Baijnath Sooraj, Shobo Adeola, Bester Linda A, Singh Sanil D, Kruger Gert, Arvidsson Per I, Naicker Tricia, Govender Thavendran
Catalysis and Peptide Research Unit, University of KwaZulu-Natal, E-Block, 6th Floor, Room E1-06-016, Westville Campus, Durban, South Africa.
Biomedical Resource Unit, University of KwaZulu-Natal, Westville Campus, Durban, South Africa.
J Mol Histol. 2016 Aug;47(4):429-35. doi: 10.1007/s10735-016-9685-0. Epub 2016 Jun 21.
A study was undertaken to determine the neuroprotective potential of Linezolid (LIN) in an animal model. Female Sprague-Dawley rats were either given a single (100 mg/kg) dose or treated daily for 4 weeks. A validated LC-MS/MS method was used to measure LIN levels in plasma and brain, this was paired with mass spectrometry imaging to determine the tissue spatial distribution of the drug. The results showed that after a single dose there was poor penetration of the drug into the brain. With multiple doses there were high tissue levels, with the drug reaching steady state in subsequent weeks. LIN displayed a promising distribution pattern with localisation in the brainstem. Systemic circulation is fed into the brain by the carotid and vertebral arteries which enter through the brain stem, therefore high drug concentrations is this area may protect against infectious agents entering via this route.
开展了一项研究以确定利奈唑胺（LIN）在动物模型中的神经保护潜力。对雌性斯普拉格-道利大鼠给予单次剂量（100毫克/千克）或每日治疗4周。采用经过验证的液相色谱-串联质谱法（LC-MS/MS）测量血浆和脑中的LIN水平，并与质谱成像相结合以确定药物的组织空间分布。结果表明，单次给药后药物进入脑内的渗透率较低。多次给药后组织中药物水平较高，且在随后几周药物达到稳态。LIN呈现出在脑干定位的有前景的分布模式。全身循环通过颈动脉和椎动脉进入脑内，这些血管穿过脑干，因此该区域的高药物浓度可能预防通过此途径进入的感染因子。
