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Synthesis and evaluation of berberine derivatives and analogues as potential anti-acetylcholinesterase and antioxidant agents

Synthesis and evaluation of berberine derivatives and analogues as potential anti-acetylcholinesterase and antioxidant agents

Roselli, Mariagrazia, Cavalluzzi, Maria Maddalena, Bruno, Claudio, Lovece, Angelo, Carocci, Alessia, Franchini, Carlo, Habtemariam, Solomon and Lentini, Giovanni (2016) Synthesis and evaluation of berberine derivatives and analogues as potential anti-acetylcholinesterase and antioxidant agents. Phytochemistry Letters, 18. pp. 150-156. ISSN 1874-3900 (Print), 1876-7486 (Online) (doi:10.1016/j.phytol.2016.10.005)

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Abstract

Two known berberine derivatives and novel N-benzyl phenethylamines as open models of berberine were synthesized and evaluated as acetylcholinesterase (AChE) inhibitors and antioxidant agents. While being less potent than the parent compound (IC50 = 0.70± 0.04 μM), both berberine derivatives performed as good AChE inhibitors (IC50 = 2.30 ± 0.29 μM and 7.8 ± 0.8 μM, respectively) and were at least 36 and four times more potent than berberine as radical scavengers. Among the synthesized compounds, demethyleneberberine bromide (2) was the most interesting because it showed both anticholinesterase and radical scavenging activities with the lowest IC50 values. As expected, catechol rings appeared as fundamental for antioxidant properties. Indeed, the most active scavenging compound in the simplified analog series was the one bearing two catechol moieties, which displayed higher potency than gallic acid.

Item Type: Article
Uncontrolled Keywords: Berberine; Acetylcholinesterase; Antioxidants; Phenethylamines; Alzheimer’s disease
Subjects: Q Science > QC Physics
Q Science > QD Chemistry
Faculty / Department / Research Group: Faculty of Engineering & Science
Faculty of Engineering & Science > Department of Pharmaceutical, Chemical & Environmental Sciences
Last Modified: 26 Oct 2017 15:27
Selected for GREAT 2016: None
Selected for GREAT 2017: None
Selected for GREAT 2018: None
URI: http://gala.gre.ac.uk/id/eprint/17598

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