Preliminary Biological Evaluation of 18F-FBEM-Cys-Annexin V a Novel Apoptosis Imaging Agent
AbstractA novel annexin V derivative (Cys-Annexin V) with a single cysteine residue at its C-terminal has been developed and successfully labeled site-specifically with 18F-FBEM. 18F-FBEM was synthesized by coupling 18F-fluorobenzoic acid (18F-FBA) with N-(2-aminoethyl)maleimide using optimized reaction conditions. The yield of 18F-FBEM-Cys-Annexin V was 71.5% ± 2.0% (n = 4, based on the starting 18F-FBEM, non-decay corrected). The radiochemical purity of 18F-FBEM-Cys-Annexin V was >95%. The specific radioactivities of 18F-FBEM and 18F-FBEM-Cys-Annexin V were >150 and 3.17 GBq/µmol, respectively. Like the 1st generation 18F-SFB-Annexin V, the novel 18F-FBEM-Cys-Annexin V mainly shows renal and to a lesser extent, hepatobiliary excretion in normal mice. In rat hepatic apoptosis models a 3.88 ± 0.05 (n = 4, 1 h) and 10.35 ± 0.08 (n = 4, 2 h) increase in hepatic uptake of 18F-FBEM-Cys-Annexin V compared to normal rats was observed after injection via the tail vein. The liver uptake ratio (treated/control) at 2 h p.i. as measured via microPET correlated with the ratio of apoptotic nuclei in liver observed using TUNEL histochemistry, indicating that the novel 18F-FBEM-Cys-Annexin V is a potential apoptosis imaging agent. View Full-Text
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Lu, C.; Jiang, Q.; Hu, M.; Tan, C.; Yu, H.; Hua, Z. Preliminary Biological Evaluation of 18F-FBEM-Cys-Annexin V a Novel Apoptosis Imaging Agent. Molecules 2015, 20, 4902-4914.
Lu C, Jiang Q, Hu M, Tan C, Yu H, Hua Z. Preliminary Biological Evaluation of 18F-FBEM-Cys-Annexin V a Novel Apoptosis Imaging Agent. Molecules. 2015; 20(3):4902-4914.Chicago/Turabian Style
Lu, Chunxiong; Jiang, Quanfu; Hu, Minjin; Tan, Cheng; Yu, Huixin; Hua, Zichun. 2015. "Preliminary Biological Evaluation of 18F-FBEM-Cys-Annexin V a Novel Apoptosis Imaging Agent." Molecules 20, no. 3: 4902-4914.