Chalcomoracin and moracin C, new inhibitors of Staphylococcus aureus enoyl-acyl carrier protein reductase from Morus alba.
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.
Korea Research Institute of Bioscience and Biotechnology, Yusong, Daejeon, Korea.
Yu Jin
YJ
Kim
Mi-Jin
MJ
Sohn
Won-Gon
WG
Kim
D019342:Acetic Acid / Q000378:metabolism; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors; D001572:Benzofurans / Q000032:analysis / Q000494:pharmacology*; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH) / Q000037:antagonists & inhibitors*; D005227:Fatty Acids / Q000096:biosynthesis; D008826:Microbial Sensitivity Tests; D031625:Morus / Q000737:chemistry*; D010936:Plant Extracts / Q000494:pharmacology*; D018515:Plant Leaves; D014176:Protein Biosynthesis / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects* / Q000254:growth & development / Q000378:metabolism; D013267:Stilbenes / Q000032:analysis / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D001572:Benzofurans; D005227:Fatty Acids; D010936:Plant Extracts; D013267:Stilbenes; C550211:chalcomoracin; C475758:moracin C; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH); D019342:Acetic Acid