Olenick J G, Hahn F E
Antimicrob Agents Chemother. 1972 Mar;1(3):259-62. doi: 10.1128/AAC.1.3.259.
The growth of a strain of Bacillus megaterium was prevented by a minimal inhibitory concentration of primaquine of 52 mug/ml or 2 x 10(-4)m. When exponentially growing cultures received the drug at 6 x 10(-4)m, the rate of growth was drastically reduced and no further growth occurred after 15 min of exposure. At this concentration, primaquine was bactericidal, causing a 50% reduction in the viable population after one doubling time of 45 min. Supplying primaquine to cultures 30 min after adding radioactive-labeled phenylalanine, thymidine, uracil, or diaminopimelic acid produced an immediate and complete inhibition of protein biosynthesis but no inhibition of deoxyribonucleic acid biosynthesis for at least 15 min, and caused the formation of ribonucleic acid and cell wall polymer to proceed linearly at rates similar to those established prior to the addition of drug. This pattern of inhibition of macromolecular biosyntheses suggests that the major in vivo action of primaquine in B. megaterium is to block protein synthesis.
52微克/毫升或2×10⁻⁴摩尔的伯氨喹最低抑菌浓度可抑制巨大芽孢杆菌菌株的生长。当指数生长的培养物接受6×10⁻⁴摩尔的该药物时,生长速率急剧降低,暴露15分钟后不再有进一步生长。在此浓度下,伯氨喹具有杀菌作用,在45分钟的一个倍增时间后,活菌数量减少50%。在添加放射性标记的苯丙氨酸、胸苷、尿嘧啶或二氨基庚二酸30分钟后向培养物中供应伯氨喹,可立即完全抑制蛋白质生物合成,但至少15分钟内不抑制脱氧核糖核酸生物合成,并使核糖核酸和细胞壁聚合物的形成以与添加药物之前确定的速率相似的线性速率进行。这种对大分子生物合成的抑制模式表明,伯氨喹在巨大芽孢杆菌中的主要体内作用是阻断蛋白质合成。