131I标记番泻苷A在正常小鼠体内分布和评价心肌活性研究

doi:10.7538/tws.2013.26.02.0098

同位素 ›› 2013, Vol. 26 ›› Issue (2): 98-103.DOI: 10.7538/tws.2013.26.02.0098

• 放射性药物和标记化合物 • 上一篇下一篇

¹³¹I标记番泻苷A在正常小鼠体内分布和评价心肌活性研究

王俊虎^1,2;蒋翠花²;江骁²;李玥²;孙自平³;殷志琦¹;张健²;倪以成^2,4

1.中国药科大学天然药物化学教研室, 江苏南京210009；2.江苏省中医药研究院转化医学实验室, 江苏南京210028；3.山东省医学科学院放射医学研究所, 山东济南564314；4.比利时鲁汶大学医学院医学影像部, 比利时鲁汶BE-30000

出版日期:2013-05-20 发布日期:2013-06-18

The Research onBiodistribution of ¹³¹I-Iodosennoside A in Normal Mice and toEvaluate Myocardial Activity

WANG Jun-hu^1,2;JIANG Cui-hua²;JIANG Xiao²;LI Yue²;SUN Zi-ping³;YIN Zhi-qi¹;ZHANG Jian²;NI Yi-cheng²^，4

1. Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China;2. Laboratory of Translational Medicine, Jiangsu Province Institute of Traditional Chinese Medicine, Nanjing 210028, China;3. The Radiation Medical Institute, Shandong Academy of Medical Sciences, Jinan 564314, China;4.Theragnostic Laboratory, Department of Imaging & Pathology, Biomedical Sciences Group, Leuven BE-30000, Belgium

Online:2013-05-20 Published:2013-06-18

摘要/Abstract

摘要：

采用Iodogen法标记番泻苷A得到¹³¹I标记番泻苷A溶液，并研究¹³¹I标记番泻苷A在小鼠体内分布和用于检测坏死心肌细胞的可行性。将标记物静脉注射到正常小鼠体内，分别在给药4、24、48 h后处死，测定标记物在主要脏器的分布。采用结扎左冠状动脉前降支法建立大鼠急性心肌梗死模型，考察¹³¹I标记番泻苷A给药24h后，在主要脏器、梗死心肌上分布，并采用2,3,5-氯化三苯基四氮唑（TTC）染色和磷屏自显影对心脏切片进行组织学分析。结果显示：¹³¹I标记番泻苷A在小鼠血中清除较快，肾脏的放射性摄取高。¹³¹I标记番泻苷A主要分布在大鼠的梗死心肌区域，梗死心肌与正常心肌放射性摄取比为11.9。TTC染色和磷屏自显影对比证明，¹³¹I标记番泻苷A对坏死心肌具有较强靶向性。结果表明，¹³¹I标记番泻苷A能选择性的在大鼠坏死心肌区域聚集，在心肌梗死诊断方面具有较好的开发前景。

关键词: ^{font-family: 'Times New Roman'">¹³¹}font-family: 'Times New Roman'">Ifont-family: 宋体">标记番泻苷font-family: 'Times New Roman'">A, font-family: 宋体">心肌梗死font-family: 'Times New Roman'">, font-family: 宋体">磷屏自显影font-family: 'Times New Roman'">, 2,3,5-font-family: 宋体">氯化三苯基四氮唑（font-family: 'Times New Roman'">TTCfont-family: 宋体">）

Abstract:

Purpose: The objective ofthis project is to evaluate biodistribution of [¹³¹I]Iodosennoside Ain normal mice and explore the feasibility on the diagnosis of myocardialinfarction. Methods: Iodogen method was used to radioiodinate sennoside A with ¹³¹I.[¹³¹I]Iodosennoside A was intravenously injected into mice. Threegroups of mice were killed at 4 h, 24 h and 48 h post injection respectivelyand the radioactive uptake in major organs were calculated. Rats were subjectedto left anterior descending (LAD) coronary artery ligation to induce acutemyocardial infarction. Rat models of myocardial infarction were intravenouslyinjected [¹³¹I]iodosennoside A. 24 h after injection of [¹³¹I]iodosennosideA, the regional distribution of radioiodinated sennoside A was determined byradioactivity counting technique. 2,3,5-triphenyl tetrazolium chloride (TTC)staining and autoradiography were performed with 2 mm thick sections of heartsfor postmortem verifications. Results: The study showed high uptake of [¹³¹I]iodosennosideA in kidneys and fast blood clearance. At 24 h post injection, radioactivityconcentration in infarcted myocardium was over 11.9 times higher than in normalmyocardium. Preferential uptake of the [¹³¹I]iodosennoside A innecrotic tissue was confirmed by perfect match of images from TTC staining andautoradiography. Conclusion: The result proved that [¹³¹I]iodosennosideA has myocardial necrosis affinity and may serve as a marker on the diagnosisof myocardial infarction.

Key words: ^{font-family: 'Times New Roman'">131}font-family: 'Times New Roman'">I-Iodosennoside A, myocardial infarction, autoradiography, 2,3,5-triphenyltetrazolium chloride(TTC)

王俊虎;蒋翠花;江骁;李玥;孙自平;殷志琦;张健;倪以成. ¹³¹I标记番泻苷A在正常小鼠体内分布和评价心肌活性研究[J]. 同位素, 2013, 26(2): 98-103.

WANG Jun-hu;JIANG Cui-hua;JIANG Xiao;LI Yue;SUN Zi-ping;YIN Zhi-qi;ZHANG Jian;NI Yi-cheng. The Research onBiodistribution of ¹³¹I-Iodosennoside A in Normal Mice and toEvaluate Myocardial Activity[J]. Journal of Isotopes, 2013, 26(2): 98-103.

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¹³¹I标记番泻苷A在正常小鼠体内分布和评价心肌活性研究

The Research onBiodistribution of ¹³¹I-Iodosennoside A in Normal Mice and toEvaluate Myocardial Activity

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