Wang Junjie, Xue Xinyue, Miao Xiaoqing
Marine College, Shandong University, Weihai 264209, China.
SDU-ANU Joint Science College, Shandong University, Weihai 264209, China.
Pharmaceuticals (Basel). 2023 Aug 25;16(9):1209. doi: 10.3390/ph16091209.
Quercetin, a flavonoid compound rich in hydroxyl groups, possesses antioxidant properties, whereas its poor water solubility limits its bioavailability. In pursuit of addressing the water solubility of quercetin and comprehending the impact of nanocrystal particle size on antioxidant efficacy, we prepared three different-sized quercetin nanocrystals, namely small (50 nm), medium (140 nm), and large (360 nm), using a nanosuspension method in this study. Within the in vitro setting, assessments employing solubility and radical scavenging assays revealed that quercetin nanocrystals displayed superior solubility (26, 21, and 13 fold corresponding to small, medium, and large particle sizes) and antioxidant performance compared to the coarse quercetin. Furthermore, quercetin nanocrystals of three particle sizes all demonstrated significant protection effects on the survival rate of HO-treated zebrafish at 72 h (77.78%, 73.33%, and 66.67% for small, medium, and large particle sizes, respectively), while the coarse quercetin group exhibited a low survival rate (53.3%) similar to the HO-treated group (47.8%). Moreover, all quercetin nanocrystals exhibited potent antioxidant capacity on both the antioxidants and enzymatic antioxidant system in HO-treated zebrafish to restore zebrafish to a normal state under oxidative stress. For instance, the levels of reactive oxygen species were reduced to 101.10%, 108.83%, and 109.77% of the normal levels for small, medium, and large particle-sized quercetin nanocrystals, respectively. In conclusion, quercetin nanocrystals demonstrated enhanced solubility, robust antioxidant capacity, and protective effects in zebrafish compared to coarse quercetin.
槲皮素是一种富含羟基的黄酮类化合物，具有抗氧化特性，但其较差的水溶性限制了其生物利用度。为了解决槲皮素的水溶性问题并理解纳米晶体粒径对抗氧化功效的影响，本研究采用纳米混悬液法制备了三种不同粒径的槲皮素纳米晶体，即小粒径（50 nm）、中粒径（140 nm）和大粒径（360 nm）。在体外环境中，通过溶解度和自由基清除试验评估发现，与粗槲皮素相比，槲皮素纳米晶体具有更高的溶解度（小、中、大粒径分别为26倍、21倍和13倍）和抗氧化性能。此外，三种粒径的槲皮素纳米晶体在72小时时均对过氧化氢处理的斑马鱼存活率表现出显著的保护作用（小、中、大粒径分别为77.78%、73.33%和66.67%），而粗槲皮素组的存活率较低（53.3%），与过氧化氢处理组（47.8%）相似。此外，所有槲皮素纳米晶体在过氧化氢处理的斑马鱼中对抗氧化剂和酶促抗氧化系统均表现出强大的抗氧化能力，使斑马鱼在氧化应激下恢复到正常状态。例如，小、中、大粒径槲皮素纳米晶体的活性氧水平分别降至正常水平的101.10%、108.83%和109.77%。总之，与粗槲皮素相比，槲皮素纳米晶体在斑马鱼中表现出增强的溶解度、强大的抗氧化能力和保护作用。
