[1]何燕,苏晋,郑晓霞,等.P-糖蛋白抑制剂在PET显像中的应用研究[J].国际放射医学核医学杂志,2016,40(1):1-5,21.[doi:10.3760/cma.j.issn.1673-4114.2016.01.001]
　He Yan,Su Jin,ZhengXiaoxia,et al.Developing P-glycoprotein inhibitor marked by PET[J].International Journal of Radiation Medicine and Nuclear Medicine,2016,40(1):1-5,21.[doi:10.3760/cma.j.issn.1673-4114.2016.01.001]
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P-糖蛋白抑制剂在PET显像中的应用研究(/HTML)
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《国际放射医学核医学杂志》[ISSN:1673-4114/CN:12-1381/R]

卷:
40
期数:
2016年第1期
页码:
1-5,21
栏目:
出版日期:
2016-01-25

文章信息/Info

Title:
Developing P-glycoprotein inhibitor marked by PET
作者:
何燕;  苏晋;  郑晓霞;  温莉;  孙树兰
251700, 山东省滨州市中心医院放射科
Author(s):
He Yan;  Su Jin;  ZhengXiaoxia;  Wen Li;  Sun Shulan
Department of Radiology, Binzhou City Center Hospital of Shandong Province, Binzhou 251700, China
关键词:
P-糖蛋白; 肿瘤; 正电子发射断层显像术; 乳腺癌耐药蛋白
Keywords:
P-glycoprotein; Neoplasms; Positron-emission tomography; Breast cancer resistance protein
DOI:
10.3760/cma.j.issn.1673-4114.2016.01.001
摘要:
目的 探讨11C-GF120918作为PET显像探针对人体P-糖蛋白(P-gp)和乳腺癌耐药蛋白(BCRP)功能的检测及其意义。方法 化学合成11C-GF120918;给小鼠注射11C-GF120918,使用自动伽玛粒子计数管测定不同时间、不同剂量、小鼠各组织器官中11C-GF120918的放射性强度;并使用高效液相色谱监测30 min后小鼠脑部和血液中11C-GF120918代谢情况;P-gp基因敲除组、BCRP基因敲除组、P-gp/BCRP基因敲除组和野生型对照组小鼠分别注射11C-GF120918,进行PET显像,实时监测小鼠大脑中的11C-GF120918放射强度变化。结果 11C-GF120918在小鼠各个组织器官中均有广泛分布,相对于正常小鼠差异有统计学意义(χ2=8.14,P<0.05);且>11C-GF120918代谢稳定,注射后30 min,在大脑和血液中仍有(99.3±0.5)%和(83.2±3.5)%未被代谢,具有较好的生物化学稳定性和辐射稳定性。P-gp/BCRP基因敲除组小鼠大脑中11C-GF120918放射性强度是野生型对照组的9倍(χ2=7.69,P<0.05),而bcrp基因敲除组小鼠大脑中放射性强度是野生型对照组的3倍(>χ2=8.24,P<0.05),差异有统计学意义。且>11C-GF120918标记效果比较稳定。结论 使用11C-GF120918作为PET显像探针可以用来评价P-gp和BCRP的耐药功能。
Abstract:
Objective To explore a PET probe,11C-GF120918 in the assessing of the function and significance of P-glycoprotein(P-gp) and breast cancer resistance protein(BCRP).Methods The mice were injected with chemically synthesized 11C-GF120918.An automatic gamma counter was used to measure the 11C-GF120918 radiation intensity of the various organs of the mice at different times and dosages.Simultaneously,HPLC was employed to detect the metabolism of 11C-GF120918 in the brain and blood of the mice.The four mice groups,namely,P-gp knockdown mice,BCRP knockdown mice,P-gp/BCRP knockdown mice,and wild mice,were manually injected with 11C-GF120918.The radiation intensity of 11C-GF120918 in the mice brain was detected by PET.Results After the 11C-GF120918 injection,the tissues and organs of mice were more widely distributed compared with those of the wild mice(χ2=8.14,P<0.05).thirty minutes="" after="" injection,the="">11C-GF120918 radiation intensity in the brain and blood were still(99.3±0.5)% and(83.2±3.5)%,respectively,with better biochemistry and radiation stability.In PET studies,AUCbrain[0~60 min] in the P-gp knockout mice was nine times higher than that in the wild group(χ2=7.69,P<0.05).the aucbrain[0-60 min] of the BCPR knockout mice was three times higher than that in the wild group(χ2=8.24,P<0.05).the evident="" effect="" of="">11C-GF120918 was relatively stable.Conclusion 11C-GF120918 can be used as PET probes to evaluate the multi-drug resistance of P-gp and BCRP.

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备注/Memo

备注/Memo:
收稿日期:2015-04-05;改回日期:。
通讯作者:何燕
更新日期/Last Update: 1900-01-01