吡啶丙烯酸衍生物的合成及放射增敏作用的研究

吡啶丙烯酸衍生物的合成及放射增敏作用的研究

李宁¹,周晓靓¹,施培基²,王浩¹,王荣先³

1. 北京协和医学院中国医学科学院放射医学研究所
2. 天津放射医学研究所
3. 中国医学科学院放射医学研究所

收稿日期:2010-08-25 修回日期:2010-10-25 出版日期:2011-02-15 发布日期:2011-02-15
通讯作者: 周晓靓

Study of synthesis and radiosensitizing effect of pyridylacryl acid derivative

Received:2010-08-25 Revised:2010-10-25 Published:2011-02-15 Online:2011-02-15

李宁1 ,周晓靓1 ,施培基2 ,王浩1 ,王荣先3 . 吡啶丙烯酸衍生物的合成及放射增敏作用的研究[J]. .

摘要/Abstract

摘要： 目的：合成新化合物 N-(3-(3-吡啶基)丙烯酰基)-2-氨基丁酸并研究其对Hela 细胞在有氧和乏氧条件下的毒性及放射增敏作用。方法：以 3-吡啶丙烯酸和2-氨基丁酸乙酯盐酸盐为原料合成出 N-(3-(3-吡啶基)丙烯酰基)-2-氨基丁酸，用噻唑蓝比色法（MTT实验）测定不同浓度化合物的细胞存活分数及其 20%抑制浓度，运用集落形成实验测定放射增敏比。结果：首次合成出 N-(3-(3-吡啶基)丙烯酰基)-2-氨基丁酸，总收率为 78%，MTT 实验测得其对有氧条件下 Hela 细胞的 IC20 是 1.66 mmol/L，乏氧条件下 IC20 为 1.32 mmol/L，通过集落形成实验得到有氧放射增敏比为 1.44，乏氧放射增敏比为 1.84。结论：N-(3-(3-吡啶基)丙烯酰基)-2-氨基丁酸合成方法简便，对体外 Hela 细胞毒性较小，具有一定的放射增敏作用。

关键词: 3-吡啶丙烯酸衍生物, 放射增敏, 集落形成实验

Abstract: Objective:To study the toxicity and radiosensitizing effect of N-(3-(3-pyridyl)acryl)-2-aminobutyric acid on hyperoxic and hypoxic Hela cells. Methods:Synthesized N-(3-(3-pyridyl)acryl)-2-aminobutyric acid with 3-pyridylacrylic acid and 2-aminobutyric acid ethyl ester hydrochloride. The survival rate and IC20 of the compound was determined by MTT assay. Sensitizing enhancement ratio(SER) was measured using colony formation test. Result:N-(3-(3-pyridyl)acryl)-2-aminobutyric acid was synthesized for the first time, the total yield was 78%. IC20 of the compound on hyperoxic and hypoxic Hela cells was 1.66 mmol/L and 1.32 mmol/L separately measured by MTT assay and SER was 1.44 and 1.84 separately by colony formation test. Conclusion:N-(3-(3-pyridyl)acryl)-2-aminobutyric acid is easy synthesized and with low cytotoxicity and radiosensitizing effect on Hela cells.

Key words: 3-pyridylacryl acid derivative, radiosensitization, colony formation test