抗癌中药活性成分毛兰素衍生物 <sup>18</sup> F-FEE的 <sup>18</sup> F标记及其体内性质MicroPET/CT评价

王撵; 张丰盛; 张勇平; 宋少莉; 杨红; 王明伟

doi:10.19732/j.cnki.2096-6210.2022.04.005

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抗癌中药活性成分毛兰素衍生物 ¹⁸ F-FEE的 ¹⁸ F标记及其体内性质MicroPET/CT评价

论著 | 更新时间：2025-12-15

- 抗癌中药活性成分毛兰素衍生物 ¹⁸ F-FEE的 ¹⁸ F标记及其体内性质MicroPET/CT评价
- ¹⁸ F radiolabeling and MicroPET/CT evaluation of in vivo properties of 18 F-FEE as the derivative of erianin, an active component of anticancer traditional Chinese medicine
- 肿瘤影像学 2022年31卷第4期页码：372-379
- 作者机构：
  
  1. 上海师范大学化学与材料科学学院,上海,200234
  2. 复旦大学附属肿瘤医院核医学科，复旦大学上海医学院肿瘤学系,上海,200032
  3. 复旦大学生物医学影像研究中心,上海,200032
  4. 上海分子影像探针工程技术研究中心,上海,200032
- 作者简介：
- 基金信息：
  
  国家自然科学基金（21771041）
- DOI：10.19732/j.cnki.2096-6210.2022.04.005
  中图分类号：
- 网络出版：2022-08-28，
  
  纸质出版：2022-08-28
- 稿件说明：
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王撵,张丰盛,张勇平,等. 抗癌中药活性成分毛兰素衍生物 ¹⁸ F-FEE的 ¹⁸ F标记及其体内性质MicroPET/CT评价[J]. 肿瘤影像学, 2022, 31(4): 372-379 https://doi.

org/10.19732/j.cnki.2096-6210.2022.04.005
王撵,张丰盛,张勇平,等. 抗癌中药活性成分毛兰素衍生物 ¹⁸ F-FEE的 ¹⁸ F标记及其体内性质MicroPET/CT评价[J]. 肿瘤影像学, 2022, 31(4): 372-379 https://doi. DOI： 10.19732/j.cnki.2096-6210.2022.04.005.

org/10.19732/j.cnki.2096-6210.2022.04.005 DOI：

摘要

目的：

开展抗癌中药活性成分毛兰素衍生物氟乙氧基毛兰素（fluoroethoxylerianin，FEE）的

F标记及

F-FEE的Micro正电子发射体层成像（positron emission tomography，PET）/计算机体层成像（computed tomography，CT），初步探索

F等正电子核素标记与PET/CT在中药活性成分来源的新药评价中的应用。

方法：

开展

F-FEE的制备条件优化实验，包括影响

F标记和水解反应的多种反应条件，利用放射性薄层色谱法（radio-TLC）检测标记率和水解效率，放射性高效液相色谱法（radio-HPLC）测量

F-FEE的放射化学纯度，并进行正常BALB/c小鼠与HepG2细胞的BALB/c裸小鼠移植瘤模型的体内生物分布和MicroPET/CT评价。

结果：

优化的

F标记反应条件是时间10 min、温度100 ℃、前体浓度5 mg/mL、溶剂为乙腈，优化的水解反应条件是时间10 min、温度100 ℃、HCl溶液浓度6 mol/L。根据优化条件，成功合成了

F-FEE，其放射化学纯度大于95%。正常小鼠生物分布和MicroPET/CT显示，

F-FEE主要分布于肝、肠、肾和膀胱等代谢组织，心、肺等组织的分布较低。HepG2肝癌细胞移植瘤模型MicroPET/CT发现，

F-FEE长时间弥散分布于肿瘤组织，肿瘤%ID/g高，注射60 min后肿瘤-肌肉比值（T/M）高达10以上。

结论：

本研究优化了抗癌中药活性成分毛兰素衍生物

F-FEE的优化制备条件，

F-FEE的合成条件可靠、放射化学纯度高，在体内主要分布于肝、肠、肾等代谢组织，而且其在HepG2肿瘤内分布明显，为FEE抗肿瘤作用提供了直观的实验手段，为抗癌天然活性中药成分及其衍生物提供了新的评价技术。

Abstract

Objective:

To investigate

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

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

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

Methods:

The optimized preparation conditions of

F-FEE were carried out

including the multiple reaction parameters affecting

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

and the radiochemical purity of

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

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

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

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

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

F radiolabeling conditions of

F-FEE as the derivative of erianin

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

F-FEE were reliable with high radiochemical purity.

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.

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抗癌中药活性成分毛兰素衍生物 18 F-FEE的 18 F标记及其体内性质MicroPET/CT评价

18 F radiolabeling and MicroPET/CT evaluation of in vivo properties of 18 F-FEE as the derivative of erianin, an active component of anticancer traditional Chinese medicine

DOI：10.19732/j.cnki.2096-6210.2022.04.005

摘要

Abstract

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抗癌中药活性成分毛兰素衍生物 ¹⁸ F-FEE的 ¹⁸ F标记及其体内性质MicroPET/CT评价

¹⁸ F radiolabeling and MicroPET/CT evaluation of in vivo properties of 18 F-FEE as the derivative of erianin, an active component of anticancer traditional Chinese medicine