...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Journal of Biomolecular Structure and Dynamics >Cytotoxicity and comparative binding mechanism of piperine with human serum albumin and alpha-1-acid glycoprotein
【24h】

Cytotoxicity and comparative binding mechanism of piperine with human serum albumin and alpha-1-acid glycoprotein

机译：胡椒碱与人血清白蛋白和α-1-酸糖蛋白的细胞毒性及比较结合机制

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Human serum albumin (HSA) and alpha-1-acid glycoprotein (AGP) (acute phase protein) are the plasma proteins in blood system which transports many drugs. To understand the pharmacological importance of piperine molecule, here, we studied the anti-inflammatory activity of piperine on mouse macrophages (RAW 264.7) cell lines, which reveals that piperine caused an increase in inhibition growth of inflammated macrophages. Further, the fluorescence maximum quenching of proteins were observed upon binding of piperine to HSA and AGP through a static quenching mechanism. The binding constants obtained from fluorescence emission were found to be K-piperine = 5.7 +/-.2x10(5)M(-1) and K-piperine=9.3 +/- .25 x 10(4)M(-1) which correspond to the free energy of -7.8 and -6.71kcalM(-1)at 25 degrees C for HSA and AGP, respectively. Further, circular dichrosim studies revealed that there is a marginal change in the secondary structural content of HSA due to partial destabilization of HSA-piperine complexes. Consequently, inference drawn from the site-specific markers (phenylbutazone, site I marker) studies to identify the binding site of HSA noticed that piperine binds at site I (IIA), which was further authenticated by molecular docking and molecular dynamic (MD) studies. The binding constants and free energy corresponding to experimental and computational analysis suggest that there are hydrophobic and hydrophilic interactions when piperine binds to HSA. Additionally, the MD studies have showed that HSA-piperine complex reaches equilibration state at around 3ns, which prove that the HSA-piperine complex is stable in nature.
机译：人血清白蛋白（HSA）和α-1-酸糖蛋白（AGP）（急性期蛋白）是血液系统中的血浆蛋白，可转运多种药物。为了了解胡椒碱分子的药理重要性，在这里，我们研究了胡椒碱对小鼠巨噬细胞（RAW 264.7）细胞系的抗炎活性，这表明胡椒碱引起炎症巨噬细胞抑制生长的增加。此外，在胡椒碱通过静态猝灭机制结合到HSA和AGP上时，观察到蛋白质的荧光最大猝灭。发现从荧光发射获得的结合常数为K-胡椒碱= 5.7 +/-。2x10（5）M（-1）和K-胡椒碱= 9.3 +/- .25 x 10（4）M（-1）这分别对应于25摄氏度下HSA和AGP的-7.8和-6.71kcalM（-1）的自由能。此外，圆二色性研究显示，由于HSA-胡椒碱配合物的部分不稳定，HSA的二级结构含量有少量变化。因此，从用于鉴定HSA结合位点的位点特异性标记（苯基丁but，位点I标记）研究得出的推论发现，胡椒碱在位点I（IIA）结合，这已通过分子对接和分子动力学（MD）研究得到进一步验证。对应于实验和计算分析的结合常数和自由能表明，当胡椒碱结合HSA时，存在疏水和亲水相互作用。另外，MD研究表明，HSA-胡椒碱复合物在3ns左右达到平衡状态，这证明了HSA-胡椒碱复合物在本质上是稳定的。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号