Cheminformatics analysis shows that most marine microbial natural products are like terrestrial microbial natural products. New methods to access novel marine microbial chemistry are needed.
Bioassay-guided investigation of the sponge Aaptos lobata resulted in the isolation and identification of two new amphiphilic polyamines, aaptolobamines A (1) and B (2). Their structures were determined through analysis of NMR and MS data. MS analysis also indicated that A. lobata contained a complex mixture of aaptolobamine homologues. Both aaptolobamines A (1) and B (2) show broad bioactivity, including cytotoxicity against cancer cell lines, moderate antimicrobial activity against a methicillin-resistant strain of Staphylococcus aureus, and weak activity against a Pseudomonas aeruginosa strain. The mixtures of aaptolobamine homologues were shown to contain compounds that bind to the Parkinson's disease associated amyloid protein α-synuclein and inhibit its aggregation.
One new furoquinoline alkaloid, leptanoine D (1) and nine known alkaloids 2–10 were isolated from Pitaviaster haplophyllus. Leptanoine D (1) contains a typically unstable vinyl ether moiety and was structurally elucidated based on 2D NMR, (+)-HR-ESI-MS, and ECD data. The structures of the known furoquinoline alkaloids leptanoine A (11) and B (12) have also been revised. Compounds 1–10 were screened against three species of bacteria (Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli), however they showed no activity at the highest dose tested (32µg mL−1). The compounds were also evaluated for anti-proliferative action against PC-3 and WPMY-1 cells, with 7–9 displaying weak activity at 100μM.
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