| Title |
Radiosynthesis and pharmacokinetics of [18F]fluoroethyl bufalin in hepatocellular carcinoma-bearing mice
|
|---|---|
| Published in |
OncoTargets and therapy, January 2017
|
| DOI | 10.2147/ott.s110281 |
| Pubmed ID | |
| Authors |
Zhaoshuo Yang, Jianhua Liu, Qingqing Huang, Zhouji Zhang, Jiawei Zhang, Yanjia Pan, Yunke Yang, Dengfeng Cheng |
| Abstract |
Bufalin, the main component of a Chinese traditional medicine chansu, shows convincing anticancer effects in a lot of tumor cell lines. However, its in vivo behavior is still unclear. This research aimed to evaluate how bufalin was dynamically absorbed after intravenous injection in animal models. We developed a radiosynthesis method of [(18)F]fluoroethyl bufalin to noninvasively evaluate the tissue biodistribution and pharmacokinetics in hepatocellular carcinoma-bearing mice. [(18)F]fluoroethyl bufalin was synthesized with conjugation of 18F-CH2CH2OTs and bufalin. The radiochemical purity was proved by the radio-high-performance liquid chromatography (HPLC). The pharmacokinetic studies of [(18)F]fluoroethyl bufalin were then performed in Institute of Cancer Research (ICR) mice. Furthermore, the biodistribution and metabolism of [(18)F]fluoroethyl bufalin in HepG2 and SMMC-7721 tumor-bearing nude mice were studied in vivo by micro-positron emission tomography (micro-PET). The radiochemical purity (RCP) of [(18)F]fluoroethyl bufalin confirmed by radio-HPLC was 99%±0.18%, and [(18)F]fluoroethyl bufalin showed good in vitro and in vivo stabilities. Blood dynamics of [(18)F]fluoroethyl bufalin conformed to the two compartments in the ICR mice model. The pharmacokinetic parameters of [(18)F]fluoroethyl bufalin were calculated by DAS 2.0 software. The area under concentration-time curve (AUC0-t) and the values of clearance (CL) were 540.137 μg/L·min and 0.001 L/min/kg, respectively. The half-life of distribution (t1/2α ) and half-life of elimination (t1/2β ) were 0.693 and 510.223 min, respectively. Micro-PET imaging showed that [(18)F]fluoroethyl bufalin was quickly distributed via the blood circulation; the major tissue biodistribution of [(18)F]fluoroethyl bufalin in HepG2 and SMMC-7721 tumor-bearing mice was liver and bladder. [(18)F]fluoroethyl bufalin was accumulated rapidly in the liver at an early time point (5 min) post injection (pi) and then declined slowly, mainly through both the hepatic pathway and the renal pathway. Our study showed the biodistribution of [(18)F]fluoroethyl bufalin in micro-PET images and provided visible information for demonstrating the bioactivities of bufalin. |
X Demographics
The data shown below were collected from the profiles of 2 X users who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Germany | 1 | 50% |
| Pakistan | 1 | 50% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 2 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 3 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 3 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Professor > Associate Professor | 1 | 33% |
| Researcher | 1 | 33% |
| Student > Doctoral Student | 1 | 33% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 1 | 33% |
| Agricultural and Biological Sciences | 1 | 33% |
| Medicine and Dentistry | 1 | 33% |
Attention Score in Context
This research output has an Altmetric Attention Score of 2. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 11 July 2018.
All research outputs
#16,721,717
of 25,374,647 outputs
Outputs from OncoTargets and therapy
#982
of 3,016 outputs
Outputs of similar age
#255,077
of 421,653 outputs
Outputs of similar age from OncoTargets and therapy
#35
of 64 outputs
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