Cunningham D, Schafer D, Tanenbaum S W, Flashner M
J Bacteriol. 1979 Feb;137(2):925-32. doi: 10.1128/jb.137.2.925-932.1979.
Cytochalasin A at 5 to 25 microgram/ml (1.0 x 10(-5) to 5.2 x 10(-5) M) inhibited the growth of three gram-positive bacteria, Arthrobacter sialophilus, Staphyloccus aureus, and Bacillus amyloliquifaciens, but had little or no effect on the growth of three gram-negative bacteria, Excherichia coli, Pseudomonas maltophilia, and Aeromonas proteolytica. A. sialophilus and S. aureus recovered spontaneously from cytochalasin A-mediated growth inhibition after a considerable lag period, which was dependent on the drug dose. It was demonstrated that this long-term recovery did not involve selection of resistant variants. Cytochalasin A had no detrimental effect on cell viability in A. sialophilus or S. aureus, but caused lysis of B. amyloliquifaciens. The drug prevented enzyme inductions and inhibited transport of valine, uridine, and glucose in the gram-positive organisms. It had little or no effect on these processes in the gram-negative organisms. In studies with A. sialophilus, the drug inhbitied respiration of exogenous substrates, but did not depress endogenous respiration. These results constitute the first unequivocal evidence for the bacteriostatic properties of this class of compounds and indicate that cytochalasin A halts various physiological processes in gram-positive bacteria primarily by inhibiting solute transport.
浓度为5至25微克/毫升(1.0×10⁻⁵至5.2×10⁻⁵摩尔)的细胞松弛素A抑制了三种革兰氏阳性菌嗜唾液节杆菌、金黄色葡萄球菌和淀粉液化芽孢杆菌的生长,但对三种革兰氏阴性菌大肠杆菌、嗜麦芽窄食单胞菌和溶蛋白气单胞菌的生长几乎没有影响或没有影响。嗜唾液节杆菌和金黄色葡萄球菌在一段相当长的延迟期后从细胞松弛素A介导的生长抑制中自发恢复,延迟期取决于药物剂量。结果表明,这种长期恢复不涉及抗性变体的选择。细胞松弛素A对嗜唾液节杆菌或金黄色葡萄球菌的细胞活力没有有害影响,但会导致淀粉液化芽孢杆菌裂解。该药物可防止酶诱导,并抑制革兰氏阳性菌中缬氨酸、尿苷和葡萄糖的转运。它对革兰氏阴性菌中的这些过程几乎没有影响或没有影响。在对嗜唾液节杆菌的研究中,该药物抑制外源底物的呼吸,但不抑制内源呼吸。这些结果构成了这类化合物具有抑菌特性的首个明确证据,并表明细胞松弛素A主要通过抑制溶质转运来阻止革兰氏阳性菌中的各种生理过程。