Xiao Wu, Scott Thomas M, Feng Liping, Yu Zhongshui, Wang Lili, Hughes Jeffrey A, Liu Hu
School of Pharmacy, Memorial University of Newfoundland, St. John's, Newfoundland, Canada.
J Nucl Med. 2003 May;44(5):770-3.
A cholesteryl ester analog, cholesteryl 1,3-diiopanoate glyceryl ether (C2I), was synthesized and investigated for its potential use for the detection of atherosclerotic lesions in rabbits.
(125)I-labeled C2I was incorporated into acetylated low-density lipoprotein (AcLDL). The resultant complex, (125)I-C2I-AcLDL, was injected intravenously into 2 groups of rabbits, fed cholesterol and normal chow, at a dose of 555 kBq/kg. Tissue samples were taken 24 h after injection for the biodistribution study. Atherosclerotic lesions and C2I deposition in aortic samples were examined by Sudan IV staining and autoradiography, respectively.
The levels of C2I in blood and aortic samples in cholesterol-fed animals were 2- to 3-fold higher than those in the control group (P < 0.05). The autoradiography results correlated well with the Sudan IV staining results, indicating sites of C2I deposition superimposed on lesion sites.
C2I was preferentially taken up and retained at atherosclerotic lesion sites, suggesting its potential use for the detection of early atherosclerosis.
合成了一种胆固醇酯类似物，1,3 - 二碘泛酸胆固醇甘油醚（C2I），并研究了其用于检测兔动脉粥样硬化病变的潜在用途。
将（125）I标记的C2I掺入乙酰化低密度脂蛋白（AcLDL）中。将所得复合物（125）I - C2I - AcLDL以555 kBq/kg的剂量静脉注射到两组分别喂食胆固醇和正常食物的兔体内。注射后24小时采集组织样本进行生物分布研究。分别通过苏丹IV染色和放射自显影检查主动脉样本中的动脉粥样硬化病变和C2I沉积。
喂食胆固醇动物的血液和主动脉样本中C2I水平比对照组高2至3倍（P < 0.05）。放射自显影结果与苏丹IV染色结果相关性良好，表明C2I沉积部位与病变部位重叠。
C2I优先在动脉粥样硬化病变部位摄取和保留，表明其在早期动脉粥样硬化检测中的潜在用途。
