期刊
MARINE DRUGS
卷 17, 期 8, 页码 -出版社
MDPI
DOI: 10.3390/md17080465
关键词
Callyspongia siphonella; LC-HRESIMS; metabolomic profiling; oxindole alkaloids; tisindoline; antibacterial; antibiofilm; antitrypanosomal; anticancer
资金
- German Research Foundation (DFG)
- University of Wuerzburg
In the present study, LC-HRESIMS-assisted dereplication along with bioactivity-guided isolation led to targeting two brominated oxindole alkaloids (compounds 1 and 2) which probably play a key role in the previously reported antibacterial, antibiofilm, and cytotoxicity of Callyspongia siphonella crude extracts. Both metabolites showed potent antibacterial activity against Gram-positive bacteria, Staphylococcus aureus (minimum inhibitory concentration (MIC) = 8 and 4 mu g/mL) and Bacillus subtilis (MIC = 16 and 4 mu g/mL), respectively. Furthermore, they displayed moderate biofilm inhibitory activity in Pseudomonasaeruginosa (49.32% and 41.76% inhibition, respectively), and moderate in vitro antitrypanosomal activity (13.47 and 10.27 mu M, respectively). In addition, they revealed a strong cytotoxic effect toward different human cancer cell lines, supposedly through induction of necrosis. This study sheds light on the possible role of these metabolites (compounds 1 and 2) in keeping fouling organisms away from the sponge outer surface, and the possible applications of these defensive molecules in the development of new anti-infective agents.
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