Anti-Infective Agent Creation Engineering Research Centre of Sichuan Province, School of Pharmacy, Chengdu University, Chengdu 610106, China.
School of Food Science and Biological Engineering, Zhejiang Gongshang University, Hangzhou 310018, China.
Molecules. 2024 May 30;29(11):2574. doi: 10.3390/molecules29112574.
Isoflavones are a class of natural products that exhibit a wide range of interesting biological properties, including antioxidant, hepatoprotective, antimicrobial, and anti-inflammatory activities. Scandenone (), osajin (), and 6,8-diprenylgenistein () are natural prenylated isoflavones that share the same polyphenol framework. In this research, the key intermediate was used for the synthesis of the natural isoflavones -, establishing a stereoselective synthetic method for both linear and angular pyran isoflavones. The antibacterial activities of - were also evaluated, and all of them displayed good antibacterial activity against Gram-positive bacteria. Among them, was the most potent one against MRSA, with a MIC value of 2 μg/mL, and the SEM assay indicated that the bacterial cell membranes of both MRSA and could be disrupted by . These findings suggest that this type of isoflavone could serve as a lead for the development of novel antibacterial agents for the treatment of Gram-positive bacterial infections.
异黄酮是一类具有广泛有趣生物活性的天然产物，包括抗氧化、保肝、抗菌和抗炎活性。紫檀芪（）、紫檀茋（）和 6,8-二烯丙基染料木黄酮（）是天然的类异戊二烯基异黄酮，它们具有相同的多酚骨架。在这项研究中，使用关键中间体 合成了天然异黄酮 - ，为线性和角型吡喃异黄酮建立了立体选择性合成方法。还评估了 - 的抗菌活性，它们都对革兰氏阳性菌表现出良好的抗菌活性。其中，对 MRSA 的活性最强，MIC 值为 2 μg/mL，SEM 试验表明，MRSA 和 的细菌细胞膜都可以被 破坏。这些发现表明，这种类型的异黄酮可以作为开发新型抗菌剂治疗革兰氏阳性菌感染的先导化合物。
