摘要
目的:合成新化合物N-[3-(3-吡啶基)丙烯酰基]-2-氨基丁酸并观察其对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: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20%细胞死亡所需药物浓度(IC20)为1.66mmol/L,乏氧条件下IC20为1.32mmol/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。
Objective： To study the toxicity and radiosensitizing effect of N-[3-（3-pyridyl） acryl]-2-aminobutyric acid on hyperoxic and hypoxic HeLa cells.Methods： N-[3-（3-pyridyl） acryl]-2-aminobutyric acid was synthesized from 3-pyridylacrylic acid and 2-aminobutyric acid ethyl ester hydrochloride.The survival rate and IC20 of the compound were determined by MTT assay.The sensitizing enhancement ratio （SER） was measured using colony formation test.Results： N-[3-（3-pyridyl） acryl]-2-aminobutyric acid was synthesized for the first time,and the total yield was 78%.The result of MTT assay showed that IC20 of the compound was 1.66 mmol/L and 1.32 mmol/L in hyperoxic and hypoxic HeLa cells.The values of SER were 1.44 and 1.84 in hyperoxic and hypoxic HeLa cells measured by colony formation test.Conclusion： N-[3-（3-pyridyl） acryl]-2-aminobutyric acid is easily synthesized,and with lower cytotoxicity and radiosensitizing effect on HeLa cells.
出处
《天津医药》
CAS
北大核心
2011年第2期153-155,共3页
Tianjin Medical Journal
基金
天津市自然科学基金资助项目(项目编号：08JCYBJC07400)
