硝唑尼特和替唑尼特对结核分枝杆菌的体外及全血培养活性
Activity of nitazoxanide and tizoxanide against Mycobacterium tuberculosis in vitro and in whole blood culture.
作者信息
Harausz Elizabeth P, Chervenak Keith A, Good Caryn E, Jacobs Michael R, Wallis Robert S, Sanchez-Felix Manuel, Boom W Henry
机构信息
Department of Medicine, Case Western Reserve University, University Hospitals Case Medical Center, 10900 Euclid Ave, Cleveland, OH 44106, USA.
Department of Pathology, Case Western Reserve University, University Hospitals Case Medical Center, 10900 Euclid Ave, Cleveland, OH 44106, USA.
出版信息
Tuberculosis (Edinb). 2016 May;98:92-6. doi: 10.1016/j.tube.2016.03.002. Epub 2016 Mar 22.
Nitazoxanide (NTZ) and its metabolite tizoxanide (TIZ) were studied as antimycobacterial agents in vitro (in mycobacterial growth indicator tube [MGIT] cultures) and in a whole blood bactericidal assay. Both NTZ and TIZ show high protein binding. In MGIT cultures (albumin concentration = 78 μM), inhibition of Mycobacterium tuberculosis growth occurred at total drug concentrations of ≥16 μg/ml, whereas in whole blood cultures (albumin concentration = 350 μM), ≥128 μg/ml was required. Free drug fractions at these two conditions were estimated to be 69% and 2%, respectively. Co-incubation of NTZ and TIZ in human plasma for 72 h nearly completely eliminated their ability to inhibit mycobacterial growth in MGIT. Interactions with plasma proteins may limit the potential of NTZ and TIZ as drugs for human tuberculosis.
硝唑尼特（NTZ）及其代谢物替唑尼特（TIZ）作为抗分枝杆菌药物进行了体外研究（在分枝杆菌生长指示管[MGIT]培养物中）以及全血杀菌试验。NTZ和TIZ均显示出高蛋白结合率。在MGIT培养物中（白蛋白浓度 = 78 μM），当总药物浓度≥16 μg/ml时，结核分枝杆菌的生长受到抑制，而在全血培养物中（白蛋白浓度 = 350 μM），则需要≥128 μg/ml。在这两种条件下，游离药物分数分别估计为69%和2%。NTZ和TIZ在人血浆中共同孵育72小时几乎完全消除了它们在MGIT中抑制分枝杆菌生长的能力。与血浆蛋白的相互作用可能会限制NTZ和TIZ作为治疗人类结核病药物的潜力。
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