Interactions of arene-Ru(II)-chloroquine complexes of known antimalarial and antitumor activity with human serum albumin (HSA) and transferrin.
Interactions of arene-Ru(II)-chloroquine complexes of known antimalarial and antitumor activity with human serum albumin (HSA) and transferrin.
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DOI：
10.1016/j.jinorgbio.2010.09.005
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发表时间：
2011-01
影响因子：
3.9
通讯作者：
Sanchez-Delgado, Roberto A.
中科院分区：
文献类型：
--
作者：
Martinez, Alberto;Suarez, Javier;Shand, Tiffany;Magliozzo, Richard S.;Sanchez-Delgado, Roberto A.
采用圆二色性（CD）、紫外可见光谱和等温滴定量热法（ITC）研究了π-芳烃- ru (II)-氯喹配合物与人血清白蛋白（HSA）、转铁蛋白和全转铁蛋白的相互作用。[Ru（η - 6-对花香烃）（CQ）（H2O）Cl]PF6(1)、[Ru（η - 6-苯）（CQ）（H2O）Cl]PF6（2)、[Ru（η - 6-对花香烃）（CQ）（H2O）2][PF6]2(3)）、[Ru（η - 6-对花香烃）（CQ）（en）][PF6]2 (4)][BF4]2 （5) （CQ：氯喹；DP：二磷酸；en：乙二胺））作为对照，与CQDP和[Ru（η - 6-对花香烃）（en）Cl][PF6](6)进行比较，表明含有可交换配体的1、2、3和5以共价方式与HSA和转铁蛋白结合。相互作用不影响转铁蛋白α-螺旋结构的含量，但导致HSA中α-螺旋结构的缺失。在两种情况下，通过降低pH和在Ru-HSA加合物的情况下，也通过添加螯合剂，结合被逆转。ITC检测到配合物4和6与HSA之间的相互作用较弱，但光谱检测不到。复合物4和6与转铁蛋白或CQDP与任一蛋白均未观察到相互作用。综合结果表明，已知对耐药疟疾和几种癌细胞具有活性的芳烃- ru (II)-氯喹复合物也表现出良好的运输行为，使其成为药物开发的良好候选者。
The interactions of π-arene-Ru(II)-chloroquine complexes with human serum albumin (HSA), apotransferrin and holotransferrin have been studied by circular dichroism (CD) and UV-Visible spectroscopies, together with isothermal titration calorimetry (ITC). The data for [Ru(η6-p-cymene)(CQ)(H2O)Cl]PF6 (1), [Ru(η6-benzene)(CQ)(H2O)Cl]PF6 (2), [Ru(η6-p-cymene)(CQ)(H2O)2][PF6]2 (3), [Ru(η6-p-cymene)(CQ)(en)][PF6]2 (4), [Ru(η6-p-cymene)(η6-CQDP)][BF4]2 (5) (CQ: chloroquine; DP: diphosphate; en: ethylenediamine), in comparison with CQDP and [Ru(η6-p-cymene)(en)Cl][PF6] (6) as controls demonstrate that 1, 2, 3, and 5, which contain exchangeable ligands, bind to HSA and to apotransferrin in a covalent manner. The interaction did not affect the α-helical content in apotransferrin but resulted in a loss of this type of structure in HSA. The binding was reversed in both cases by a decrease in pH and in the case of the Ru-HSA adducts, also by addition of chelating agents. A weaker interaction between complexes 4 and 6 and HSA was measured by ITC but was not detectable spectroscopically. No interactions were observed for complexes 4 and 6 with apotransferrin or for CQDP with either protein. The combined results suggest that the arene-Ru(II)-chloroquine complexes, known to be active against resistant malaria and several lines of cancer cells, also display a good transport behavior that makes them good candidates for drug development.
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影响因子：
3
作者：
Brindell, Malgorzata;Stawoska, Iwona;van Eldik, Rudi
通讯作者：
van Eldik, Rudi
DOI：
10.1016/0020-711x(78)90110-6
发表时间：
1978-01-01
期刊：
INTERNATIONAL JOURNAL OF BIOCHEMISTRY
影响因子：
--
作者：
HRKAL, Z;KODICEK, M;MORAVEK, L
通讯作者：
MORAVEK, L
DOI：
10.1111/j.1432-1033.1974.tb03295.x
发表时间：
1974-01-01
期刊：
EUROPEAN JOURNAL OF BIOCHEMISTRY
影响因子：
--
作者：
BEAVEN, GH;CHEN, SH;GRATZER, WB
通讯作者：
GRATZER, WB
影响因子：
3
作者：
Martinez, Alberto;Rajapakse, Chandima S. K.;Jalloh, Dalanda;Dautriche, Cula;Sanchez-Delgado, Roberto A.
通讯作者：
Sanchez-Delgado, Roberto A.
影响因子：
2.9
作者：
LIN, LN;MASON, AB;BRANDTS, JF
通讯作者：
BRANDTS, JF