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Ache Inhibitory Effect, Anti-Oxidant and Anti-Inflammatory Properties of Cyclen and L-Dopa Related Compounds: Targeting in Neurodegenerative Disease Publisher



Arabuli L1 ; Lovecka P2 ; Jezek R2 ; Viktorova J2 ; Macek T2 ; Junkova P2 ; Gakhokidze R3 ; Sharifianjazi F1 ; Esmaielkhanian A4 ; Salahshour P1 ; Poursafa P5 ; Sabouri P6
Authors
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Authors Affiliations
  1. 1. Department of Natural Sciences, School of Science and Technology, University of Georgia, Tbilisi, 0171, Georgia
  2. 2. Department of Biochemistry and Microbiology, University of Chemistry and Technology, Technicka 5, Prague, 166 28, Czech Republic
  3. 3. Faculty of Exact and Natural Sciences, Ivane Javakhishvili Tbilisi State University, Tbilisi, 0179, Georgia
  4. 4. Department of Materials and Metallurgical Engineering, Amirkabir University of Technology, Tehran, Iran
  5. 5. Child Growth and Development Research Center, Research Institute for Primordial Prevention of Non-communicable Disease, Isfahan University of Medical Sciences, Isfahan, Iran
  6. 6. School of medicine, Shiraz University of Medical Sciences (SUMS), Shiraz, Iran

Source: Journal of Molecular Structure Published:2023


Abstract

1,4,7,10-tetraazacyclododecane (cyclen), a macrocyclic polyamine, and L-3,4-dihydroxyphenylalanine (L-DOPA), a tyrosine polyphenolic compound are compounds having various applications in medicine, biology, chemistry, etc. Derivatization of these precursor compounds aims to increase their biological activity, blood-brain barrier (BBB) permeability, solubility, binding ability, and lower toxicity. Synthesis and in vitro cytotoxicity of small new peptide-modified cyclen and L-DOPA derivatives were described previously. In the present study, in vitro biological activities such as radical scavenging capacity, anti-inflammatory, and acetylcholinesterase (AChE) inhibitory activities of compounds were evaluated. The results showed that some of them are good candidates for further detailed studies targeting neurodegenerative diseases, such as Alzheimer's and Parkinson's, and their pharmacokinetics and interaction with amyloidal aggregations characterized for neurodegenerative diseases. Dopa-DH-Dopa showed the highest anti-oxidant activity (IC50, 0.12 µM) and Dopa-HH-Dopa as AChE inhibitor (21 µM). Dopa-HH mainly inhibited nitric oxide (NO) production as an inflammatory marker. © 2023 Elsevier B.V.
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