贵州医科大学学报

2018, v.43;No.212(05) 497-502+507

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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

张望明;葛章文;刘金河;晏文涛;潘卫东;焦彦朝;刘杰麟;
ZHANG Wangming;GE Zhangwen;LIU Jinhe;YAN Wentao;PAN Weidong;JIAO Yanchao;LIU Jielin;The First Affiliated Hospital of Guiyang College of Traditional Chinese Medicine;Laboratory of Tissue Engineering and Stem Cell,Guizhou Medical University;Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences;Guizhou Entry-exit Inspection and Quarantine Bureau;Department of Immunology,Guizhou Medical University;

摘要(Abstract):

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.

关键词(KeyWords): 汉防己甲素衍生物;BLM解旋酶;结合活性;解链活性;ATPase活性
tetrandrine derivative;BLM helicase;binding activity;unwinding activity;ATPase activity

Abstract:

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基金项目(Foundation): 国家自然科学基金项目(81360349,81360479);; 贵州省科技合作计划项目[黔科合LH字(2015)7282号]

作者(Author): 张望明;葛章文;刘金河;晏文涛;潘卫东;焦彦朝;刘杰麟;
ZHANG Wangming;GE Zhangwen;LIU Jinhe;YAN Wentao;PAN Weidong;JIAO Yanchao;LIU Jielin;The First Affiliated Hospital of Guiyang College of Traditional Chinese Medicine;Laboratory of Tissue Engineering and Stem Cell,Guizhou Medical University;Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences;Guizhou Entry-exit Inspection and Quarantine Bureau;Department of Immunology,Guizhou Medical University;

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DOI: 10.19367/j.cnki.1000-2707.2018.05.001

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