Antibacterial activity of guanidinylated neomycin B- and kanamycin A-derived amphiphilic lipid conjugates
Why this work is in the frame
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Bibliographic record
Abstract
OBJECTIVES: Neomycin B exhibits poor antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa, while kanamycin A shows weak activity against MRSA, methicillin-resistant Staphylococcus epidermidis (MRSE) and P. aeruginosa. The main purpose of this work was to study whether lipid conjugation of guanidinylated neomycin B- and kanamycin A-derived cationic headgroups could restore antibacterial activity against neomycin B- and kanamycin A-resistant strains, while retaining antibacterial activity against non-resistant strains. METHODS: Seven polyguanidinylated neomycin B-lipids differing in the nature of the lipid tail and two cationic kanamycin A-lipids were prepared, and their in vitro activity was assessed against a variety of neomycin B- and kanamycin A-resistant and neomycin B- and kanamycin A-non-resistant Gram-positive and Gram-negative strains. RESULTS: Conjugation of neomycin B- and kanamycin A-derived polyamine or polyguanidinylated headgroups to hydrophobic C16 or C20 lipid tails restored the anti-MRSA activity of both aminoglycosides and the anti-MRSE activity of kanamycin A. Polyguanidinylation of the neomycin B-derived headgroup lowers the hydrophobic requirement of the lipid tail segment to provide broad-spectrum antibacterial activity from C16 to C12. Moreover, guanidinylation of the polycationic headgroup in neomycin B-derived cationic lipids enhances antibacterial activity against a neomycin B-, kanamycin A- and gentamicin-resistant P. aeruginosa strain, and reduces haemolytic activity. CONCLUSIONS: These findings suggest that lipid conjugation of neomycin B- and kanamycin A-derived cationic lipids provides a general tool to enhance the antibacterial activity of these two aminoglycosides against resistant strains.
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Full frame distilled prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.
Codex and Gemma teacher scores by category
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.000 | 0.000 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.001 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.000 |
| Insufficient payload (model declined to judge) | 0.001 | 0.000 |
Machine scores (provisional)
The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.
Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.
score_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it