van Rensburg C E, Gatner E M, Imkamp F M, Anderson R
Antimicrob Agents Chemother. 1982 May;21(5):693-7. doi: 10.1128/AAC.21.5.693.
The effects of clofazimine on neutrophil activities such as random motility, migration to the leukoattractants endotoxin-activated serum and N-formyl-L-methionyl-L-leucyl-L-phenylalanine phagocytosis of Candida albicans, postphagocytic hexose-monophosphate shunt activity, and myeloperoxidase-mediated iodination and the effects of clofazimine on lymphocyte transformation to mitogens were assessed in vitro and after ingestion of the drug by normal individuals and patients with lepromatous leprosy. For in vitro studies, the concentration range of the drug investigated was 10(-6) M to 10(-2) M. for in vivo studies, subjects ingested 200 mg of clofazimine daily for a period of 5 days. At concentrations of 5 X 10(-6) M to 5 X 10(-3) M clofazimine caused a progressive dose-dependent inhibition of neutrophil motility without detectable effects on phagocytosis, postphagocytic hexose-monophosphate shunt activity, or myeloperoxidase-mediated iodination. Over the same concentration range, clofazimine inhibited lymphocyte transformation. The inhibitory effect on neutrophil motility was associated with a spontaneous stimulation of oxidative metabolism and could be prevented by coincubation of dapsone with clofazimine. after ingestion of clofazimine responsiveness of lymphocytes to mitogens was decreased in normal volunteers and leprosy patients: neutrophil motility in normal individuals was likewise inhibited.
在体外以及正常个体和瘤型麻风患者摄入该药后,评估了氯法齐明对中性粒细胞活性(如随机运动、向内毒素激活血清和N-甲酰-L-蛋氨酰-L-亮氨酰-L-苯丙氨酸趋化运动、对白色念珠菌的吞噬作用、吞噬后己糖单磷酸旁路活性以及髓过氧化物酶介导的碘化作用)的影响,以及氯法齐明对淋巴细胞向有丝分裂原转化的影响。对于体外研究,所研究药物的浓度范围为10^(-6)M至10^(-2)M。对于体内研究,受试者每天摄入200mg氯法齐明,持续5天。在浓度为5×10^(-6)M至5×10^(-3)M时,氯法齐明引起中性粒细胞运动的剂量依赖性渐进抑制,而对吞噬作用、吞噬后己糖单磷酸旁路活性或髓过氧化物酶介导的碘化作用无明显影响。在相同浓度范围内,氯法齐明抑制淋巴细胞转化。对中性粒细胞运动的抑制作用与氧化代谢的自发刺激有关,并且可通过将氨苯砜与氯法齐明共同孵育来预防。在摄入氯法齐明后,正常志愿者和麻风患者淋巴细胞对有丝分裂原的反应性降低:正常个体的中性粒细胞运动同样受到抑制。