用^(99)Tc^m-MIBI在体外评价肿瘤细胞多药耐药逆转剂逆转细胞多药耐药的效果  

In Vitro Nuclear Analysis of MDR Mediated by Pgp and Usage of MDR Reversing Agents With ^(99)Tc^m-MIBI

作　　者：李娜[1] 李亚明[1] 刘云鹏[2] 刘静[2] 

机构地区：[1]中国医科大学附属第一医院核医学科,辽宁沈阳110001 [2]中国医科大学附属第一医院肿瘤内科,辽宁沈阳110001

出　　处：《同位素》2009年第1期10-13,共4页Journal of Isotopes

摘　　要：通过观察99Tcm-MIBI细胞内摄取变化探讨了单独或低剂量联合应用多药耐药逆转剂逆转肿瘤细胞多药耐药的效果,期望为进一步解决临床恶性肿瘤化疗面临的问题提供实验依据。选择人类髓系白血病K562细胞及其耐药细胞系K562/D各2×106个,分别加入8 MBq99Tcm-MIBI,观察不同时间不同浓度多药耐药逆转剂环孢菌素A(CsA0.1～0.4 mg/L)和/或维拉帕米(Ver 2.5～10 mg/L)存在时,K562细胞及K562/D细胞对99Tcm-MIBI摄取变化。结果显示:①不同浓度Ver或CsA存在时,K562细胞99Tcm-MIBI摄取略有增加,但差异无显著性(P>0.05);K562/D细胞对99Tcm-MIBI的摄取均明显增加,但不同浓度Ver间及不同浓度CsA间,摄取增加的差异没有显著性(P>0.05)。②2.5 mg/L Ver及0.1 mg/L CsA同时加入K562细胞系中,60 min时99Tcm-MIBI摄取率为0.303±0.076,增加率为183%,接近单独应用Ver(10mg/L)或单独应用CsA(0.4 mg/L)。这说明低剂量逆转剂联合应用能达到与单一较大剂量应用逆转剂相似的效果,为临床逆转Pgp介导的多药耐药提示新的信息。The value of MDR reversing agents was studied by detecting the uptake of 99Tc^m-MIBI in cells to find simple but effective methods for estimating the MDR of tumor cells and the effect of reversing agents. 2× 10^6 cells of human myelogeneous leukemia cell line K562 and its resistant subline （K562/D） were incubated with 8 MBq 99Tc^m-MIBI, with accumulating with presence of reversal agents cyclosporin A（0.1-0.4 mg/L） and/or verapamil（2.5- 10 mg/L） at various time intervals were observed. The results were as follows： ①Different concentration of verapamil or cyclosporin A significantly increased the 99 Tcm-MIBI uptake of K562 resistant subline, while the uptake of K562 cell line expressing nondetectable Pgp was not affected. ②Combination of low dose verapamil （2.5 mg/L） and cyeolsporin A （0.1 mg/L） had similar effect on 99Tc^m-MIBI accumulation with higher dose of inhibitor lonely. The results indicated that combination of lower dosages modulators may play same reverse effect with less side effects.

关 键 词：~99Tc^m-MIBI 多药耐药 P糖蛋白(Pgp) 多药耐药逆转剂 

分 类 号：R817.4[医药卫生—影像医学与核医学]