Perumal V K, Gangadharam P R, Iseman M D
Am Rev Respir Dis. 1987 Aug;136(2):334-7. doi: 10.1164/ajrccm/136.2.334.
In order to understand the discrepant results between in vitro and in vivo activity of rifabutin (LM 427) against Mycobacterium intracellulare, we studied its effects upon the phagocytosis of M. intracellulare by resident and activated mouse peritoneal and alveolar macrophages and upon growth of M. intracellulare inside these cells. Rifabutin (ansamycin, LM 427) had no effect on the viability of resident or activated peritoneal or alveolar macrophages or on the phagocytosis of M. intracellulare by resident peritoneal macrophages. In activated peritoneal and alveolar macrophages, it had a dose-related effect on the phagocytic index and intracellular growth of M. intracellulare. Macrophages from mice pretreated with 10 or 20 mg/kg of rifabutin either orally or intraperitoneally for 4 to 10 days showed inhibition of intracellular growth of M. intracellulare in a dose-related manner. The route of administration or further addition of the drug did not enhance the inhibitory activity of these macrophages. These results indicate that rifabutin has the potential of killing M. intracellulare persisters inside macrophages.
为了理解利福布汀（LM 427）对细胞内分枝杆菌的体外和体内活性之间存在差异的结果，我们研究了其对驻留和活化的小鼠腹腔及肺泡巨噬细胞吞噬细胞内分枝杆菌的影响，以及对这些细胞内细胞内分枝杆菌生长的影响。利福布汀（安莎霉素，LM 427）对驻留或活化的腹腔或肺泡巨噬细胞的活力或驻留腹腔巨噬细胞对细胞内分枝杆菌的吞噬作用均无影响。在活化的腹腔和肺泡巨噬细胞中，它对细胞内分枝杆菌的吞噬指数和细胞内生长具有剂量相关效应。经口服或腹腔注射10或20mg/kg利福布汀预处理4至10天的小鼠的巨噬细胞，对细胞内分枝杆菌的生长呈剂量相关的抑制作用。给药途径或进一步添加药物并未增强这些巨噬细胞的抑制活性。这些结果表明，利福布汀具有杀死巨噬细胞内细胞内分枝杆菌持留菌的潜力。
