Olchowik-Grabarek Ewa, Czerkas Krzysztof, Matchanov Alimjon Davletboevich, Esanov Rahmat Sulton, Matchanov Umarbek Davlatboevich, Zamaraeva Maria, Sekowski Szymon
Laboratory of Molecular Biophysics, Department of Microbiology and Biotechnology, Faculty of Biology, University of Bialystok, 15-254 Bialystok, Poland.
Institute of Bioorganic Chemistry, Academy of Sciences of the Republic of Uzbekistan, Tashkent 100143, Uzbekistan.
J Funct Biomater. 2023 Jul 13;14(7):368. doi: 10.3390/jfb14070368.
The goal of this study is to obtain and characterize the complex of quercetin with glycyrrhizic acid, which is known to serve as a drug delivery system. Quercetin is a flavonoid with a wide range of biological activities, including an antimicrobial effect. However, quercetin instability and low bioavailability that limits its use in medical practice makes it necessary to look for new nanoformulations of it. The formation of the GAQ complex (2:1) was confirmed by using UV and FT-IR spectroscopies. It was found that the GAQ exhibited antimicrobial and antihemolytical activities against bacteria and its main virulent factor-α-hemolysin. The IC value for the antihemolytical effect of GAQ was 1.923 ± 0.255 µg/mL. Using a fluorescence method, we also showed that the GAQ bound tightly to the toxin that appears to underlie its antihemolytic activity. In addition, another mechanism of the antihemolytic activity of the GAQ against α-hemolysin was shown, namely, its ability to increase the rigidity of the outer layer of the erythrocyte membrane and thus inhibit the incorporation of α-hemolysin into the target cells, increasing their resistance to the toxin. Both of these effects of GAQ were observed at concentrations below the MIC value for growth, indicating the potential of the complex as an antivirulence agent.
本研究的目的是获得并表征槲皮素与甘草酸的复合物,已知该复合物可作为一种药物递送系统。槲皮素是一种具有广泛生物活性的黄酮类化合物,包括抗菌作用。然而,槲皮素的不稳定性和低生物利用度限制了其在医学实践中的应用,因此有必要寻找其新的纳米制剂。通过紫外光谱和傅里叶变换红外光谱证实了GAQ复合物(2:1)的形成。研究发现,GAQ对细菌及其主要致病因子α-溶血素具有抗菌和抗溶血活性。GAQ抗溶血作用的IC值为1.923±0.255μg/mL。通过荧光法,我们还表明GAQ与毒素紧密结合,这似乎是其抗溶血活性的基础。此外,还展示了GAQ对α-溶血素抗溶血活性的另一种机制,即其增加红细胞膜外层刚性的能力,从而抑制α-溶血素掺入靶细胞,增强其对毒素的抗性。GAQ的这两种作用均在低于生长的MIC值的浓度下观察到,表明该复合物作为一种抗毒力剂的潜力。