期刊
MARINE DRUGS
卷 12, 期 2, 页码 871-885出版社
MDPI
DOI: 10.3390/md12020871
关键词
Bacillus subtilis; lipopeptides; antimicrobial activity; cytotoxicity
资金
- Korea Institute of Ocean Science and Technology [PE99121]
- Ministry of Oceans and Fisheries, Korea [PM57420]
- Korea Institute of Marine Science & Technology Promotion (KIMST) [PE99121] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
Concerning the requirements of effective drug candidates to combat against high rising multidrug resistant pathogens, we isolated three new linear lipopeptides, gageostatins A-C (1-3), consisting of hepta-peptides and new 3--hydroxy fatty acids from the fermentation broth of a marine-derived bacterium Bacillus subtilis. Their structures were elucidated by analyzing a combination of extensive 1D, 2D NMR spectroscopic data and high resolution ESIMS data. Fatty acids, namely 3--hydroxy-11-methyltridecanoic and 3--hydroxy-9,11-dimethyltridecanoic acids were characterized in lipopeptides 1 and 2, respectively, whereas an unsaturated fatty acid (E)-7,9-dimethylundec-2-enoic acid was assigned in 3. The 3R configuration of the stereocenter of 3--hydroxy fatty acids in 1 and 2 was established by Mosher's MTPA method. The absolute stereochemistry of amino acid residues in 1-3 was ascertained by acid hydrolysis followed by Marfey's derivatization studies. Gageostatins 1-3 exhibited good antifungal activities with MICs values of 4-32 mu g/mL when tested against pathogenic fungi (R. solani, B. cinerea and C. acutatum) and moderate antibacterial activity against bacteria (B. subtilis, S. aeureus, S. typhi and P. aeruginosa) with MICs values of 8-64 mu g/mL. Futhermore, gageostatins 1-3 displayed cytotoxicity against six human cancer cell lines with GI(50) values of 4.6-19.6 mu g/mL. It is also noteworthy that mixed compounds 1+2 displayed better antifungal and cytotoxic activities than individuals.
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