Objective:

To investigate

18

F radiolabeling fluoroethoxylerianin (FEE) and Micro positron emission tomography (PET)/computed tomography (CT) of

18

F-FEE

a derivative of an active ingredient of anticancer traditional Chinese medicine (TCM) erianin

and to preliminarily explore the applications of positron nuclide labeling such as

18

F and PET/CT into the evaluation of new drugs derived of the active components of TCM.

Methods:

The optimized preparation conditions of

18

F-FEE were carried out

including the multiple reaction parameters affecting

18

F radiolabeling and hydrolysis. The radiolabeling rate and hydrolysis efficiency were detected by radio-TLC

and the radiochemical purity of

18

F-FEE was measured by radio-HPLC. The biodistribution and MicroPET/ CT of 18 F-FEE in normal BALB/c mice and HepG2 xenograft model in BALB/c nude mice were performed.

Results:

The optimizedconditions of

18

F adiolabeling reaction were time 10 min

temperature 100 ℃

precursor concentration of 5 mg/mL and solvent as MeCN. The optimized hydrolysis reaction conditions were time 10 min

temperature 100 ℃ and hydrochloric acid concentration of 6 mol/L. According to the optimized conditions

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F-FEE was successfully synthesized with the radiochemical purity of more than 95%. The biodistribution and MicroPET/CT in normal rats showed that

18

F-FEE was mainly distributed in metabolic tissues such as liver

intestine

kidney and bladder

while the distribution of heart

lung and other tissues was low. MicroPET/CT in HepG2 liver cancer models showed that

18

F-FEE was diffusely distributed in tumor tissues for a long time with high tumor %ID/g

and the T/ M was more than 10 at 60 min post injection.

Conclusion:

This study optimized and established the

18

F radiolabeling conditions of

18

F-FEE as the derivative of erianin

an active ingredient of anti-cancer TCM. The synthesis conditions of

18

F-FEE were reliable with high radiochemical purity.

18

F-FEE was mainly distributed in vivo in liver

intestine

kidney and other metabolic tissues

and significantly distributed in HepG2 tumor

which could provide intuitive experimental means for the anti-tumor potential of FEE

and other natural active TCM components and their derivatives with anticancer potentials.