Antibacterial activity and cytotoxicity analysis of halistanol trisulphate from marine sponge Petromica citrina.
OBJECTIVE
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 (1)H-NMR, (13)C-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 (24ε,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.
Instituto de Microbiologia Paulo de Góes, Universidade Federal do Rio de Janeiro, Av. Carlos Chagas Filho, 373, Cidade Universitária, 21941-590, Rio de Janeiro, Brazil.
Palloma R
PR
Marinho
Naomi Kato
NK
Simas
Ricardo Machado
RM
Kuster
Rafael Silva
RS
Duarte
Sergio Eduardo Longo
SE
Fracalanzza
Davis Fernandes
DF
Ferreira
Maria Teresa Villela
MT
Romanos
Guilherme
G
Muricy
Marcia
M
Giambiagi-Demarval
Marinella Silva
MS
Laport
D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D001419:Bacteria / Q000166:cytology / Q000187:drug effects*; D002457:Cell Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D045744:Cell Line, Tumor / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D005591:Chemical Fractionation; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008826:Microbial Sensitivity Tests; D008853:Microscopy; D011161:Porifera / Q000737:chemistry*; D013261:Sterols / Q000302:isolation & purification* / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D002457:Cell Extracts; D013261:Sterols; C072244:halistanol trisulfate