Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Antioxidant Activity of a Novel Acetylcholinesterase Inhibitor: In Vivo and Ex vivo Studies

Version 1 : Received: 16 December 2020 / Approved: 16 December 2020 / Online: 16 December 2020 (13:45:10 CET)

How to cite: Simeonova, R.; Stavrakov, G.; Philipova, I.; Atanasova, M.; Doytchinova, I. Antioxidant Activity of a Novel Acetylcholinesterase Inhibitor: In Vivo and Ex vivo Studies. Preprints 2020, 2020120414 (doi: 10.20944/preprints202012.0414.v1). Simeonova, R.; Stavrakov, G.; Philipova, I.; Atanasova, M.; Doytchinova, I. Antioxidant Activity of a Novel Acetylcholinesterase Inhibitor: In Vivo and Ex vivo Studies. Preprints 2020, 2020120414 (doi: 10.20944/preprints202012.0414.v1).

Abstract

The acetylcholinesterase (AChE) inhibitors are the main drugs for symptomatic treatment of neurodegenerative disorders like Alzheimer’s disease. A recently designed, synthesized and tested hybrid compound between the AChE inhibitor galantamine (GAL) and the antioxidant polyphenol curcumin (CU) showed high AChE inhibition in vitro. Here, we describe tests for acute and short-term toxicity in mice as well as antioxidant tests on brain homogenates measured the levels of malondialdehide (MDA) and glutathione (GSH). Haematological and serum biochemical analyses were also performed. In the acute toxicity tests, the novel AChE inhibitor given orally in mice showed LD50 of 49 mg/kg. The short-term administration of 2.5 and 5 mg/kg did not show toxicity. In the ex vivo tests, the GAL-CU hybrid performed better than GAL and CU themselves. In a dose of 5 mg/kg, it demonstrates 25% reduction in AChE activity, 28% and 73% increase in the levels of MDA and GSH, respectively. No significant changes in blood biochemical data were observed. The GAL-CU hybrid is a novel non-toxic AChE inhibitor with high antioxidant activity which makes it a perspective multitarget drug candidate for treatment of Alzheimer’s disease.

Keywords

galantamine; curcumin; in vivo AChE inhibition; acute toxicity in mice; antioxidant activity; malondialdehide levels; glutathione levels; brain homogenate; complete blood count; biochemical serum parameters

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