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目的探讨大黄酸联合贺普丁对乙肝病毒逆转录酶活性的影响。方法本文采用酶抑制动力学方法 ,观察大黄酸与贺普丁对逆转录酶的抑制作用、进行大黄酸对逆转录酶的抑制动力学分析,对大黄酸联合贺普丁对逆转录酶活性抑制和对乙肝病毒合成的抑制是否具有协同效应进行探讨。结果大黄酸是一种可逆的非竞争型逆转录酶抑制剂(半抑制率IC50为39.88μmol/L,抑制常数Ki为0.122μmol/L),圆二色谱分析表明大黄酸诱导逆转录酶的构象发生部分改变,α-螺旋含量从16.4%逐渐增加到25.9%,而β-折叠含量从37.1%减小到28.8%;低浓度的贺普丁与大黄酸联合使用对乙肝病毒合成的抑制具有协同作用。结论大黄酸能够使逆转录酶活性降低;进而影响乙肝病毒DNA的合成,并能够与低浓度的贺普丁起到协同作用。
Objective To investigate the effect of rhein combined with lopudin on the activity of reverse transcriptase of hepatitis B virus. Methods In this paper, enzymatic inhibition kinetics was used to observe the inhibitory effect of rhein and hinokidine on reverse transcriptase, and the inhibitory kinetics of rhein on reverse transcriptase were analyzed. The inhibition of reverse transcriptase activity by rhein combined with streptavidin And whether inhibition of hepatitis B virus synthesis has a synergistic effect. Results Rhein was a reversible non-competitive reverse transcriptase inhibitor (IC50 was 39.88 μmol / L and the inhibition constant Ki was 0.122 μmol / L). Circular dichroism analysis showed that the conformation of rhein-induced reverse transcriptase Partially changed, the α-helix content increased gradually from 16.4% to 25.9%, while the β-sheet content decreased from 37.1% to 28.8%. The combination of low concentration of Herceptin and rhein had synergistic effect on the inhibition of hepatitis B virus synthesis effect. Conclusion Rhein can reduce the activity of reverse transcriptase, further affect the synthesis of hepatitis B virus DNA and can work synergistically with low concentrations of Lamptin.