特征的四羟基黄烷酮在3.13-6.25微克/毫升时对所有MRSA菌株的生长均表现出强烈的抑制活性。目前这些羟基黄烷酮在针对MRSA感染的植物治疗策略中可能会有用处。
