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Three new helvolic acid derivatives (named sarocladilactone A ( 1 ), sarocladilactone B ( 2 ) and sarocladic acid A ( 3a )), together with five known compounds (6,16-diacetoxy-25-hy- droxy-3,7-dioxy-29-nordammara-1,17(20)-dien-21-oic acid ( 3b ), helvolic acid ( 4 ), helvolinic acid ( 5 ), 6-desacetoxy-helvolic acid ( 6 ) and 1,2-dihydrohelvolic acid ( 7 )), were isolated from the endophytic fungus DX-THL3, obtained from the leaf of Dongxiang wild rice ( Oryza rufipogon Griff.). The structures of the new compounds were elucidated via HR-MS, extensive 1D and 2D NMR analysis and comparison with reported data. Compounds 1 , 2 , 4 , 5 , 6 and 7 exhibited potent antibacterial activities. In particular, sarocladilactone B ( 2 ), helvolinic acid ( 5 ) and 6-desacetoxy-helvolic acid ( 6 ) exhibited strongly Staphylococcus aureus inhibitory activity with minimum inhibitory concentration (MIC) values of 4, 1 and 4 μg/mL, respectively. The structure-activity relationship (SAR) of these compounds was primarily summarized.

molecules/molecules online/molecules annual

New Helvolic Acid Derivatives with Antibacterial Activities from Sarocladium oryzae DX-THL3, an Endophytic Fungus from Dongxiang Wild Rice (Oryza rufipogon Griff.)