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Natural and synthetic drugs used for the treatment of the dementia.
Biochem Biophys Res Commun
April 2020
Institute of Petrochemistry and Catalysis, Russian Academy of Sciences, Ufa, 450075, Russia. Electronic address:
This review is devoted to comparative pharmacological analysis of synthetic drugs such as memantine and its isomers, as well as tacrine, velnacrine, rivastigmine, and donepezil, with natural alkaloids, terpenoids, and triterpenoid peroxides, which are used to treat dementia, Alzheimer's and Parkinson's diseases, myasthenia gravis and other neurodegenerative diseases. Recently discovered by French scientists from Marseille triterpenoid hydroperoxides demonstrate high activity as potential therapeutic agents for the treatment of dementia. The information presented in this review is of great interest to pharmacologists, medical chemists, physiologists, neurologists and doctors, as well as for the pharmaceutical industry.
View Article and Find Full Text PDFEffects of acetylcholine on an animal mode of inflammation.
Clin Hemorheol Microcirc
May 2013
Institute of Biochemistry, Institute of Molecular Medicine, University of Lisbon Medical School, Lisbon, Portugal.
Acetylcholinesterase (AChE) is found both on the membranes of neuronal and non-neuronal cells. In this study we performed intravenous administrations of velnacrine (VLN) and acetylcholine (ACh), respectively, AChE inhibitor and substrate, in an animal model of lipopolysaccharide (LPS)-induced inflammation in Wistar rats. Using intravital microscopy the number of rolling and adherent leukocytes in post-capillary venules was monitorized and blood samples were collected for TNF-α plasma concentrations determination.
View Article and Find Full Text PDFPharmacokinetics and brain dispositions of tacrine and its major bioactive monohydroxylated metabolites in rats.
J Pharm Biomed Anal
March 2012
School of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong Special Administrative Region.
The current study aims to investigate the pharmacokinetics and brain disposition of tacrine and its three major bioactive monohydroxylated metabolites (1-hydroxytacrine, 2-hydroxytacrine and 4-hydroxytacrine). An assay for simultaneous quantification of tacrine and three above metabolites in rat plasma and brain tissue was developed. Four analytes together with internal standard were extracted from rat plasma or brain tissue homogenate by liquid-liquid extraction using ethyl acetate.
View Article and Find Full Text PDFModulation of erythrocyte acetylcholinesterase activity and its association with G protein-band 3 interactions.
J Membr Biol
March 2009
Institute of Biochemistry, University of Lisbon Medical School, Lisbon, Portugal.
Circulating acetylcholine, substrate of membrane acetylcholinesterase (AChE), is known to enhance the band 3 protein degree of phosphorylation. The purpose of this study was to verify whether the band 3 phosphorylation status is associated with a G protein and whether it is an influent factor on AChE enzyme activity. From blood samples of healthy donors, erythrocyte suspensions were prepared and incubated with AChE substrate (acetylcholine) and inhibitor (velnacrine), along with protein tyrosine kinase (PTK) and tyrosine phosphatase (PTP) inhibitors.
View Article and Find Full Text PDFRedox thiol status plays a central role in the mobilization and metabolism of nitric oxide in human red blood cells.
Cell Biol Int
March 2009
Santa Maria Hospital, University of Lisbon Medical School, Portugal.
We assessed the redox thiol status influence on nitric oxide (NO) metabolism and efflux in erythrocytes stimulated with acetylcholinesterase substrate (acetylcholine, ACh) and inhibitor (velnacrine maleate, VM). Erythrocyte suspensions from healthy donors were incubated with increasing concentrations of dithiothreitol (1-50microM), in the presence and absence of acetylcholine/velnacrine (10microM). Levels of NO, nitrite/nitrate, S-nitrosohemoglobin, peroxynitrite and S-nitrosoglutathione were determined by spectrofluorimetric and spectrophotometric methods.
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