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Figure 1.
Figure 1: Characterization of platensimycin. a, Structure of
platensimycin. b, In vivo studies on platensimycin. Dosing at 50
 g
h^-1 showed small decrease in viable S. aureus cells from the
infected kidney. However, a 10^4–10^5 fold decrease (4 and 5
log reduction) were achieved with 100 and 150 g
h^-1, respectively. Dosing at 150 g
h^-1 showed 40% of the kidneys with no viable S. aureus, whereas
dosing at 100 g
h^-1 showed 20% of the kidneys without detectable viable S.
aureus. Error bars indicate s.d. observed with five infected
mice. The results were confirmed by a repeat experiment. c,
Whole-cell labelling assay^16 with platensimycin. The assay was
performed with a serial dilution of platensimycin, starting at
500 g
ml^-1. Platensimycin showed no significant inhibition against
syntheses of DNA (open circles), cell wall (filled triangles),
protein (open squares) and RNA (open triangles) but greatly
inhibited phospholipid synthesis (filled circles), providing an
IC[50] value of 0.1 g
ml^-1. Error bars indicate s.d. for three individual
experiments. d, Direct binding assay results of
[^3H]dihydroplatensimycin and E. coli FabF (ecFabF) in the
presence and absence of n-dodecanoyl coenzyme A (lauroyl-CoA;
C[12]-CoA) and the C163Q mutant protein. Error bars indicate
s.d. observed with six replicate wells. Experimental details are
given in Supplementary Information.
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