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- Title
Antibacterial activity and cytotoxicity analysis of halistanol trisulphate from marine sponge Petromica citrina.
- Authors
Marinho, Palloma R.; Simas, Naomi Kato; Kuster, Ricardo Machado; Duarte, Rafael Silva; Fracalanzza, Sergio Eduardo Longo; Ferreira, Davis Fernandes; Romanos, Maria Teresa Villela; Muricy, Guilherme; Giambiagi-DeMarval, Marcia; Laport, Marinella Silva
- Abstract
Objectives An aqueous extract and fraction from the marine sponge Petromica citrina have antibacterial activity. We performed a chemical and biological characterization of the antibiotic substance from P. citrina and investigated its mode of action on Staphylococcus aureus cells. Methods The inhibitory activity of the aqueous extract of P. citrina was determined against 14 bacteria belonging to type strains and clinical antibiotic-resistant strains. The aqueous extract was fractionated under bioassay guidance and the bioactive substance was identified by its 1H-NMR, 13C-NMR and mass spectra. The MIC and the MBC of this substance were determined. This substance was also subjected to cytotoxic bioassays. The mode of action on S. aureus cells was investigated by light and transmission electron microscopy analysis. Results P. citrina showed a large spectrum of activity against type strains and resistant-bacteria such as S. aureus, Staphylococcus epidermidis, Enterococcus faecalis, Mycobacterium fortuitum and Neisseria gonorrhoeae. The aqueous extract was fractionated and halistanol trisulphate (24ɛ,25-dimethylcholestane-2β,3α,6α-triol trisodium sulphate) was isolated for the first time from P. citrina. Halistanol trisulphate had a bactericidal effect on exponentially growing S. aureus cells at the MIC (512 mg/L). Cytotoxicity biossays showed moderate toxicity against cancer cell line L929 (fibrosarcoma). This substance apparently acts by damaging the cell membrane, with subsequent cell lysis. Conclusions Halistanol trisulphate is a broad-spectrum antibiotic isolated from P. citrina with a mode of action involving disruption of the cytoplasmic membrane. It is a new candidate for research on antibacterial substances.
- Subjects
SPONGES (Invertebrates); ANTIBIOTICS; BIOCHEMICAL mechanism of action; STAPHYLOCOCCUS aureus; ANIMAL extracts; BIOLOGICAL assay; DRUG resistance in microorganisms; CANCER cells
- Publication
Journal of Antimicrobial Chemotherapy (JAC), 2012, Vol 67, Issue 10, p2396
- ISSN
0305-7453
- Publication type
Article
- DOI
10.1093/jac/dks229