汉防己甲素衍生物HL-22对BLM解旋酶生物学特性的影响

The Effects of Bisbenzylisoquinoline Alkaloid Tetrandrine Derivative HL-22 on the Biological Properties of the BLM Helicase

目的:探讨汉防己甲素衍生物HL-22对BLM^(642-1290)解旋酶生物学特性的影响。方法:采用荧光偏振法检测HL-22对BLM^(642-1290)解旋酶DNA结合活性和解链活性的影响,用孔雀绿-磷钼酸铵比色法检测HL-22对BLM^(642-1290)解旋酶ATPase活性的影响,采用紫外吸收光谱法检测HL-22对BLM^(642-1290)解旋酶构象的影响。结果:33.34μmol/L的HL-22对BLM解旋酶复性后双链DNA(ds DNA)结合活性的抑制率为49.07%、单链(ss DNA)结合活性的抑制率为50.00%,50μmol/L的HL-22对BLM解旋酶DNA解链活性的抑制率为93.58%,100μmol/L的HL-22对BLM解旋酶ATPase活性的抑制率为90.3%。结论:HL-22对BLM^(642-1290)解旋酶的DNA结合活性、解链活性和ATPase活性均有抑制作用。

Objective： To research the effects of bisbenzylisoquinoline alkaloid tetrandrine derivative HL-22 on the biological properties of the BLM helicase. Methods： Fluorescence polarization techniques was used to study the effects of HL-22 on the DNA binding activity and unwinding activity of the BLM helicase. Malachite green-phosphate ammonium molybdate colorimetry was used to detect the effects of HL-22 on the ATPase activity of the BLM helicase. Ultraviolet spectral scanning method was used to research the effects of HL-22 on the conformation of the BLM helicase. Results： When the concentration of HL-22 was 33. 34 μmol/L,the inhibition ratio of ds DNA binding activity and ss DNA binding activity of the BLM helicase were 49. 07% and 50. 00%; When the concentration of HL-22 was 50 μmol/L,the inhibition ratio of DNA unwinding activity of the BLM helicase was 93. 58%;When the concentration of HL-22 was 100 μmol/L,the inhibition ratio of ATPase activity of the BLM helicase was 90. 3%. Conclusions： The DNA binding activity,unwinding activity and ATPase activity of the BLM helicase were inhibited by HL-22.