Preparation of <sup>131</sup>I-23-hydroxybetulinic acid and in vivo evaluations in liver cancer HepA tumor-bearing mice

YANG Min1 WANG Guangji2 XU Yuping1 PAN Donghui1 WANG Songpei1 LI Xiaomin1 TANG Jie1 LUO Shineng1 1

doi:null

您当前的位置：

首页 >

文章列表页 >

Preparation of ¹³¹I-23-hydroxybetulinic acid and in vivo evaluations in liver cancer HepA tumor-bearing mice

更新时间：2021-03-12

- Preparation of ¹³¹I-23-hydroxybetulinic acid and in vivo evaluations in liver cancer HepA tumor-bearing mice
- NUCLEAR TECHNIQUES Vol. 31, Issue 8, (2008)
- 作者机构：
  
  1. 江苏省原子医学研究所,卫生部核医学重点实验室
  2. 中国药科大学
- 作者简介：
- 基金信息：
  
  吴阶平医学基金(320.6750.06116)资助;江苏省333高层次人才培养工程;江苏省医学重点人才(RC2007096)资助;江苏省卫生厅面上项目(H200735)
- DOI：
  CLC： R735.7;R817.9
- Published：01 August 2008
- 稿件说明：
移动端阅览
[1]杨敏,王广基,徐宇平,潘栋辉,王颂佩,李晓敏,唐婕,罗世能.23-羟基白桦酸的碘标记及其在荷肝癌HepA肿瘤鼠体内的分布[J].核技术,2008,31(08):637-640.

YANG Min1 WANG Guangji2 XU Yuping1 PAN Donghui1 WANG Songpei1 LI Xiaomin1 TANG Jie1 LUO Shineng1 1. Preparation of ¹³¹I-23-hydroxybetulinic acid and in vivo evaluations in liver cancer HepA tumor-bearing mice[J]. Nuclear techniques, 2008, 31(8): 637-640.
[1]杨敏,王广基,徐宇平,潘栋辉,王颂佩,李晓敏,唐婕,罗世能.23-羟基白桦酸的碘标记及其在荷肝癌HepA肿瘤鼠体内的分布[J].核技术,2008,31(08):637-640. DOI：

YANG Min1 WANG Guangji2 XU Yuping1 PAN Donghui1 WANG Songpei1 LI Xiaomin1 TANG Jie1 LUO Shineng1 1. Preparation of ¹³¹I-23-hydroxybetulinic acid and in vivo evaluations in liver cancer HepA tumor-bearing mice[J]. Nuclear techniques, 2008, 31(8): 637-640. DOI：

摘要

采用双氧水法对23-羟基白桦酸进行131I标记;以硅胶纸为支持介质

V二氯甲烷:V甲醇=9:1为展开剂

测定标记率及标记物放化纯;ICR小鼠和荷肝癌HepA肿瘤鼠尾静脉注射131I-23-羟基白桦酸（0.74MBq/只）后考察标记物的药代动力学性质及荷瘤鼠体内分布。结果显示

131I-23-羟基白桦酸标记率达98%

其放化纯在1、4、8d分别为98.5%、97.3%、95.8%。131I-23-羟基白桦酸在正常小鼠体内血液清除较快

其药代动力学模型符合二室模型。注射后0.5h荷肝癌HepA肿瘤鼠肝摄取最高（9.14%ID·g-1组织）

其次为肾、血、脾、肠、肺、肿瘤

脑中分布最少

仅为0.28%ID·g-1组织;肿瘤/肌肉比值>3。表明碘标23-羟基白桦酸标记率高

标记物稳定;碘标记物在荷肝癌HepA肿瘤鼠中的肿瘤靶向摄取提高2倍

可能是一新型增效的核素靶向治疗药物。

Abstract

In this work

preparation of 131I-labeled 23-hydroxybetulinic acid (131I-23-HBA) and its pharmacokinetics in mice were studied. 23-HBA was labeled with 131I using the hydrogen peroxide method. Purity and stability of the 131I-23-HBA were evaluated by silicon TLC

in which the substratum of Vdichoromethane: Vmethanol =9:1 was used as the developing agent. The dynamic distribution in ICR mice and liver cancer HepA tumor-bearing mice were studied. The results showed that the labeling yield of 131I-23-HBA was 98% and the radiochemical purities were 98.5%

97.3%

and 95.8% after 1

4 and 8 days

respectively. In ICR mice

the blood clearance was quick and the profile of the blood concentration-time was fitted with two compartment model. In tumor-bearing mice 0.5 h after intravenous injection

the liver uptake was the highest (9.14% ID·g-1). The radioisotope was concentrated in kidney

blood

spleen

intestine

lung and tumor

too. The brain uptake was the lowest as 0.28% ID/g at pi. 0.5 h. The tumor-to-muscle ratio was over 3. The labeling yield and purity of 131I-23-HBA are high and 131I-23-HBA is stable. The tumor uptake of 131I-23-HBA is higher than 23-HBA. 131I-23-HBA is a potent cancer treatment drug.

关键词

Keywords

references

Views

下载量

CSCD

Alert me when the article has been cited

提交

Tools

Publicity Resources

Radioiodine-labeling of tetrahydropalmatine and its biodistribution in mice

Synthesis and biological property evaluation of ⁹⁰Y radiolabeled glycosylated somatostatin

Radioiodine-labeling of salidroside and its biodistribution in mice

Progress of the targeted tumor therapy with α-emitting nuclides

Preparation of 3H-23-hydroxylbetulinic acid and in vivo evaluations in mice

Related Author

曹国宪

宋翠翠

陈波

张莉

林秀峰

2 LIN Xiufeng1 ZHANG Li1 CHEN Bo1 SONG Cuicui2 CAO Guoxian1 1

TAN Cheng1 YU Huixin1

ZHAI Shizhen1 DU Jin1

Related Institution

江南大学化工学院

Key Laboratory of Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Ministry of Health, Wuxi 214063, China) 2

北京100083 中国原子能科学研究院同位素研究所北京102413 中国同位素公司北京

北京大学基础医学院生物物理系

中国原子能科学研究院同位素研究所

AI问答

Address：2019 Jialuo Road, Jiading, Shanghai, China Postal code：201800
Tel：021-39194977 Email：LHB@sinap.ac.cn
Technical support is provided by Beijing Founder electronics co., LTD 沪ICP备05005479号-1 京公网安备11010802024621
It is recommended to read the content of this site in Chrome&IE9+. Please switch to extreme mode in browser 360.
Cookies We use cookies to help provide and enhance our service and tailor content. By continuing, you agree to the use of cookies.
Total Visits：881163 Visits Today：690

⁰

Preparation of 131I-23-hydroxybetulinic acid and in vivo evaluations in liver cancer HepA tumor-bearing mice

DOI：

摘要

Abstract

关键词

Keywords

references

Preparation of ¹³¹I-23-hydroxybetulinic acid and in vivo evaluations in liver cancer HepA tumor-bearing mice