γ计数仪测定^(99m)Tc-3PRGD_2在肺癌肿瘤模型小鼠中的组织分布  

Determination of biodistribution of ^(99m)Tc-3PRGD_2 in mice bearing the lung carcinoma xenograft by γ counter

作　　者：牛立云 李俭[2] 贾兵[3] 孟志云[2] 刘桃云[2] 顾若兰[2] 朱晓霞[2] 甘慧[2] 吴卓娜[2] 马百平[4] 窦桂芳[2] 

机构地区：[1]天津中医药大学,天津300193 [2]军事医学科学院野战输血研究所,北京100850 [3]北京大学医学同位素研究中心,北京100191 [4]军事医学科学院放射与辐射医学研究所,北京100850

出　　处：《国际药学研究杂志》2017年第8期795-799,共5页Journal of International Pharmaceutical Research

摘　　要：目的建立一种由γ计数仪测定放射性肿瘤显像剂锝[99mTc]标记的联肼尼克酰胺-3聚乙二醇-精氨酸-甘氨酸-天冬氨酸环肽二聚体(99mTc-3PRGD2)的方法,并研究肺癌肿瘤模型小鼠注射该显像剂后体内组织分布特点。方法设置4个正常分布组和1个冷肽封闭组(对照组),均经由尾静脉注射该显像剂(8μg/kg)于肺癌肿瘤模型小鼠,正常分布组分别于0.5、1、2和4 h取其组织,对照组在注射放射性药物前0.5 h,腹腔注射0.2 ml 3PRGD2生理盐水溶液(浓度2.5 mg/ml),并于2 h取其组织,肿瘤及其他组织使用γ计数仪检测其放射强度。结果模型小鼠的肿瘤中放射性药物含量很高,脑组织药物透过量极少;肾和膀胱放射性都很高,提示该药物可能主要经肾排泄;对照组小鼠除肾和膀胱外,其他组织的放射性均很低。结论该显像剂具有肿瘤靶向性;冷肽可竞争性地抑制99mTc-3PRGD2与整合素αvβ3受体结合。Objective To establish a quantitative analysis method for determining99 mTc-HYNIC-PEG4-E[PEG4-c（RGDf K）]2（99 mTc-3 PRGD2,a radioactive tumor agent）by γ counter, and to investigate the distribution of99 mTc-3 PRGD2 in mice bearing with lung carcinoma xenograft. Methods The mice were divided into 4 normal groups and one blocking peptide group（control group）.The99 mTc-3 PRGD2（8 μg/kg）was injected to mice bearing with lung carcinoma xenograft through the tail intravenous administration.Tissues of the normal mice were taken at 0.5,1,2 and 4 h. The control group were treated by 3 PRGD2 and99 mTc-3 PRGD2. The control mice were injected with the 3 PRGD2 saline solution（2.5 mg/ml,0.2 ml）at 0.5 h earlier before the injection of99 mTc-3 PRGD2. The tumor and organ tissues of the control mice were taken at 2 h. The radioactivity was detected by Gamma Counter. Results The radioactivity of99 mTc-3 PRGD2 detected was high in the tumor and very low in brain. In addition,high radioactivity in kidneys and bladder suggested that the drug excreted by renal. Conclusion The results proved that the blocking peptide can competitively inhibit the combination of99 mTc-3 PRGD2 and integrin αvβ3 receptors.

关 键 词：99mTc-3PRGD2 生物分布 肿瘤靶向 肺癌 

分 类 号：R965[医药卫生—药理学]