目的 研究汉防己甲素衍生物HL-27对BLM642-1290解旋酶生物学特性的影响.方法 利用荧光偏振技术研究汉防己甲素衍生物 HL-27 对 BLM642-1290解旋酶 DNA 结合活性、解链活性的影响;利用孔雀绿-磷钼酸铵比色法研究汉防己甲素衍生物HL-27对BLM642-1290解旋酶ATPase活性的影响;利用紫外吸收光谱法研究汉防己甲素衍生物HL-27对BLM642-1290解旋酶构象的影响.结果 当 HL-27 浓度达到33.34 μmol·L-1时,其对dsDNA或ssDNA与BLM642-1290解旋酶结合活性的抑制率分别为41.35% 、59.54% ;当HL-27浓度达到50 μmol·L-1时,其对BLM642-1290解旋酶解链活性的抑制率为78.68% ;当HL-27的浓度为100 μmol·L-1时,其对BLM642-1290解旋酶ATPase活性的抑制率为43.8% .结论 汉防己甲素衍生物HL-27 可以抑制BLM642-1290解旋酶的DNA结合活性、解链活性与ATPase活性.%Aim To investigate the effects of bisbenzyl-isoquinoline alkaloid tetrandrine derivative HL-27 on the biological properties of the BLM642-1290 helicase. Methods Fluorescence polarization technique was used to investigate the effects of bisbenzylisoquinoline alkaloid tetrandrine derivative HL-27 on the DNA bind-ing activity and unwinding activity of the BLM642-1290 helicase. Malachite green-phosphate ammonium molyb-date colorimetry was used to investigate the effects of HL-27 on the ATPase activity of the BLM642-1290 heli-case. Ultraviolet spectral scanning was used to investi-gate the effects of HL-27 on the conformation of the BLM642-1290 helicase. Results When the concentra-tion of HL-27 reached 33.34 μmol·L-1, the inhibi-tion ratio of dsDNA and ssDNA binding activity of the BLM642-1290 helicase was 41.35% and 59.54% , re-spectively. When the concentration of HL-27 reached 50 μmol·L-1, the inhibition ratio of DNA unwinding activity of the BLM642-1290 helicase was 78.68% . When the concentration of HL-27 reached 100 μmol· L-1, the inhibition ratio of ATPase activity of the BLM642-1290 helicase was 43.8% . Conclusion The DNA binding activity, ATPase activity and unwinding activity of the BLM642-1290 helicase can be inhibited by bisbenzylisoquinoline alkaloid tetrandrine derivative HL-27.
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