Hand W L, King-Thompson N L, Steinberg T H
J Antimicrob Chemother. 1983 Oct;12 Suppl C:1-11. doi: 10.1093/jac/12.suppl_c.1.
Optimal therapy of infections due to organisms capable of surviving within phagocytes would include use of antimicrobials that penetrate phagocytic cells and inactivate intracellular organisms. To establish those characteristics of drug and cell that mediate the antibiotic-phagocyte interaction, we have studied the uptake of radiolabelled antibiotics by rabbit alveolar macrophages (AM), human AM from smokers and non-smokers, and human polymorphonuclear leukocytes (PMN). Relative entries of drug groups into the three types of phagocytic cells were similar. Penicillin G and cephalosporin antibiotics were taken up poorly by phagocytes. Lipid-soluble antibiotics, such as rifampicin and chloramphenicol, were concentrated several-fold (2-5) by phagocytes. Ethambutol, erythromycin and clindamycin were concentrated many-fold (5-50) by phagocytic cells. Human AM of smokers accumulated certain antibiotics more avidly than AM of non-smokers. Clindamycin entry into phagocytes was shown to be an active, energy-requiring process, mediated by the nucleoside transport system. Ingestion of microbial particles by PMN stimulated transport of both clindamycin and nucleoside (adenosine) into the cell.
对于由能够在吞噬细胞内存活的微生物引起的感染，最佳治疗方法应包括使用能够穿透吞噬细胞并使细胞内微生物失活的抗菌药物。为了确定介导抗生素与吞噬细胞相互作用的药物和细胞的那些特性，我们研究了兔肺泡巨噬细胞（AM）、吸烟者和非吸烟者的人AM以及人多形核白细胞（PMN）对放射性标记抗生素的摄取情况。不同药物组进入这三种吞噬细胞的相对情况相似。青霉素G和头孢菌素类抗生素被吞噬细胞摄取的情况较差。脂溶性抗生素，如利福平和氯霉素，被吞噬细胞浓缩了几倍（2至5倍）。乙胺丁醇、红霉素和克林霉素被吞噬细胞浓缩了许多倍（5至50倍）。吸烟者的人AM比非吸烟者的AM更 avidly地积累某些抗生素。已证明克林霉素进入吞噬细胞是一个由核苷转运系统介导的活跃的、需要能量的过程。PMN摄取微生物颗粒刺激了克林霉素和核苷（腺苷）向细胞内的转运。 （注：avidly这个词在中文里不太好准确对应一个词，这里保留英文，可能需要结合上下文来理解其确切含义，大致可理解为“强烈地、热切地”等意思 ）
