Abstract

In the current study, via using the mixed-ligand synthesis approach, a new Co(II)-bearing coordination polymer (CP) [Co₃(biimb)(BPDC)₃(H₂O)]·2DMF·H₂O (1) has been successfully prepared by reaction of 1,3-bis(1-imidazolyl)-5-(imidazol-1-ylmethyl)benzene (biimb) and biphenyl-4,4’-dicarboxylic acid (H₂BPDC) with Co(II) salt in a mixed solvent of DMF and CH₃CN. The biological activity of the new compound was evaluated and the mechanism of the compound was revealed. Firstly, the diluted micro-plates assay was conducted and the colony-forming units (CFU) numbers of the Candida albicans after the compound treatment was determined. Besides, the enzyme-linked immunosorbent assay (ELISA) detection kit was also carried out and the levels of inflammatory cytokines released into the vaginal discharge was measured. The compound exhibited excellent treatment activity on vulvovaginal candidiasis through reducing Candida albicans growth. Simulation results suggest that only the diphenic acid functional group has activities to the active sites on the target protein, however, the iminazole group doesn’t have activities.

摘要

在目前的研究中，通过使用混合配体合成方法，一种新的含 Co(II) 的配位聚合物 (CP) [Co ₃ (biimb)(BPDC) ₃ (H ₂ O)]·2DMF·H ₂ O ( 1 ) 已通过 1,3-双(1-咪唑基)-5-(咪唑-1-基甲基)苯 (biimb) 和联苯-4,4'-二羧酸 (H ₂ BPDC) 与 Co反应成功制备(II) DMF和CH ₃混合溶剂中的盐CN. 评价了新化合物的生物活性并揭示了该化合物的作用机制。首先，进行稀释的微孔板测定并测定化合物处理后白色念珠菌的菌落形成单位(CFU)数。此外，还进行了酶联免疫吸附试验（ELISA）检测试剂盒，并测量了释放到阴道分泌物中的炎性细胞因子水平。该化合物通过减少白色念珠菌的生长，对外阴阴道念珠菌病表现出优异的治疗活性。模拟结果表明，只有地苯酸官能团对目标蛋白的活性位点有活性，而咪唑基没有活性。