Anderson R, Jooné G K
Department of Immunology, University of Pretoria, South Africa.
Chemotherapy. 1993 Nov-Dec;39(6):424-31. doi: 10.1159/000238988.
In this study the intraphagocytic bioactivities of the new fluoroquinolone antimicrobial agents clinafloxacin (CI-960) and PD 131628 (the active metabolite of CI-990) were investigated in vitro at final concentrations of 0.0005-0.5 microgram/ml using human neutrophils and the combination of a radiometric and a colony-counting method, which enabled us to distinguish between intracellular bacteriostatic and bactericidal mechanisms. Ciprofloxacin was included for comparison. Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 25922) were used as the test intraphagocytic microbial pathogens. Clinafloxacin (> or = 0.05 microgram/ml) displayed potent intraphagocytic bactericidal activity against S. aureus, while PD 131628 was merely bacteriostatic. Ciprofloxacin displayed relatively unimpressive bacteriostatic rather than bactericidal activity for S. aureus. Against E. coli, the intraphagocytic activity of clinafloxacin (0.001-0.005 microgram/ml and above) was superior to that of PD 131628 or ciprofloxacin, which were approximately equipotent. Clinafloxacin is a potent intraphagocytic bactericidal agent for both gram-positive and gram-negative bacteria.
在本研究中，使用人中性粒细胞以及放射性测量法与菌落计数法相结合的方法，在体外以0.0005 - 0.5微克/毫升的终浓度研究了新型氟喹诺酮抗菌剂克林沙星（CI - 960）和PD 131628（CI - 990的活性代谢产物）的吞噬细胞内生物活性，这使我们能够区分细胞内抑菌和杀菌机制。环丙沙星作为对照。金黄色葡萄球菌（ATCC 25923）和大肠杆菌（ATCC 25922）用作测试吞噬细胞内的微生物病原体。克林沙星（≥0.05微克/毫升）对金黄色葡萄球菌表现出强大的吞噬细胞内杀菌活性，而PD 131628仅仅具有抑菌作用。环丙沙星对金黄色葡萄球菌表现出相对不显著的抑菌而非杀菌活性。对于大肠杆菌，克林沙星（0.001 - 0.005微克/毫升及以上）的吞噬细胞内活性优于PD 131628或环丙沙星，后两者活性大致相当。克林沙星对革兰氏阳性菌和革兰氏阴性菌都是一种强大的吞噬细胞内杀菌药物。
