摘要
目的 研究体外苯甲酸雌二醇对大肠杆菌RecQ解旋酶生物学活性的影响及作用机制。方法 运用荧光偏振技术和ATPase检测技术分析苯甲酸雌二醇对大肠杆菌RecQ解旋酶活性、DNA结合活性和ATPase活性的影响。结果 苯甲酸雌二醇对RecQ解旋酶活性、DNA结合活性及ATPase活性均有弱抑制作用,对RecQ解旋酶活性抑制常数Ki为5×10-3 nmol·L-1,对dsDNA和ssDNA结合活性的Ki分别为5×10-2和0.5 nmol·L-1。结论 在体外苯甲酸雌二醇对大肠杆菌RecQ解旋酶生物学活性具有弱抑制作用,二者至少有两个作用位点。
Abstract
OBJECTIVE To study the effects of estradiol benzoate on the bioactivity of Escherichia coli RecQ helicase in vitro and the molecular mechanisms. METHODS The helicase activity, DNA binding activity, and ATPase activity of E.coli RecQ helicase were determined by fluorescence polarization and PiColorLock Gold reagent. RESULTS The helicase activity, DNA binding activity and ATPase activity were weakly inhibited by estradiol benzoate. The inhibition constants (Ki) for the helicase activity was 5×10-3 nmol·L-1. The Ki for DNA binding activity was 5×10-2 nmol·L-1 when the substrate was dsDNA, and 0.5 nmol·L-1 when the substrate was ssDNA.CONCLUSION The biological activity of E.coli RecQ helicase is weakly inhibited by estradiol benzoate in vitro. There are at least two binding sites between them.
关键词
苯甲酸雌二醇 /
RecQ解旋酶 /
解旋酶活性 /
DNA结合活性 /
ATPase活性
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Key words
estradiol benzoate /
RecQ helicase /
helicase activity /
DNA binding activity /
ATPase activity
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段丽霞 许厚强 陈祥 c 骆衡 c .
苯甲酸雌二醇对大肠杆菌RecQ解旋酶生物学活性的影响[J]. 中国药学杂志, 2011, 46(15): 1146-1149
DUN Li-xi;XU Hou-qing;CHEN Xing;c;LUO Heng;c.
Effects of Estradiol Benzoate on the Bioactivity of Escherichia coli RecQ Helicase[J]. Chinese Pharmaceutical Journal, 2011, 46(15): 1146-1149
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参考文献
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脚注
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