槲皮素和维生素E对黑色素生成的抑制作用在文献中有广泛的报道,独立,由于渗透较少,抗氧化潜力有限,溶解度,降低生物利用度,降低了稳定性。因此,本研究的目的是合成金属离子(铜和锌)与槲皮素的新型配合物,以增强抗氧化性能,这是由对接研究证实。合成复合物的聚己内酯基纳米颗粒(PCL-NP,Q-PCL-NP,Zn-Q-PCL-NP,Cu-Q-PCL-NP)后来负载了维生素E,这使该研究在增强抗氧化剂谱方面更加有趣。纳米颗粒的zeta大小进行了表征,charge,和多分散指数,同时通过FTIR加强了纳米颗粒的理化分析。Cu-Q-PCL-NPs-E显示维生素E的最大体外释放,即,80±0.54%。在Cu-Q-PCL-NPs-E中观察到2,2-二苯基-1-吡啶酰肼的非细胞抗氧化作用为93±0.23%,与Zn-Q-PCL-NPs-E相比是两倍。密歇根癌症基金会-7(MCF-7)癌细胞系用于研究装载和卸载的纳米颗粒的抗癌和细胞抗氧化剂谱。结果表明,在6和24小时后,Cu-Q-PCL-NPs-E显示的活性氧活性为90±0.32%,其抗癌行为为89±0.64%。同样,Cu-Q-PCL-NP-E还显示黑素细胞的80±0.53%抑制和角质形成细胞的95±0.54%增加,证实了酪氨酸酶的抑制作用。最后,在未负载和维生素E负载的纳米颗粒中使用锌和铜复合物可以提供增强的抗氧化性能,抑制黑色素,可用于治疗黑色素生成疾病。
Inhibition of melanogenesis by quercetin and vitamin E is extensively reported in the literature, independently, with limitations in antioxidant potential owing to less permeation, solubility, decreased bioavailability, and reduced stability. Thus, the aim of the present study was to synthesize a novel complex of metal ions (copper and zinc) with quercetin to enhance antioxidant properties which were confirmed by docking studies. Polycaprolactone-based nanoparticles of the synthesized complex (PCL-NPs, Q-PCL-NPs, Zn-Q-PCL-NPs, Cu-Q-PCL-NPs) were made later loaded with vitamin E which made the study more interesting in enhancing antioxidant profile. Nanoparticles were characterized for zeta size, charge, and polydispersity index, while physiochemical analysis of nanoparticles was strengthened by FTIR. Cu-Q-PCL-NPs-E showed maximum in vitro release of vitamin E, i.e., 80 ± 0.54%. Non-cellular antioxidant effect by 2,2-diphenyl-1-picrylhydrazyl was observed at 93 ± 0.23% in Cu-Q-PCL-NPs-E which was twofold as compared to Zn-Q-PCL-NPs-E. Michigan Cancer Foundation-7 (MCF-7) cancer cell lines were used to investigate the anticancer and cellular antioxidant profile of loaded and unloaded nanoparticles. Results revealed reactive oxygen species activity of 90 ± 0.32% with the addition of 89 ± 0.64% of its anticancer behavior shown by Cu-Q-PCL-NPs-E after 6 and 24h. Similarly, 80 ± 0.53% inhibition of melanocyte cells and 95 ± 0.54% increase of keratinocyte cells were also shown by Cu-Q-PCL-NPs-E that confirmed the tyrosinase enzyme inhibitory effect. Conclusively, the use of zinc and copper complex in unloaded and vitamin E-loaded nanoparticles can provide enhanced antioxidant properties with inhibition of melanin, which can be used for treating diseases of melanogenesis.