Engle E C, Manes S H, Drlica K
J Bacteriol. 1982 Jan;149(1):92-8. doi: 10.1128/jb.149.1.92-98.1982.
Both oxolinic acid and coumermycin A1, inhibitors of DNA gyrase, block DNA synthesis in Escherichia coli. At low concentrations of oxolinic acid, the rate of bacterial DNA synthesis first declines rapidly but then gradually increases. This gradual increase in synthesis rate depended on the presence of wild-type recA and lexA genes; mutations in either gene blocked the increase in synthesis rate. In such mutants, oxolinic acid caused a rapid decline, followed by a slow, further decrease in DNA synthesis rate. Coumermycin A1, however, produced a more gradual decline in synthesis rate which is unaffected by defects in the recA or lexA genes. An additional difference between the two drugs was observed in a dnaA mutant, in which initiation of replication is temperature sensitive. Low concentrations of oxolinic acid, but not coumermycin A1, reduced thermal inhibition of DNA synthesis rate.
喹诺酮酸和香豆霉素A1都是DNA促旋酶抑制剂,它们能阻断大肠杆菌中的DNA合成。在低浓度喹诺酮酸作用下,细菌DNA合成速率首先迅速下降,但随后逐渐增加。合成速率的这种逐渐增加取决于野生型recA和lexA基因的存在;任一基因发生突变都会阻断合成速率的增加。在这类突变体中,喹诺酮酸会导致DNA合成速率迅速下降,随后缓慢进一步降低。然而,香豆霉素A1使合成速率下降更为缓慢,且不受recA或lexA基因缺陷的影响。在dnaA突变体中观察到了这两种药物的另一个差异,该突变体中复制起始对温度敏感。低浓度的喹诺酮酸能降低DNA合成速率的热抑制,而香豆霉素A1则不能。