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采用Iodogen法对叶酸-青霉素G酰化酶(Folate-conjugated Penicillin G Amidase,F-PGA)和PGA进行125I标记。将纯化后的标记物由尾静脉注入荷SKOV3实体瘤裸鼠体内,观察F-PGA对叶酸受体阳性的SKOV3的靶向性。结果显示:标记产品纯化后放化纯度>95%,且体内外稳定性较好;荷SKOV3肿瘤的裸鼠注射125I-F-PGA后4~24 h肿瘤显像较清晰,而注射125I-PGA组所有时相均未见明显的肿瘤部位放射性浓聚影;125I-F-PGA组的肿瘤与健侧肌肉的摄取比值(T/M)明显高于对照组(F=13.38,P=0.014 6),且在非靶组织中清除较快。表明F-PGA在荷瘤鼠体内能特异性地与叶酸受体阳性的SKOV3实体肿瘤进行靶向结合,其T/NT>1,有望用于靶向治疗。
The Iodogen method was used to label 125I with Folate-conjugated Penicillin G Amidase (F-PGA) and PGA. The purified marker was injected into SKOV3 solid tumor-bearing nude mice via the tail vein to observe the targeting of F-PGA to folate receptor-positive SKOV3. The results showed that the purity of the labeled product was> 95% after purification, and its stability in vitro and in vivo was good. The tumor imaging of the SKOV3 tumor-bearing nude mice was clear 4 ~ 24 h after 125I-F-PGA injection, while 125I-PGA There was no significant radioactive accumulation of tumor site in all the groups at all time points. The T / M ratio of tumor to contralateral muscle in 125I-F-PGA group was significantly higher than that in control group (F = 13.38, P = 0.014 6 ), And cleared faster in non-target tissues. It is indicated that F-PGA can specifically bind to folate receptor positive SKOV3 solid tumor in tumor-bearing mice. Its T / NT> 1 is expected to be used in targeted therapy.