摘要
目的 探讨正电子显像探针folate-NOTA-Al^18F（^18F-FNA）作为叶酸受体阳性表达的KB鼻咽癌显像剂的可行性.方法 采用氟化铝配位标记法制备^18F-FNA,考察相转移催化剂K2.2.2的加入是否可以提高标记率;取20只KB荷瘤鼠注射3.7 MBq ^18F-FNA,并分别于注射后10、30和90 min处死,取各脏器称质量并测定放射性计数,计算放射性摄取值（%ID/g）;观察生物学分布,计算肿瘤对肝脏、大脑、肺、心、骨骼、肌肉的T/NT比值.另取3只KB荷瘤鼠注射^18F-FNA后40 min行microPET/CT显像,观察肿瘤摄取情况.结果 加入K2.2.2可提高分子探针的标记率.^18F-FNA为无色澄明溶液,放射化学产率大于98%,放化纯大于99%,37 ℃保温4 h放化纯大于98%.荷瘤鼠体内生物学分布结果显示,肿瘤和肾脏摄取较高,注射后30 min的放射性摄取值分别为（1.37±0.20）与（5.12±0.58） %ID/g],KB荷瘤裸鼠microPET/CT显像示肿瘤组织对^18F-FNA明显高摄取.结论 加入K2.2.2可明显提高^18F-FNA的标记率,^18F-FNA T/NT比值较好,具有潜在应用前景.
Objective To prepare PET molecular probe folate-NOTA-Al^18F（^18F-FNA） and to explore its feasibility as an imaging agent in folate receptor positive KB tumor.Methods ^18F-FNA was prepared by the method of aluminum fluoride coordination labeling, and the effect of phase transfer catalyst K2.2.2 on the labeling yield was evaluated.Biological distribution was carried out at 10, 30 and 90 min after injection of 3.7 MBq ^18F-FNA in nude mice （n=20） xenografted with KB tumor, and the radioactive uptake （%ID/g） and T/NT ratios were then calculated in different organs or tissues.MicroPET imaging was performed at 40 min after injection of ^18F-FNA （3.7 MBq）.Results The labeling yield of ^18F-FNA increased with the presence of K2.2.2.The radiochemical yield was above 98%.The radiochemical purity was above 99%, and still above 98% after maintained in PBS and FBS at 37 ℃ for 4 h.The biodistribution showed that the blood clearance of the probe was slow, and the uptakes in kidneys and tumor which overexpressed folate receptor were significantly high （（5.12±0.58） %ID/g and （1.37±0.20） %ID/g）.The high radioactive uptake was observed in KB xenografted mice using microPET imaging.Conclusions The labeling yield of ^18F-FNA could increase with the presence of K2.2.2.Furthermore, the encouraging biological distribution and microPET imaging results indicate that ^18F-FNA may be a candidate for PET imaging in targeting folate receptor.
出处
《中华核医学与分子影像杂志》
北大核心
2017年第8期482-485,共4页
Chinese Journal of Nuclear Medicine and Molecular Imaging
基金
中国博士后科学基金（2013M532161）
广东省自然科学基金（$2013040016926）
