检索结果-南通市图书馆

C0818,a novel curcumin derivative,interacts with Hsp90 and inhibits Hsp90 ATPase activity

Acta Pharmaceutica Sinica B 2017年第1期7卷 91-96页

作者： Yingjuan Fan Yang Liu Lianru Zhang Fang Cai Liping Zhu Jianhua Xu School of Pharmacy Fujian Medical UniversityFuzhou 350108China Fuijan Provincial Key Laboratory of Natural Medicine Pharmacology Fuzhou 350108China School of Life Science Xiameng UniversityXiamen 361005China

The aims of the present study were to estimate the affinity between 3,5-(E)-bis(3-methoxy-4-hydroxybenzal)-4-piperidinone hydrochloride(C0818) and heat shock protein 90 (Hsp90) and to investigate the inhibitory effects of this compound on Hsp90 ATPase activity. Fluorescence spectroscopy was used to examine the affinity between varying concentrations of C0818 and Hsp90, N-Hsp90, MHsp90 and C-Hsp90. Fluorescence intensities were recorded in the range of 290–510 nm at 293, 303 and 310 K, respectively. A colorimetric assay for inorganic phosphate(based on the formation of a phosphomolybdate complex and the subsequent reaction with malachite green) were used to examine the inhibitory effects of C0818 on Hsp90 ATPase activity. The equilibrium dissociation constant K_D value of C0818 was found to be 23.41270.943 μmol/L. The interaction between C0818 and Hsp90 was driven mainly by electrostatic interactions. C0818 showed the strongest affinity with C-Hsp90. These results conclusively demonstrate the inhibitory activity of C0818 on the activity of Hsp90 ATPase.

关键词： curcumin derivative Hsp90 ATPase activity Fluorescence spectrometry Interaction

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Fluorescence spectroscopy for interaction between diacetyl curcumin and bovine serum albumin

Fluorescence spectroscopy for interaction between diacetyl c...

引用

河南省化学会2016年学术年会

作者： Dai Zeng Yue Hua Ai-ping Xing Huai-xia Yang College of Pharmacy Henan University of Chinese Medicine

In this work, we synthesized a curcumin derivative: diacetyl curcumin. The structure of diacetyl curcumin was characterized by FT-IR and ’H-NMR. The interaction between diacetyl curcumin and bovine serum slbumin was investigated by fluorescence spectroscopy under physiological conditions. The Stern-Volmer analysis indicated that the interaction resulted in the endogenous fluorescence quenching of bovine serum albumin, which belonged to a static quenching mechanism. The binding site number(n) was 0.95 and the binding constant(K b) was 7.38×10 L/mol at 308 K between diacetyl curcumin and BSA, respectively. The corresponding thermodynamic parameters ΔH, ΔS, and ΔG were calculated at 298 K and 308 K. According to the theoretical and experimental results, hydrophobic interaction was found to play major role in the binding reaction. Furthermore, synchronous fluorescence spectra indicated that the conformation of BSA was changed.The investigation of the interaction mechanism between diacetyl curcumin and BSA is of great importance to understand the general rule of their interaction and shows great reference value to the design of new drugs as well.

关键词： curcumin derivative bovine serum albumin（BSA） fluorescence spectroscopy

来源： cnki会议评论

在线全文

cnki会议

学校读者我要写书评

暂无评论

欢迎您,

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

在线全文

请选择保存的检索档案：

请选择收藏分类：

通借通还

欢迎您,

建议与咨询 留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

在线全文

请选择保存的检索档案： 新增检索档案 确定 取消

请选择收藏分类： 新增自定义分类 确定 取消

通借通还

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

请选择保存的检索档案：

请选择收藏分类：