Amphiphilic Polyamine α-Synuclein Aggregation Inhibitors from the Sponge Aaptos lobata.

Abstract

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.

• Authors: Tanja M Voser, Joshua B Hayton, Dale W Prebble, Ju Jin, Gary Grant, Merrick G Ekins, Anthony R Carroll
• Journal: Journal of natural products (J Nat Prod) Vol. 86 Issue 3 Pg. 475-481 (03 24 2023) ISSN: 1520-6025 [Electronic] United States
• PMID: 36795859 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• alpha-Synuclein
• Antineoplastic Agents
• Polyamines

Topics

• Animals
• alpha-Synuclein
• Antineoplastic Agents (pharmacology)
• Cell Line
• Staphylococcus aureus
• Polyamines (pharmacology)
• Porifera