Acetylated Low-Density Lipoprotein-Encapsulated Cholesteryl 1,3-Diiopanoate Glyceryl Ether for the Detection of Atherosclerosis in Rabbits

A cholesteryl ester analog, cholesteryl 1,3-diiopanoate glyceryl ether (C21), was synthesized and investigated for its potential use for the detection of atherosclerotic lesions in rabbits. Methods: 125 I-labeled C21 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 C21 deposition in aortic samples were examined by Sudan IV staining and autoradiography, respectively. Results: 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 C21 deposition superimposed on lesion sites. Conclusion: C21 was preferentially taken up and retained at atherosclerotic lesion sites, suggesting its potential use for the detection of early atherosclerosis.