TABLE 5.
In vivo analysis of membrane-active small molecules and AMPs against S. aureus
Membrane-active small molecules and AMPs | Effect against in vivo model | Effective concn against S. aureus | Animal model | References |
---|---|---|---|---|
nTZDpa | 90% survival | 16 μg/mL | C. elegans | 187 |
PQ401 | 100% survival | 2 μg/mL | C. elegans | 98 |
Small cationic molecule | 5.3-log MRSA biofilm reduction (>99.99%) | 40 mg/kg | Murine model of superficial skin wound infection | 194 |
l-lysine-based lipidated biphenyls | Reduced bacterial burden (P value 0.0001) | 200 mg/kg | Murine model of skin infection | 90 |
Xanthones derivatives | MRSA reduction by 2.56 logs (99.7%) and 3.03 logs (99.9%) | 3 mg/mL | Mouse model of corneal infection | 106 |
Bithionol + gentamicin | 90% MRSA persister killed | 30 mg/kg of bithionol + gentamicin | Mouse thigh infections | 97 |
Cationic peptide DFT561 | S. aureus USA300 LAC decreased by 1.8 logs (liver) and 1.4 logs (kidney) | 5 mg/kg | Neutropenic mouse model | 185 |
AMP is based on the cationic structure of honokiol/magnolol amphiphiles | Reduction in bacterial loads in the liver, spleen, and kidney in 3 days | 5 and 10 mg/kg | Murine sepsis model | 113 |