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[二乙烯三胺五乙酸钙对肿瘤亲和性金属配合物生物行为的影响]

[The effect of Ca-diethylenetriamine pentaacetate on the bio-behavior of tumor-affine metal complexes].

作者信息

Schomäcker K, Franke W G, Jantsch K, Shukla S K, Limouris G S

机构信息

Klinik und Poliklinik für Nuklearmedizin, Universität zu Köln, FRG.

出版信息

Nuklearmedizin. 1992 Dec;31(6):242-8.

PMID:1491964
Abstract

The complexon CaDTPA was injected into tumour-bearing mice in concentrations of 0.05, 0.1, 0.3, and 0.6 mole/l (pH:6) 30 min after the 169Yb-injection. 100 microliters of a 0.3 M CaDTPA solution were injected at different time points (simultaneously, 2, 5, 10, 20, 30, 40 and 50 min, 1, 1.25, 1.5, 2.5 and 10 h) after 169Yb-citrate injection. The animals were killed 24 h after radionuclide administration. A strong radioactivity decrease was observable 24 h p.i. not only in blood, liver, spleen, muscle and bone but also in the tumour if CaDTPA was administered within the first 2 h after ytterbium injection. Thereafter no change in radioactivity could be achieved by DTPA. A time phase in which the Yb could be eliminated from the tissues by means of DTPA (time intervals < 2 h) was distinguishable from a time phase in which it was not attainable for DTPA (time intervals > 5 h). This indicates that the incorporation of Yb into the cells is completed after 5 h and that the metals are intracellularly bound, probably to the lysosomes. Improvements of the scintigraphic tumour detection cannot be expected from the use of complexons.

摘要

在注射¹⁶⁹Yb后30分钟,将不同浓度(0.05、0.1、0.3和0.6摩尔/升,pH值为6)的CaDTPA络合剂注入荷瘤小鼠体内。在注射¹⁶⁹Yb柠檬酸盐后的不同时间点(同时、2、5、10、20、30、40和50分钟,1、1.25、1.5、2.5和10小时)注射100微升0.3M的CaDTPA溶液。在给予放射性核素24小时后处死动物。如果在注射镱后的前2小时内给予CaDTPA,在注射后24小时可观察到血液、肝脏、脾脏、肌肉和骨骼以及肿瘤中的放射性显著降低。此后,DTPA无法使放射性发生变化。通过DTPA可以从组织中清除镱的时间段(时间间隔<2小时)与DTPA无法清除镱的时间段(时间间隔>5小时)是可区分的。这表明镱在5小时后完成了向细胞内的掺入,并且金属在细胞内结合,可能是与溶酶体结合。使用络合剂无法预期改善肿瘤的闪烁显像检测效果。

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