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Original Research

Radiosynthesis and pharmacokinetics of [18F]fluoroethyl bufalin in hepatocellular carcinoma-bearing mice

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Pages 329-338 | Published online: 11 Jan 2017

Figures & data

Scheme 1 A scheme of fluoroethyl bufalin and [18F]fluoroethyl bufalin synthesis.

Abbreviation: DMF, N,N-dimethylformamide.
Scheme 1 A scheme of fluoroethyl bufalin and [18F]fluoroethyl bufalin synthesis.

Figure 1 HPLC chromatogram of [19F]fluoroethyl bufalin and [18F]fluoroethyl bufalin.

Notes: HPLC chromatogram of (isocratic, 0.05 mol/L phosphate buffer [pH =7.0], flow 1 mL/min) (A) [19F]fluoroethyl bufalin, TR =17.78 min (UV =280 nm) and (B) [18F]fluoroethyl bufalin, TR =17.86 min.
Abbreviations: DAD, diode array detector; HPLC, high-performance liquid chromatography; RCP, radiochemical purity; TR, retention time; UV, ultraviolet.
Figure 1 HPLC chromatogram of [19F]fluoroethyl bufalin and [18F]fluoroethyl bufalin.

Figure 2 Stability of [18F]fluoroethyl bufalin at different intervals in 0.1 mol/L PBS (A) and mouse serum (B).

Abbreviations: PBS, phosphate-buffered saline; RCP, radiochemical purity.
Figure 2 Stability of [18F]fluoroethyl bufalin at different intervals in 0.1 mol/L PBS (A) and mouse serum (B).

Figure 3 Biodistributions of [18F]fluoroethyl bufalin in SMMC-7721 (A) and HepG2 (B) xenograft-bearing nude mice.

Notes: SMMC-7721 (A) and HepG2 (B) mice were injected with 7.4 MBq of [18F]fluoroethyl bufalin, and biodistribution was studied at 45, 120 and 240 min after injection. Radioactivity accumulation was expressed as %ID/g after a single intravenous injection of 7.4 MBq of [18F]fluoroethyl bufalin in 0.5 mL at 45, 120, and 240 min (n=5/group, mean ± SD). %ID/g, percentage of injected dose per gram of tissue per body weight.
Abbreviation: T, tumor.
Figure 3 Biodistributions of [18F]fluoroethyl bufalin in SMMC-7721 (A) and HepG2 (B) xenograft-bearing nude mice.

Table 1 Biodistribution of [18F]fluoroethyl bufalin in nude mice

Figure 4 The blood drug concentration–time curve for [18F]fluoroethyl bufalin in the ICR mice.

Notes: The blood drug concentration–time curve for [18F]fluoroethyl bufalin in the ICR mice till 10 hour pi. %ID/g, percentage of injected dose per gram of tissue per body weight.
Abbreviations: ICR, Institute of Cancer Research; pi, post injection.
Figure 4 The blood drug concentration–time curve for [18F]fluoroethyl bufalin in the ICR mice.

Table 2 Pharmacokinetic parameters of the [18F]fluoroethyl bufalin in ICR mice

Figure 5 Dynamic small-animal PET scans obtained for [18F]fluoroethyl bufalin with SMMC-7721 T-bearing mice and HepG2 T-bearing mice.

Notes: Coronal whole-body slices that contained Ts are shown; arrows indicate Ts.
Abbreviations: PET, positron emission tomography; Ts, tumors.
Figure 5 Dynamic small-animal PET scans obtained for [18F]fluoroethyl bufalin with SMMC-7721 T-bearing mice and HepG2 T-bearing mice.

Figure 6 Quantified time–activity curves of major organs in SMMC-7721 and HepG2 T-bearing mice.

Notes: (A) Quantified time–activity curves of major organs (T, liver, heart, and kidney) after injection of 7.4 MBq [18F]fluoroethyl bufalin in SMMC-7721 T-bearing mice (n=3). (B) Quantified time–activity curves of major organs (T, liver, heart, and kidney) after injection of 7.4 MBq [18F]fluoroethyl bufalin in HepG2 T-bearing mice (n=3). %ID/g, percentage of injected dose per gram of tissue per body weight.
Abbreviation: T, tumor.
Figure 6 Quantified time–activity curves of major organs in SMMC-7721 and HepG2 T-bearing mice.