中国药理学通报2018，Vol.34Issue(7)：934-939,6.DOI:10.3969/j.issn.1001-1978.2018.07.010
汉防己甲素衍生物HL-27对BLM解旋酶生物学特性的影响
Effects of bisbenzylisoquinoline alkaloid tetrandrine derivative HL-27 on biological properties of BLM helicase
摘要
Abstract
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.关键词
BLM642-1290解旋酶/HL-27/荧光偏振/结合活性/解链活性/ATPase活性Key words
BLM642-1290 helicase/HL-27/fluorescence polarization/binding activity/unwinding activity/AT-Pase activity分类
医药卫生引用本文复制引用
张望明,葛章文,晏文涛,潘卫东,焦彦朝,刘杰麟..汉防己甲素衍生物HL-27对BLM解旋酶生物学特性的影响[J].中国药理学通报,2018,34(7):934-939,6.基金项目
国家自然科学基金资助项目( No 81360349) （ No 81360349）
贵州省科技合作计划资助项目(No 黔科合LH字[2015]7282号) （No 黔科合LH字[2015]7282号）
