Tomecková Vladimíra, Perjési Pál, Guzy Juraj, Kusnír Jaroslav, Chovanová Zuzana, Chavková Zenóbia, Mareková Mária
Department of Medical Chemistry, Biochemistry and Clinical Biochemistry, Faculty of Medicine UPJS, Trieda SNP 1, Kosice, Slovakia.
J Biochem Biophys Methods. 2004 Oct 29;61(1-2):135-41. doi: 10.1016/j.jbbm.2004.04.010.
Effect on mitochondrial outer membrane of six selected synthetic cyclic chalcone analogues, E-2-arylmethylene-1-tetralones (2) and E-2-arylmethylene-1-benzosuberones (3), were investigated by fluorescence spectroscopy. The selected compounds represent derivatives with different degree of cytotoxicity against murine and human cancer lines. Excitation and emission fluorescence spectra of the cyclic chalcone analogues 2 and 3 were recorded in respiration medium containing 1 mM succinate. It was found that the ring size as well as the nature and location of the aromatic substituents have significant effect on fluorescence of the compounds. Interaction of subtoxic concentration of compounds 2 and 3 with the outer mitochondrial membrane was investigated by recording their fluorescence polarization in the presence of rat liver mitochondria. The most cytotoxic E-2-(4'-methoxybenzylidene)-1-benzosuberone (3b) was found to display a continuous increase of fluorescence polarization signal in the presence of mitochondria--a different pattern of interaction with the mitochondrial outer membrane from that observed for rest of the investigated compounds.
通过荧光光谱法研究了六种选定的合成环状查耳酮类似物，即E-2-芳基亚甲基-1-四氢萘酮（2）和E-2-芳基亚甲基-1-苯并环庚酮（3）对线粒体外膜的影响。所选化合物代表了对小鼠和人类癌细胞系具有不同细胞毒性程度的衍生物。在含有1 mM琥珀酸的呼吸培养基中记录了环状查耳酮类似物2和3的激发和发射荧光光谱。发现环的大小以及芳族取代基的性质和位置对化合物的荧光有显著影响。通过记录化合物2和3的亚毒性浓度在大鼠肝线粒体存在下的荧光偏振，研究了它们与线粒体外膜的相互作用。发现细胞毒性最强的E-2-（4'-甲氧基亚苄基）-1-苯并环庚酮（3b）在有线粒体存在时荧光偏振信号持续增加，这与其他研究化合物与线粒体外膜相互作用的模式不同。
