5-[I-123]IODO-2'-DEOXYURIDINE IN THE RADIOTHERAPY OF AN EARLY ASCITES TUMOR-MODEL
5-[I-123]IODO-2'-DEOXYURIDINE IN THE RADIOTHERAPY OF AN EARLY ASCITES TUMOR-MODEL
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DOI：
10.1016/0360-3016(91)90331-w
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发表时间：
1991-11-01
影响因子：
7
通讯作者：
KASSIS, AI
中科院分区：
文献类型：
--
作者：
BARANOWSKAKORTYLEWICZ, J;MAKRIGIORGOS, GM;KASSIS, AI
俄歇发射体的极端生物毒性是由与衰变相关的高度局部化的能量沉积引起的。 在腹膜内（i. p.）雌性C3 HeB/FeJ小鼠中的鼠卵巢肿瘤（MOT）。 在每只小鼠腹膜内接种0.5至1.6 × 10（6）个肿瘤细胞后24、28、32、36和40小时，以5个等分部分腹膜内给予总剂量为0.37至8.88 MBq（10-240 μ Ci）（IUdR）-I-123。 对照荷瘤动物以4小时间隔注射相同体积的盐水。 生物分布研究表明，MOT细胞中（IUdR）-I-123的明显和局部摄取（最后一次注射后24小时，注射剂量的1%与MOT细胞相关），而在无肿瘤的动物中，腹膜细胞无放射性。 类似的结果，获得了腹部活动的焦点区域仅持续在MOT荷瘤小鼠，而它从腹部的对照组的图像。 对照组每只动物接种1.6 × 106个MOT细胞的50%存活率（中位存活率）为19天，而用（IUdR）-I-123处理的携带MOT的动物的中位存活率在最高给药剂量（8.88 MBq，240 μ Ci）下增加了11天，并导致7周时20%的绝对存活率。 在所有总给药剂量下均观察到统计学显著性绝对生存期延长。 用（IUdR）-I-123处理的荷瘤动物的中位和绝对存活时间的延长最终表明俄歇电子发射体碘-123的显著的放射活性。
The extreme biological toxicity of Auger emitters is caused by the decay-associated, highly localized deposition of energy. The antineoplastic capability of an Auger-electron emitter, iodine-123, incorporated into the thymidine analog, 5-iodo-2'-deoxyuridine (IUdR) was evaluated in an intraperitoneal (i.p.) murine ovarian tumor (MOT) in female C3HeB/FeJ mice. Total doses of 0.37 to 8.88 MBq (10-240-mu-Ci) (IUdR)-I-123 were administered i.p. in five equally divided fractions at 24, 28, 32, 36, and 40 hr after the i.p. inoculation of 0.5 to 1.6 x 10(6) tumor cells per mouse. Control tumor-bearing animals were injected with identical volumes of saline at 4-hr intervals. Biodistribution studies demonstrated a distinct and localized uptake of (IUdR)-I-123 in the MOT cells (1 % of the injected dose was associated with MOT cells 24 hr after the last injection), whereas in animals without tumor there was no radioactivity associated with the peritoneal cells. Analogous results were obtained from scintigraphic images where the focal area of abdominal activity persisted only in MOT-bearing mice while it cleared from the abdomen of the controls. The 50% survival (median survival) of the control group was 19 days for an inoculum of 1.6 x 10(6) MOT cells per animal, whereas the median survival of MOT-bearing animals treated with (IUdR)-I-123 increased by 11 days for the highest administered dose (8.88 MBq, 240-mu-Ci) and resulted in a 20% absolute survival at 7 weeks. Statistically significant absolute survival prolongation was found with all of the total administered doses. The prolongation of both median and absolute survival time of the tumor-bearing animals treated with (IUdR)-I-123 conclusively indicates the substantial antineoplastic activity of the Auger-electron emitter iodine-123.