Spectroscopic and dynamic light scattering studies of the interaction between pterodontic acid and bovine serum albumin
Spectroscopic and dynamic light scattering studies of the interaction between pterodontic acid and bovine serum albumin
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DOI：
10.1016/j.apsb.2011.12.001
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发表时间：
2012-02-01
影响因子：
14.5
通讯作者：
Mei, Zhinan
中科院分区：
文献类型：
--
作者：
Li, Yunfang;Yang, Guangzhong;Mei, Zhinan
从中草药臭灵丹中分离得到一种具有抗菌活性的化合物--臭灵丹酸（PA）。为了促进其临床前的发展，PA和牛血清白蛋白（BSA）之间的相互作用进行了研究，使用荧光猝灭技术，紫外可见分光光度法和动态光散射（DLS）。在297 K和310 K，282 nm激发波长下，BSA的荧光强度随PA浓度的增加而显著降低，这是由于PA与BSA形成了复合物。计算了表观结合常数、结合位点数和相应的热力学参数，表明分子间的主要吸引力来自氢键和货车范德华力。同步荧光光谱显示，复合物中的结合位点接近色氨酸的微环境，三维荧光光谱显示结合引起BSA构象的变化。使用DLS，PA浓度的增加被证明会导致流体动力学直径的逐渐增加和复合物的显著聚集。(C)2012年中国医学科学院药物研究所、中国药学会。制作和主办Elsevier B. V.保留所有权利。
Pterodontic acid (PA) has been isolated from Laggera pterodonta, a Chinese herbal medicine, and shown to possess antibacterial activity in vitro. To facilitate its preclinical development, the interaction between PA and bovine serum albumin (BSA) was studied using a fluorescence quenching technique, ultraviolet visible spectrophotometry and dynamic light scattering (DLS). At temperatures of 297 K and 310 K and an excitation wavelength of 282 nm, the fluorescence intensity of BSA decreased significantly with increasing concentration of PA attributed to the formation of a PA BSA complex. The apparent binding constant, number of binding sites and corresponding thermodynamic parameters were calculated and the main intermolecular attraction shown to result from hydrogen bonding and van der Waals forces. Synchronous fluorescence spectrometry revealed that the binding site in the complex approached the microenvironment of Trp and three-dimensional fluorescence spectroscopy showed the binding induced conformational changes in BSA. Using DLS, increasing PA concentration was shown to cause a gradual increase in hydrodynamic diameter and significant aggregation of the complex. (C) 2012 Institute of Materia Medica, Chinese Academy of Medical Sciences and Chinese Pharmaceutical Association. Production and hosting by Elsevier B.V. All rights reserved.