Korea Research Institute of Bioscience and Biotechnology, Yusong, Daejeon, Korea.
Biol Pharm Bull. 2012;35(5):791-5. doi: 10.1248/bpb.35.791.
Bacterial enoyl-acyl carrier protein (ACP) reductase has been confirmed as a novel target for antibacterial drug development. In the screening of inhibitors of Staphylococcus aureus enoyl-ACP reductase (FabI), we found that a methanol extract of leaves of Morus alba L. potently inhibited S. aureus FabI as well as growth of S. aureus. The active principles were identified as chalcomoracin and moracin C by MS and NMR analysis. Chalcomoracin and moracin C inhibited S. aureus FabI with IC(50) of 5.5 and 83.8 µM, respectively. They also prevented the growth of S. aureus with minimum inhibitory concentration (MIC) of 4 and 32 µg/mL, respectively. Consistent with their inhibition against FabI and bacterial growth, they prevented (14)C]acetate incorporation into fatty acid in S. aureus while didn't affect protein synthesis. In this study, we reported that chalcomoracin and moracin C, potent antibacterial compounds from Morus alba, inhibited FabI and fatty acid synthesis.
细菌烯酰-酰基载体蛋白（ACP）还原酶已被证实是一种新的抗菌药物开发靶点。在筛选金黄色葡萄球菌烯酰-ACP 还原酶（FabI）抑制剂的过程中，我们发现桑科植物白桑的甲醇提取物能有效抑制金黄色葡萄球菌 FabI 以及金黄色葡萄球菌的生长。通过 MS 和 NMR 分析，确定活性成分为桑黄酮和桑辛素 C。桑黄酮和桑辛素 C 对金黄色葡萄球菌 FabI 的抑制 IC50 分别为 5.5 和 83.8 µM。它们还分别以 4 和 32 µg/mL 的最小抑菌浓度（MIC）抑制了金黄色葡萄球菌的生长。与它们对 FabI 和细菌生长的抑制作用一致，它们阻止了（14）C]乙酸盐掺入金黄色葡萄球菌的脂肪酸中，而不影响蛋白质合成。在这项研究中，我们报道了白桑中的强效抗菌化合物桑黄酮和桑辛素 C 抑制 FabI 和脂肪酸合成。
