S-thanatin,an analogue of thanatin,was synthesised by substituting the fifteenth amino acid threonine with serine and showed broad antimicrobial activity against Gram-negative and Gram-positive *** evaluate its antimi...
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S-thanatin,an analogue of thanatin,was synthesised by substituting the fifteenth amino acid threonine with serine and showed broad antimicrobial activity against Gram-negative and Gram-positive *** evaluate its antimicrobial activity against a multidrug-resistant（MDR）clinical isolate as well as its anti-endotoxin activity,its lipopolysaccharide（LPS）-binding and-neutralising activity in vitro and its therapeutic efficacy in an experimental model of septic shock caused by a MDR clinical isolate of Escherichia coli were *** ability of S-thanatin to bind or neutralise LPS from *** O111:B4 was determined using a quantitative assay *** ICR mice were given an intraperitoneal（i.p.）administration of 2×10colony-forming units of *** *** bacterial challenge,all animals were randomised to receive *** of saline,40 mg/kg ceftazidime（CAZ）,or 40 mg/kg CAZ+ S-thanatin（10,20 or 40 mg/kg）.The results showed that S-thanatin not only completely bound to the LPS （median effective concentration of 17.5μg/mL）but also improved the survival and reduced the number of inoculated bacteria in a mouse model of septic shock.S-thanatin may be an attractive candidate to develop as an anti-MDR bacterial agent.
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