DCTD, University of Azores, Rua Mãe de Deus, Ponta Delgada 9501-801, Portugal.
Department of Chemistry & QOPNA, University of Aveiro, Campus de Santiago, Aveiro 3810-193, Portugal.
Molecules. 2014 Jun 19;19(6):8317-33. doi: 10.3390/molecules19068317.
Natural and synthetic xanthone derivatives are well-known for their ability to act as antioxidants and/or enzyme inhibitors. This paper aims to present a successful synthetic methodology towards xanthenedione derivatives and the study of their aromatization to xanthones. Additionally their ability to reduce Fe(III), to scavenge DPPH radicals and to inhibit AChE was evaluated. The results demonstrated that xanthenedione derivative 5e, bearing a catechol unit, showed higher reduction capacity than BHT and similar to quercetin, strong DPPH scavenging activity (EC50 = 3.79 ± 0.06 µM) and it was also showed to be a potent AChEI (IC50 = 31.0 ± 0.09 µM) when compared to galantamine (IC50 = 211.8 ± 9.5 µM).
天然和合成的黄烷酮衍生物以其作为抗氧化剂和/或酶抑制剂的能力而闻名。本文旨在介绍一种成功的黄烷酮二酮衍生物的合成方法，并研究其芳构化为黄烷酮。此外，还评估了它们还原 Fe(III)、清除 DPPH 自由基和抑制 AChE 的能力。结果表明，具有儿茶酚单元的黄烷酮二酮衍生物 5e 表现出比 BHT 更高的还原能力，与槲皮素相当，具有很强的 DPPH 清除活性（EC50 = 3.79 ± 0.06 µM），并且当与加兰他敏（IC50 = 211.8 ± 9.5 µM）相比时，它也是一种有效的 AChEI（IC50 = 31.0 ± 0.09 µM）。
