期刊
TETRAHEDRON
卷 85, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2021.132065
关键词
Endophyte; Fusarium sp.; Lipodepsipeptide; Fusaristatin; Cytotoxicity; Antibacterial activity
资金
- German Academic Exchange Service (DAAD)
- Deutsche Forschungsgemeinschaft (DFG, German Research Foundation) [270650915/GRK 2158, RTG 2578]
- Duesseldorf School of Oncology - Comprehensive Cancer Center Duesseldorf/Deutsche Krebshilfe
- Duesseldorf School of Oncology - Medical Faculty of the Heinrich Heine University Duesseldorf
Three new lipodepsipeptides and a new alpha-pyrone derivative were isolated from solid rice cultures of a Chinese medicinal plant endophyte. The structures of the new metabolites were determined using spectroscopic techniques, and their cytotoxicity and antibacterial activities were evaluated. One compound showed moderate cytotoxicity against lymphoma cell lines, while another exhibited good to weak antibacterial activity against Gram-positive bacteria.
Three new lipodepsipeptides, fusaristatins D-F (1-3) and a new alpha-pyrone derivative, (7S,8R)(-)-chlamydospordiol (5), together with eight known compounds (4, 6-12) were obtained from solid rice cultures of Fusarium sp. BZCB-CA, an endophyte of the Chinese medicinal plant, Bothriospermum chinense. The planar structures of the new metabolites (1-3, 5) were established by spectroscopic techniques (1D/2D NMR and HRESIMS). Marfey's method was applied to determine the absolute configuration of 1, while the absolute configuration of 5 was determined by single-crystal X-ray crystallography analysis in addition to Mosher's method. Crystallographic data of inflatin C(7) are also supplied here for the first time. In cytotoxicity assays, rubrofusarin (8) showed a moderate effect on the lymphoma cell lines L5178Y, Ramos and Jurkat, with IC50 values of 7.7, 6.2 and 6.3 mu M, respectively, while the remaining compounds were inactive. When subjected to antibacterial assay, only lateropyrone (9) exhibited good to weak activity against a panel of Gram-positive bacteria including drug-resistant strains with MICs ranging from 3.1 to 25 mu M. (C) 2021 Elsevier Ltd. All rights reserved.
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