Abstract
The synthesis of two derivatives of lignan 4'-O-methylhonokiol (MH), i.e., 4'-methoxy-5-propyl-1,1'-biphenyl-2-ol (III) and 4'-(2-fluoroethoxy)-2-hydroxy-5-propyl-1,1'-biphenyl (VI) has been described. Derivative (VI) demonstrates the highest anti-inflammatory activity in the lipopolysaccharide-induced (LPS-induced) neuroinflammation mouse model. Its effect on the morphological changes in the brain is comparable to that of celecoxib, a well-known nonsteroid anti-inflammatory drug and a selective inhibitor of cyclooxygenase-2 (COX 2).
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ACKNOWLEDGMENTS
The work was performed using the equipment of the Engineering Center of SPSTI (TU).
Funding
The work was supported by grant no. 17-04-02119 from the Russian Foundation of Basic Research.
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All of the animal experiments were adhered to regulations of DIRECTIVE 2010/63/EU on the protection of animals used for scientific purposes and the guidelines of the Ethics Committee of Smorodintsev Research Institute of Influenza.
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Translated by A. Levina
Abbreviations: МН, 4'-О-methylhonokiol; СОХ, cyclooxygenase-2; LPS, lipopolysaccharide; brain WC, brain weight coefficient; HRMS(ESI), High resolution mass spectroscopy in the ESI mode.
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Sivak, K.V., Stosman, K.I., Muzhikyan, A.A. et al. Evaluation of Antiinflammatory Activity of 4'-О-Methylhonokiol Derivatives in a Neuroinflammation Model. Russ J Bioorg Chem 45, 425–429 (2019). https://doi.org/10.1134/S1068162019040113
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DOI: https://doi.org/10.1134/S1068162019040113