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Hepatoprotective Effect of a New FFAR1 Agonist—N-Alkylated Isobornylamine Full article

Journal Molecules
, E-ISSN: 1420-3049
Output data Year: 2023, Volume: 28, Number: 1, Pages: 396 Pages count : 1 DOI: 10.3390/molecules28010396
Tags hepatoprotective effect; bornyl derivatives; FFAR1 agonist; carbon tetrachloride; liver injury
Authors Pon`kina Darya 1 , Kuranov Sergey 1 , Khvostov Mikhail 1 , Zhukova Nataliya 1 , Meshkova Yulia 1 , Marenina Mariya 1 , Luzina Olga 1 , Tolstikova Tatyana 1 , Salakhutdinov Nariman 1
Affiliations
1 N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry of Siberian Branch of Russian Academy of Sciences

Funding (1)

1 Российский Научный Фонд 21-73-00246

Abstract: Free fatty acid receptor-1 (FFAR1) is one of the possible therapeutic targets in the search for new hepatoprotective drugs. FFAR1 agonists were found to have hypolipidemic, antifibrotic, anti-inflammatory, antiproliferative and antioxidant effects in addition to hypoglycemic action. In this work, we conducted a study of the hepatoprotective effect of the compound QS-528 (previously discovered as an agonist of FFAR1) at doses of 60, 90, 120 and 150 mg/kg on carbon tetrachloride (CCl4 )-induced liver injury. At the end of the experiment, a biochemical blood assay demonstrated that the introduction of QS-528 dose-dependently reduces the levels of liver enzymes (AST, ALT and ALKP). Histological and morphometric studies of animals’ livers treated with QS-528 at doses of 120 and 150 mg/kg showed a decrease in degenerative/necrotic changes in hepatocytes and an increase in the regenerative activity of the liver. In addition, no toxicity at a single oral dose of 1000 mg/kg and an increase in HepG2 cell viability in vitro were found. Thus, the compound QS-528 was found to exhibit a hepatoprotective effect against CCl4 -induced toxic liver damage.
Cite: Pon`kina D. , Kuranov S. , Khvostov M. , Zhukova N. , Meshkova Y. , Marenina M. , Luzina O. , Tolstikova T. , Salakhutdinov N.
Hepatoprotective Effect of a New FFAR1 Agonist—N-Alkylated Isobornylamine
Molecules. 2023. V.28. N1. P.396. DOI: 10.3390/molecules28010396 WOS Scopus РИНЦ OpenAlex
Dates:
Submitted: Dec 14, 2022
Published print: Jan 3, 2023
Accepted: Dec 29, 2023
Identifiers:
Web of science: WOS:000910154900001
Scopus: 2-s2.0-85145688178
Elibrary: 60331791
OpenAlex: W4313432992
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