Aiyelabola Temitayo, Akinkunmi Ezekiel, Ojo Isaac, Obuotor Efere, Adebajo Clement, Isabirye David
Department of Chemistry, Obafemi Awolowo University, Ile-Ife, Osun State, Nigeria.
Department of Pharmaceutics, Obafemi Awolowo University, Ile-Ife, Osun State, Nigeria.
Bioinorg Chem Appl. 2017;2017:2956145. doi: 10.1155/2017/2956145. Epub 2017 Feb 15.
Enantiomerically enriched coordination compounds of aspartic acid and racemic mixtures of coordination compounds of glycine metal-ligand ratio 1 : 3 were synthesized and characterized using infrared and UV-Vis spectrophotometric techniques and magnetic susceptibility measurements. Five of the complexes were resolved using (+)--dichlorobis(ethylenediamine)cobalt(III) chloride, (+)-bis(glycinato)(1,10-phenanthroline)cobalt(III) chloride, and (+)-tris(1,10-phenanthroline)nickel(II) chloride as resolving agents. The antimicrobial and cytotoxic activities of these complexes were then determined. The results obtained indicated that aspartic acid and glycine coordinated in a bidentate fashion. The enantiomeric purity of the compounds was in the range of 22.10-32.10%, with (+)--dichlorobis(ethylenediamine)cobalt(III) complex as the more efficient resolving agent. The resolved complexes exhibited better activity in some cases compared to the parent complexes for both biological activities. It was therefore inferred that although the increase in the lipophilicity of the complexes may assist in the permeability of the complexes through the cell membrane of the pathogens, the enantiomeric purity of the complexes is also of importance in their activity as antimicrobial and cytotoxic agents.
合成了天冬氨酸的对映体富集配位化合物以及甘氨酸金属 - 配体比例为1∶3的配位化合物外消旋混合物，并采用红外和紫外 - 可见分光光度技术以及磁化率测量对其进行了表征。使用（+） - 二氯双（乙二胺）钴（III）氯化物、（+） - 双（甘氨酸根）（1,10 - 菲咯啉）钴（III）氯化物和（+） - 三（1,10 - 菲咯啉）镍（II）氯化物作为拆分剂拆分了其中五种配合物。然后测定了这些配合物的抗菌和细胞毒性活性。所得结果表明天冬氨酸和甘氨酸以双齿方式配位。化合物的对映体纯度在22.10 - 32.10%范围内，其中（+） - 二氯双（乙二胺）钴（III）配合物是更有效的拆分剂。在某些情况下，拆分后的配合物在两种生物活性方面均比母体配合物表现出更好的活性。因此可以推断，尽管配合物亲脂性的增加可能有助于配合物透过病原体的细胞膜，但配合物的对映体纯度在其作为抗菌和细胞毒性剂的活性中也很重要。
