Stężycka Olga, Frańska Magdalena
Institute of Chemistry and Technical Electrochemistry, Poznań University of Technology, Berdychowo 4, 60-965 Poznań, Poland.
ACS Omega. 2023 Oct 11;8(42):39816-39821. doi: 10.1021/acsomega.3c06016. eCollection 2023 Oct 24.
Recently, much interest has been devoted to finding effective G-quadruplex ligands, both of synthetic or natural origins, which may be of potential use in the field of cancer therapy. Among compounds of natural origin, a common flavonol quercetin has attracted notable attention. Yet, only a modest number of papers have been concerned with a comparison of quercetin conjugates binding to G-quadruplexes. In this study, we applied the survival yield (SY) method in order to compare the stability of G-tetrad complexes with quercetin and its conjugates, namely, 3-O-glycosides and O-methylated conjugates. According to the determined values of , flavonol glycosides bind most effectively with G-tetrads, whereas, among flavonols, 3-O-methylquercetin makes the most effective bonds. Because the aglycone structure is of crucial importance for biological processes, 3-O-methylquercetin seems to be a suitable candidate for anticancer therapeutics, and the extracts from the plants, which contain high amounts of 3-O-methylquercetin or its glycosides, should be considered as interesting materials for preparation of pharmaceuticals or dietary supplements.
最近，人们对寻找有效的G-四链体配体投入了大量关注，这些配体无论是合成的还是天然来源的，都可能在癌症治疗领域具有潜在用途。在天然来源的化合物中，常见的黄酮醇槲皮素引起了显著关注。然而，只有少数论文关注槲皮素缀合物与G-四链体结合的比较。在本研究中，我们应用存活产额（SY）方法来比较G-四联体复合物与槲皮素及其缀合物（即3-O-糖苷和O-甲基化缀合物）的稳定性。根据所确定的值，黄酮醇糖苷与G-四联体结合最有效，而在黄酮醇中，3-O-甲基槲皮素形成的键最有效。由于苷元结构对生物过程至关重要，3-O-甲基槲皮素似乎是抗癌治疗的合适候选物，并且含有大量3-O-甲基槲皮素或其糖苷的植物提取物应被视为制备药物或膳食补充剂的有趣材料。
