Life Sciences (2020)
Update date:2022-08-29
Topics:
Dutra, Rafael Cypriano
Goliatt, Priscila Vanessa Zabala Capriles
Marion, Gabriel Macedo
Meinel, Raissa Soares
Nunes, Vinicius Schmitz Pereira
da Silva, Adilson David
Fávero, Amanda
Menegasso, Jaíne Ferrareis
Raposo, Nádia Rezende Barbosa
de Assis, Pollyana Mendon?a
Inflammaging is known as an imbalance between pro-inflammatory and anti-inflammatory immune mechanisms, being related to the onset of neurological disorders, such as major depression and Alzheimer's disease. Considering the known disadvantages regarding the FDA approved drug to manage such illnesses, resveratrol emerges as a natural drug candidate, despite its low bioavailability. In this study, resveratrol analogues were evaluated for their capacity of inhibiting acetylcholinesterase in silico, in vitro, and in vivo. Molecular docking simulations pointed out RSVA1 and RSVA6 as potent inhibitors, even more than resveratrol. Ellman's assay demonstrated RSVA6 as capable of inhibiting 92.4% of the enzyme activity. Further, male Swiss mice were pretreated with RSVA6 (100 mg kg?1) 60 min before receiving scopolamine (1 mg kg?1). The Novel Recognition Object (NOR), Object Location (OLT), and Buried Pellet tests (BPL) demonstrated an RSVA6 neuroprotective effect. In the second round of tests, mice received a single intraperitoneal injection of lipopolysaccharide (0.5 mg kg?1) 24 h before treatment with RSVA6 (1, 10, and 100 mg kg?1). The Open Field (OFT), Tail Suspension (TST), and Splash tests (ST) were evaluated. LPS had no significant effect on the crossing and rearing number, indicating an association between the immobility time and anhedonia observed in the TST and ST, respectively, with depressive-like behavior. RSVA6 significantly reduced the depressive-like behavior triggered by LPS in the TST and ST. Altogether, our data suggest RSVA6 as a potential drug candidate for the treatment of neuroinflammatory conditions.
View MoreZhejiang Golden-Shell Pharmaceutical Co.,Ltd.
Contact:+86-576-87501888 / 87501988
Address:No.89 Zhongxing Road. Li'ao, Yuhuan, Zhejiang, China
Hangzhou Haiqiang Chemical Co.,Ltd.
Contact:+86-571-86960370
Address:Add: 5/F, Around Town North Road,No. 10, Hangzhou, Zhejiang,China
Quzhou Ruiyuan chemical Co., Ltd
Contact:+86-570-3039321/3039361/3039308
Address:18# Huayang Road,Quzhou High-tech Industrial Park, Zhejiang China.
puyang hongda shengdao new material co.,ltd.
Contact:+86-393- 4896278
Address:No.29 East Zhongyuan Road
Contact:+86-27-67841589
Address:Add: 999 Gaoxin Road, Donghu New Technology Development Zone, Wuhan City, Hubei, China
Doi:10.1021/ja01121a026
(1952)Doi:10.1021/jo00873a030
(1976)Doi:10.1246/bcsj.60.420
(1987)Doi:10.1016/j.tet.2010.04.054
(2010)Doi:10.1002/jps.2600570644
(1968)Doi:10.1021/jo00881a037
(1976)