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[1]梁 瑞,刘 莹,赵 倩,等.131I标记新型靶向FGF8分子探针的制备及生物活性评价[J].宁夏医科大学学报,2018,(04):389-392,407.[doi:10.16050/j.cnki.issn1674-6309.2018.04.004]
 LIANG Rui,LIU Ying,ZHAO Qian,et al.Preparation and Bioactivity Evaluation of a New 131I Labeled FGF8 Targeting Molecular Probe[J].Ningxia Medical University,2018,(04):389-392,407.[doi:10.16050/j.cnki.issn1674-6309.2018.04.004]
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131I标记新型靶向FGF8分子探针的制备及生物活性评价(PDF)
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《宁夏医科大学学报》[ISSN:1005-8486/CN:64-1029/R]

卷:
期数:
2018年04期
页码:
389-392,407
栏目:
论 著
出版日期:
2019-09-30

文章信息/Info

Title:
Preparation and Bioactivity Evaluation of a New 131I Labeled FGF8 Targeting Molecular Probe
作者:
梁 瑞1 刘 莹2 赵 倩2 庄晓青2 李 娟2
(1.宁夏医科大学,银川 750004; 2.宁夏医科大学总医院核医学科,银川 750004)
Author(s):
LIANG Rui1 LIU Ying2 ZHAO Qian2 ZHUANG Xiaoqing2 LI Juan2
(1. Ningxia Medical University,Yinchuan 750004; 2. The General Hospital of Ningxia Medical University, Yinchuan 750004)
关键词:
131IFGF8分子探针性能评价HSQAAVP
Keywords:
131 I tagFGF8 molecular probesperformance evaluationpeptide HSQAAVP
分类号:
R817.4
DOI:
10.16050/j.cnki.issn1674-6309.2018.04.004
文献标志码:
A
摘要:
目的 探索131I标记小分子多肽HSQAAVP(组氨酸-丝氨酸-谷氨酰胺-丙氨酸-缬氨酸-脯氨酸)制备的最佳条件,并研究131I-HSQAAVP在体外的稳定性及生物学活性。方法 采用氯胺-T法对多肽HSQAAVP进行131I标记,通过正交实验筛选最优标记条件。测定131I–HSQAAVP的标记率、放射化学纯度。将标记好的131I-HSQAAVP放置在室温及37℃温水浴箱内观察其稳定性。用CCK-8法检测131I-HSQAAVP对人前列腺癌细胞系LNCaP、DU145的增殖抑制率,判定131I-HSQAAVP的生物学活性。结果 最佳标记条件为室温下(25℃)在50?滋L、0.5 mol·L-1、pH 7.4 PBS缓冲液中,加入50?滋g多肽、131I 74BMq(2mCi),再加入10?滋g·?滋L-1的新鲜配制的氯胺T,震荡反应时间5min,终止反应,测得标记率可达(71.5±3.03)%。经分离纯化后,其放射化学纯度为(97.8±1.6)%。体外稳定性实验表明在体外放置24h后,其放射化学纯度仍大于90%。131I-HSQAAVP和HSQAAVP对前列腺癌细胞LNCaP、DU145增殖的抑制率差异无统计学意义(P>0.05)。结论 本研究制备的131I-HSQAAVP方法简单、高效,新分子探针131I-HSQAAVP的生物活性仍被保留,可用于进一步诊断和治疗的研究。
Abstract:
Objective To explore the best condition for the preparation of small molecular peptide HSQAAVP (histidine-Glutamine-alanine-valine proline) by 131I, and to study the stability and biological activity of 131I -HSQAAVP in vitro. Methods HSQAAVP was labeled by 131I through chloramine-T method and the best labeling condition was screened by orthogonal experiment. The labeling rate and radiochemical purity of 131I - HSQAAVP were measured. The marked 131I -HSQAAVP was placed in room temperature and 37℃ water bath to observe its stability. CCK-8 assay was used to detect the proliferation inhibition rate of 131I -HSQAAVP on human prostate cancer cell lines LNCaP and DU145,and to determine the biological activity of 131I -HSQAAVP. Results The best labeling condition is at room temperature(25℃) in 50?滋L,0.5 mol·L-1,pH 7.4 PBS buffer solution,50?滋g polypeptide,131I 74BMq(2mCi),and 10?滋g·?滋L-1 freshly prepared chloramine T were added, and reacted for 5min. After terminating reaction, the mark rate can reach(71.5±3.03)%. After separation and purification,the radiochemical purity was(97.8±1.6)%. In vitro stability experiments showed that the radiochemical purity was still >90% after placing in vitro for 24h. The inhibition rates of 131I -HSQAAVP and HSQAAVP on proliferation of prostate cancer cells LNCaP and DU145 were not statistically significant(P>0.05). Conclusion 131I babeled peptides HSQAAVP by method of chloramines-T is sample and efficientive, and the biological activity of new molecular probes 131I-HSQAAVP remains unchanged especially has not obvious damage. It can be used for diagnosion and treatment in the further experimental reseach.

参考文献/References:


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备注/Memo

备注/Memo:
收稿日期:2017-05-14
基金项目:国家自然科学基金(81460270);宁夏自然科学基金(NZ14126)
作者简介:梁瑞(1989-),女,甘肃人,在读硕士研究生,研究方向为肿瘤核医学。
通信作者:李娟(1962-),女,陕西人,主任医师,从事核医学临床工作。
更新日期/Last Update: 2018-04-30