光谱法研究核苷类逆转录酶抑制剂药物与DNA的相互作用  

Study on the interaction mode between nucleoside reverse transcriptase inhibitors and DNA with Fluorescence spectra

作　　者：孟彦波[1] 程艳[1] 蒋晔[2] 

机构地区：[1]邢台医学高等专科学校,河北邢台054000 [2]河北医科大学药学院,河北石家庄050017

出　　处：《华西药学杂志》2010年第3期306-308,共3页West China Journal of Pharmaceutical Sciences

摘　　要：目的研究核苷类逆转录酶抑制剂药物(阿德福韦、拉米夫定、恩去他滨)与小牛胸腺DNA(ct-DNA)的相互作用及其作用机制。方法采用荧光光谱法和热力学理论进行研究。结果确定核苷类逆转录酶抑制剂药物与ct-DNA间的猝灭过程是静态猝灭;求得27℃时,药物与ct-DNA间的结合常数(K)分别为3.41×103、2.63×103、1.02×103L·mol-1,结合位点数n分别为1.05、0.958、1.03,猝灭速率常数(Kq)分别为2.07×1011、3.50×1010、7.80×1010L·mol-1·s-1。结论核苷类逆转录酶抑制剂药物与小牛胸腺DNA间的主要作用为嵌插作用,与DNA结合的作用机制相似。OBJECTIVE To study interactions of three chosen nucleoside reverse transcriptase inhibitors（Adefovir,Lamivudine,Emtricitabine） with calf thymus DNA（ct-DNA） by fluorescence spectra.METHODS Fluorescence spectra and thermodynamic theory was adopted.RESULTS The quenching mechanism of the combination of nucleoside reverse transcriptase inhibitors with DNA was proved to be the single static quenching process.The binding constant（K） was 3.41 × 103,2.63 × 103,1.02 × 103 L·mol-1（27 ℃）respectively,binding sites n were 1.05,0.958,1.03 respectively,and quenching rate constant Kq was 2.07 × 1011,3.50 × 1010,7.80 × 1010 L·mol-1·s-1 respectively.CONCLUSION The phenomena proved that nucleoside reverse transcriptase inhibitors could intercalate into the base pairs of ct-DNA,and the mechanism is similar to the interaction between of nucleoside reverse transcriptase inhibitors and DNA.

关 键 词：阿德福韦 拉米夫定 恩去他滨 嵌插作用 小牛胸腺DNA 逆转录酶抑制剂 

分 类 号：R96[医药卫生—药理学]