Inhibition
of DNA gyrase supercoiling activity by 1−3. The table summarizes the IC50 values for ciprofloxacin
and gyramides (R)-1, 2, 3,
and (S)-1. A representative gel obtained from the analysis
of the inhibition of DNA gyrase supercoiling activity is shown. The
open circle graphic represents relaxed closed circular DNA, the coiled
graphic signifies supercoiled DNA, and the arrow shows the direction
of increased mobility of supercoiled DNA states. Supercoiled (“S”),
linear (“L”), and relaxed (“R”) pUC19
controls are labeled above the lanes. Gel data for assays with 2 and 3 are shown (in μM); the label “C”
indicates the lane for the solvent control. The lane labeled “CIP”
represents treatment with 0.7 μM ciprofloxacin, which is the
IC50 for ciprofloxacin in our assay.