Xanthenedione Derivatives, New Promising Antioxidant and Acetylcholinesterase Inhibitor Agents

Molecules

Ana M. L. Seca¹  Stephanie B. Leal²  Diana C. G. A. Pinto²  Maria Carmo Barreto¹ 

[1] 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

关键词: xanthene-1;    9(2H)-diones;    scavenging activity;    reduction power;    acetylcholinesterase inhibitors;    xanthones;    3-cinnamoyl-5-hydroxy-2-styrylchromones;   

DOI  :  10.3390/molecules19068317

来源: mdpi

【 摘 要 】

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).

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.