在这项研究中,银杏叶聚戊烯醇(GBP)和聚吡啶金属配合物分别用作功能配体和主配体,成功合成了四种新型的基于GBP的聚吡啶金属配合物,明暗稳定性,光解离效率,ROS生产能力,通过紫外可见分光光度计(UV-vis)系统研究了光控抗菌和抗肿瘤活性及其机制,共聚焦激光扫描显微镜(CLSM),凝胶电泳(GE),扫描电子显微镜(SEM),牛津杯法,MTT方法等.复合物1、2和4的脂水分布系数均在0~3范围内,与GBP相比,具有更好的细胞吸收能力和更高的生物利用度潜力。所有合成的配合物在黑暗环境中都具有优异的稳定性,除配合物1外,均能在可见光照射条件下进行配体解离。其中,复合物2和复合物4能够在5分钟内达到37.9%和54.4%的降解率,分开。此外,复合物2和复合物4由于其更强的ROS生产能力而对HN-3肿瘤细胞表现出优异的抑制活性。此外,BCL-2和NF-kBp-p65的表达抑制,尤其是BAX的表达促进可能是根本原因之一。4种合成的配合物在可见光照射条件下对金黄色葡萄球菌有较好的抑制作用,其中配合物4最好,其MIC和MBC值分别为6.25和12.5μg/mL,分别。复合物4的抗菌机制可能与多种因素的协同作用有关,包括细菌内含物的泄漏,细胞膜通透性的改变和细胞壁的破坏等。所有这些研究都将为基于GBP的功能产品的高价值开发和应用铺平道路。
In this study, Ginkgo biloba leave polyprenols (GBP) and polypyridine metal complex were individually utilized as functional ligand and main ligand, four kinds of novel GBP-based polypyridine metal complexes were successfully synthesized and their cell absorption capacity, light-dark stability, photodissociation efficiency, ROS production capacity, light-controlled antibacterial and anti-tumor activities as well as mechanisms were systematically investigated by ultraviolet visible spectrophotometer (UV-vis), confocal laser scanning microscope (CLSM), gel electrophoresis (GE), scanning electron microscope (SEM), oxford cup method, MTT method etc. The lipid water distribution coefficients of complex 1, 2 and 4 were all within the range of 0∼3, demonstrating their better cell absorption capacity and more competitive bioavailability potentiality compared with GBP. All of the synthesized complexes possessed excellent stability in a dark environment, and could conduct ligand dissociation under the condition of visible light irradiation except complex 1. In which, complex 2 and complex 4 were able to achieve degradation rates of 37.9 % and 54.4 % within 5 min, separately. In addition, complex 2 and complex 4 exhibited superior inhibitory activities on the HN-3 tumor cells on account of their stronger ROS production capacity. Moreover, the constricted expression of BCL-2 and NF-kB p-p65, especially the promoted expression of BAX may be one of the root cause. The four synthesized complexes had preferable inhibition effects against S. aureus under the condition of visible light irradiation in contrast to darkness, in which complex 4 was the best and its MIC and MBC values were 6.25 and 12.5 μg/mL, respectively. The antibacterial mechanism of the complex 4 may be in relation to the synergistic effect of multiple factors, including leakage of bacterial inclusion, change of cell membrane permeability and disruption of cell wall etc. All of the above generalized researches will pave a way for the high-value development and application of GBP-based functional products.