Zhang Changwei, Yuan Hua, Shen Hong, Ye Jianzhong, Wang Chengzhang
Institute of Chemical Industry of Forest Products, CAF, Nanjing, 210042, Jiangsu, China.
Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, Nanjing Forestry University, Nanjing, 210042, Jiangsu, China.
Heliyon. 2024 Jul 31;10(16):e35479. doi: 10.1016/j.heliyon.2024.e35479. eCollection 2024 Aug 30.
In this study, 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 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.
在本研究中，分别以叶聚戊烯醇（GBP）和聚吡啶金属配合物作为功能配体和主配体，成功合成了四种新型的基于GBP的聚吡啶金属配合物，并通过紫外可见分光光度计（UV-vis）、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法等系统研究了它们的细胞吸收能力、光暗稳定性、光解离效率、活性氧生成能力、光控抗菌和抗肿瘤活性及其作用机制。配合物1、2和4的脂水分配系数均在0至3范围内，表明与GBP相比，它们具有更好的细胞吸收能力和更具竞争力的生物利用度潜力。所有合成的配合物在黑暗环境中均具有优异的稳定性，除配合物1外，在可见光照射条件下均可进行配体解离。其中，配合物2和配合物4在5分钟内分别能够实现37.9%和54.4%的降解率。此外，配合物2和配合物4因其更强的活性氧生成能力，对HN-3肿瘤细胞表现出优异的抑制活性。此外，BCL-2和NF-kB p-p65的表达受限，尤其是BAX表达的促进可能是根本原因之一。与黑暗条件相比，四种合成的配合物在可见光照射条件下对[具体细菌]具有较好的抑制作用，其中配合物4最佳，其MIC和MBC值分别为6.25和12.5μg/mL。配合物4的抗菌机制可能与多种因素的协同作用有关，包括细菌内含物泄漏、细胞膜通透性改变和细胞壁破坏等。上述所有综合研究将为基于GBP的功能产品的高值开发和应用铺平道路。
