Hou Yunlong, Fan Shengjun, Zhang Hong, Gu Yuanqin, Yu Xuhui, Li Baoxin
Department of Pharmacology, Harbin Medical University, Harbin, PR China.
Mol Vis. 2010 Aug 17;16:1659-68.
Although the naturally occurring antioxidant mangiferin has been widely used, it is not yet known whether it can cross the blood-retina barrier (BRB) and enter the eye. The purpose of this experiment was to investigate the ability of mangiferin to pass the blood-retina barrier.
Sprague-Dawley rats were used for biologic fluid sampling after intravenous administration of mangiferin at doses of 10, 25, and 50 mg/kg. Blood and retina samples were collected at different time points post-dose. High-performance liquid chromatography (HPLC) separation was conducted on a COSMOSIL 5C(18)-MS-II column (4.6 mm x 250 mm, 5 microm) with a flow rate of 1.0 ml/min using a mobile phase comprised of methanol -2% glacial acetic acid (40:60 v:v).
The HPLC method has proven suitable to determine the presence of mangiferin in the eye. The plasma concentration of mangiferin was dose dependent. Pharmacokinetic parameters of mangiferin in plasma after intravenous administration were fitted to the two-compartment model with the first-order elimination and first-order transfer between central and peripheral compartments. The concentration of mangiferin in the retina goes with that in the blood. Mangiferin concentrations in the retina reached 5.69+/-1.48 microg/ml 0.5 h after intravenous administration (50 mg/kg) and then dropped gradually to 0.30+/-0.02 microg/ml 5.0 h later. The eye-to-plasma concentration ratio was 2.80%.
Mangiferin can pass the blood-retina barrier after a single intravenous administration and may be a potential natural antioxidant in treating eye diseases.
尽管天然存在的抗氧化剂芒果苷已被广泛使用，但尚不清楚它是否能够穿过血视网膜屏障（BRB）并进入眼内。本实验的目的是研究芒果苷穿过血视网膜屏障的能力。
将Sprague-Dawley大鼠用于静脉注射剂量为10、25和50mg/kg的芒果苷后的生物流体采样。给药后在不同时间点采集血液和视网膜样本。使用由甲醇-2%冰醋酸（40:60 v:v）组成的流动相，在COSMOSIL 5C(18)-MS-II柱（4.6mm×250mm，5μm）上以1.0ml/min的流速进行高效液相色谱（HPLC）分离。
HPLC方法已被证明适用于测定眼中芒果苷的存在。芒果苷的血浆浓度呈剂量依赖性。静脉给药后芒果苷在血浆中的药代动力学参数符合具有一级消除以及中央室和外周室之间一级转运的二室模型。视网膜中芒果苷的浓度与血液中的浓度一致。静脉注射（50mg/kg）后0.5小时，视网膜中芒果苷浓度达到5.69±1.48μg/ml，然后在5.0小时后逐渐降至0.30±0.02μg/ml。眼与血浆浓度比为2.80%。
单次静脉给药后芒果苷能够穿过血视网膜屏障，可能是治疗眼部疾病的一种潜在天然抗氧化剂。
